2012
28 February 2012: Appendix 4D - Half Year Consolidated Report
Highlights during the period included the commencement of negotiations with one of the world’s leading
Fast Moving Consumer Goods companies (FMCG) for a wide ranging Joint Development Agreement in
beauty, an expansion of the Company’s oral health partnership with GSK and significant progress in the
development of a range of musculoskeletal patch products that the Company plans to developindependently of its existing international partners.
Commercial Activities
OBJ remains committed to its three-part commercial development program which focuses on
partnering with major international pharmaceutical, cosmetic and FMCG companies, developing
value added products and processes utilising OBJ’s proprietary design and development of its
range of products to be distributed by channel partners.
In 2011, the Company announced that it planned to develop a new range of high value pain and
pain management products utilising the unique benefits of the Company’s technologies. An
extensive internal development program commenced and is currently being supported by an
extensive international market research program based in the UK. Work has continued and the
program has gained increased momentum during the period.
The Company received notification from the US Patent Office in August 2011 that its Dermaportation or powered technology device patent had been allowed. This has subsequently allowed the Company to gain considerable interest from major cosmetic groups for the Company’s new e-skin product range. The potential market exclusivity provided by the US patent has considerably strengthened market interest.
Late in 2011, the Company reported that the previously announced Strategic Alliance program with one of the world's leading Consumer Products companies had further progressed following successful technical evaluations. In October, the Company learned that the FMCG company was seeking world-wide exclusive access rights to OBJ’s technologies in the area of a beauty.
Negotiations commenced regarding the various financial, developmental and investment commitments by the FMCG company to OBJ’s technologies and considerable progress in these negotiations was achieved during the period.
Technology Development
During the period, the Company was rewarded by positive results in its technology development
programs in surface hygiene. Data provided through the Company’s close working relationship with
Bradford University in the UK, has supported an expansion of this work.
The Company’s work with microneedles was also expanded during the period with the receipt of
The Company’s work with microneedles was also expanded during the period with the receipt of
the first positive results of enhanced drug delivery when used in conjunction with microneedles.
This has led to the development of new Intellectual Property and the development of a number of
new product forms that utilise this combination of technologies.3. Capabilities
This has led to the development of new Intellectual Property and the development of a number of
new product forms that utilise this combination of technologies.3. Capabilities
During the period, the Company has focused on a number of technical and development
relationships with major universities in both Australia and UK. This has added substantially to the
technical scope available to the Company’s R&D and partnering programs.
technical scope available to the Company’s R&D and partnering programs.
The trend towards utilising specialised centres of excellence around the world as a means of
expanding the Company’s technical capabilities is expected to continue.
Outlook
The Company has made substantial progress during the period in its key interest areas of
technology utilisation, international partnering and moving towards the development of its own
products. The recent FMCG negotiations, expansion of collaborations with major international
groups and strong consumer research to OBJ’s product plans should result in an exciting and
expansive 2012.
products. The recent FMCG negotiations, expansion of collaborations with major international
groups and strong consumer research to OBJ’s product plans should result in an exciting and
expansive 2012.
Appendix 4D - Half Year Consolidated Report
26 April 2012 - March Shareholder Update
Global FMCG
Negotiations and discussions with the global FMCG, previously announced by the Company are proceeding to the satisfaction of the Company. OBJ’s technical team is working with their international brand groups to determine the scope of the collaborative development programs going forward.
GSK
The Company is pleased to report that the work with GSK in the field of oral health is proceeding with a view to expanding the scope of the current collaboration to include additional key oral health active ingredients. A number of study programs are currently being planned. During the quarter the relationship with GSK was expanded to include discussions with the GSK Pharmaceutical groups in the US.
Micro-needles
The Company has been working with the University of Queensland and in particular Dr Tarl Prow in the development of enhancing micro-needle performance with the addition of OBJ’s ETP magnetic technology. OBJ’s ETP technology, when integrated into a traditional micro-needle delivery system, showed substantially greater drug delivery than micro-needles alone. The resulting technology was the subject of a recent patent application and the results of that work were presented at the PPP Drug delivery Conference in France early in the month by OBJ Director, Dr Chris Quirk. A number of commercial opportunities are now being explored following the scientific presentation.
Knee Guard
The Company’s Musculoskeletal Patch program moved another step forward during the quarter with market research data indicating a commercial opportunity for the Company in both the retail analgesic and sporting markets. New product concepts are now being tested internationally prior to the Company determining the level of investment required to meet the commercial challenge in each category.
Hygiene
The Company’s work in deep hygiene applications continued during the quarter with further encouraging results from the University of Bradford (UK) regarding disinfectant penetration into nonpermeable surfaces under the influences of Field in Motion (FIM). This is early work however the Company is encouraged by progress to date
26 April 2012: March Shareholder Update
18 May 2012:
PROCTER & GAMBLE ENTERS JOINT DEVELOPMENT AGREEMENT
PROCTER & GAMBLE ENTERS JOINT DEVELOPMENT AGREEMENT
OBJ Limited (ASX: OBJ) is pleased to announce that it has signed an exclusive multi‐product Joint Development Agreement (JDA) with The Procter and Gamble Company (P&G) to investigate the development for new products that utilise OBJ’s magnetic enhanced delivery technologies.
P&G is the world’s largest consumer products company with a brand portfolio of over 300
household names – from Gillette to Duracell, Olay to Cover Girl. P&G provides globalmarket access across 180 countries and serves some 4.4 billion consumers daily. P&G’sannual turnover is about $US83 billion/annum.
The two companies began collaborations over a year ago as part of P&G’s Connect+Develop
open innovation program. The signing of the JDA comes after extensive evaluations aimed
at identifying commercially viable opportunities for OBJ’s unique technologies. Under the
JDA, P&G and OBJ will jointly evaluate the application of OBJ’s micro‐array technologies
with products in P&G’s global brand portfolio.
P&G announced:
“P&G’s partnership with OBJ and our joint commitment of collaboration directly aligns with P&G’s business strategies, working to develop new solutions and innovations that can touch and improve the lives of our consumers all over the world,” said Jeff Weedman, P&G Vice President of Global Business Development.
The signing of the JDA follows the successful completion of a series of proof of principle studies where P&G and OBJ focused on determining the most suitable commercial opportunities for OBJ’s unique technology. OBJ Director Mr Glyn Denison commented on the signing of the JDA:
“The JDA is a significant milestone in the Company’s progression from technology development to commercial application. Having the world’s largest consumer company as our consumer product development partner is an exciting development and working in high volume consumer applications plays to the strength of OBJ’s technologies and expertise. We warmly welcome the collaboration with Procter & Gamble and congratulate the technical and marketing team for this achievement.
Procter & Gamble Enters Joint Development Agreement
P&G Beauty 2012
Connect + Develop 10 Year Anniversary
P&G - Connect + Develop
www.futureworks.pg.com
www.pgbeautygroomingscience.com
www.scienceinthebox.com
www.pgperspectives.com
www.pgbioscience.com
www.pg.com
P&G Corporate Newsroom
P&G New "Beauty Recommended" App
Olay: World's Most Valuable Beauty Brand
Olay was named the Top Beauty Brand for 2012 in the recently released BrandFinance® Top 50 Beauty Brands report. First published in 2011, the Brand Finance Top 50 Beauty Brands is released annually and is the first publicly available study analysing the financial value of the world’s top beauty brands.“Procter & Gamble should be rightly proud of their well established and impressive beauty brand, Olay,” said David Haigh, CEO of Brand Finance. “For a brand which demands consumers to ‘Challenge what’s possible’ so too has Olay challenged the expectations of the beauty industry and it is no surprise that this multi-billion-dollar brand is the outright global leader in beauty brands this year.”
Brand Finance PLC, the world’s leading independent brand valuation consultancy firm, evaluates all publicly listed beauty companies to determine the Top 50 Most Valuable Beauty Brands. The valuation is based on a number of financial metrics such as market demand, intangible assets and perpetuity of growth. Based on the data collected by their international team of analysts, they determined that in 2012, Olay is the Most Valuable Beauty Brand. This is the second year in a row Olay has earned the number one spot on the list. See the full list.
“On Olay, we try to be at the forefront of innovation, with new ingredients and technologies that really transform the skin, so it’s a true honour to be recognized for this and ranked as the world’s top beauty brand,” said Michael Kuremsky, P&G’s Global Vice President and General Manager of Skin Care, on the Top 50 Beauty Brands. “This year also marks Olay’s 60th anniversary, so we are grateful that millions of women around the world continue to trust Olay for their skin care needs.”
Pantene also earned a spot in the Top 50 on the list.
“Approaching the London 2012 Games, P&G seeks to maintain its brand awareness not only through sponsoring the American gymnast, Alicia Sacramone, as their beauty brands ambassador, but the brand has also secured an impressive Worldwide Partnership with the International Olympic Committee,” according to the press release issued by Brand Finance, which is headquartered in London.
15 August 2012 - Shareholder Update
OBJ is pleased to provide shareholders with an update of the activities that the Company is undertaking with partnering companies and independent laboratories around the world. OBJ is establishing itself as the selected technology partner for enhanced delivery and product performance to an increasing number of major international corporations in both the pharmaceutical and consumer healthcare fields.
The relationships fostered with these partnering companies over many years is leading to a number of potential commercial undertakings as the testing and development process achieves expected levels of performance.Over recent months, OBJ has worked diligently on its internal testing, external evaluations and working with partners to define the parameters that may ultimately lead to commercial production of the Company’s partners’ products incorporating OBJ’s technologies.
The following outlines key testing and development programs that are at various stages in their lifecycle. All of these programs are progressing satisfactorily.
PROCTER AND GAMBLE
OBJ’s Joint Development Agreement (JDA) with the world’s largest consumer products company announced in May 2012 moved another step forward this month with the Company’s technical team presenting the initial results of an internal development program to the Cincinnati-based product groups. This first program progresses to the next development stage in the USA while a second program involving a new P&G nominated molecule enters development by our R&D team.
ORAL HEALTH
An ongoing relationship with GSK (UK) and OBJ’s own internal development programs in the Oral Health sector advanced with the completion of successful OBJ sponsored ex-vivo studies showing enhanced delivery of key oral health ingredients used in the treatment of teeth hypersensitivity (sensitive teeth) and tooth demineralization (re-hardening). The studies undertaken by the independent Modus Laboratories of the UK demonstrated statistically significant increases in the delivery of key compounds into the tooth enamel in as little as two minutes using a toothbrush-styled applicator incorporating OBJ’s FIM technology.
COSMETIC AND SKIN CARE
The Company’s eM-patch, FIM and eSkin systems are currently attracting interest from a number of US and European cosmetic and skin care companies. Current US-based programs with a number of prestige cosmetic brands were expanded this month with the completion of pre-clinical studies showing commercially important levels of enhanced delivery of a multi-million dollar peptide based cosmetic agent in partner-funded programs. OBJ is now in discussions with a large European-based international partner involved in prestige skin care.
OBJ is working through the various options in the establishment of exclusive development relationships within the industry. Cosmetic and Skin Care remain key areas of activity for the Company.
PHARMACEUTICAL
The Company’s work with one of the world’s largest pharmaceutical companies also advanced with the presentation of the results of a recently fully-funded development in the area of analgesics. The levels of increased transdermal delivery demonstrated by OBJ’s R&D team were in accordance with our partners’ expectations and OBJ’s commercial team is now engaged in discussions which may result in a product development program.
NEW OBJ DELIVERY DEVICES
There is a growing need across all industry sectors for innovative and cost effective measured and controlled dose applicators for various compounds and drugs. The ability to deliver precise volumes of formulations using a single action measured patch opens significant opportunities for utilizing OBJ’s technologies.
OBJ responded to these commercial opportunities last year by developing and filing patents covering a unique platform of new products based on micro-chambers combined with the Company’s existing drug delivery technologies.
During the period OBJ partnered with the Centre for Pharmaceutical Engineering Science at Bradford University, UK in engineering, stability and compliance requirements for these new products and with an Asian-based multi-national manufacturer for low–cost, high-volume manufacturing. Commercial interest from OBJ’s current partners in these new delivery devices has been encouraging
SURFACE HYGIENE
The ability of OBJ’s technologies to force anti-microbial and disinfectant agents deep into the micro-cracks and fissures in hard and non-porous surfaces creates a potentially valuable market in the hospital, industrial and home markets for a new generation of hygiene products containing OBJ’s technologies.
A testing program is underway and took a step forward with a successful follow-up study by a major UK University showing significantly greater antiseptic penetration into these key microchambers by OBJ’s FIM technology compared with traditional disinfection methods. The ability to increase the efficacy of disinfectant agents without additional chemical or toxicity effects opens a potentially important non-medical area for OBJ. The Company is encouraged by the first potential non-biological applications for its technologies and believes this could be a potentially attractive application. Work continues in this key commercial sector.
MICRO-NEEDLES
The Company’s work with the
University of Queensland in
enhancing the passage of drug from
the skin into the viable epidermis
following micro-needle application
continues. The previous
encouraging results by the
University are now being developed
into more potentially commercially
focused opportunities. This forms
part of the Company’s technology
diversification program.
30 August 2012 - Supplementary Appendix 4E information - Reporting period to June 2012
Commentary of the results for the period:
Procter and Gamble
Engaging with Procter and Gamble (P&G) on a regular basis resulted in wide ranging discussions with various product groups to determine the most suitable potential commercial targets for OBJ’s technologies.
Discussions and negotiations continued for some time before a final Joint Development Agreement (JDA) was agreed and announced in May 2012.
OBJ’s technical team has been working closely with P&G’s product groups towards clinical trials, planned for later in 2012.
GlaxoSmithKline (UK)
During the same period, the Company reported continuing successes in the Oral Health field in its exclusive
collaboration with GSK in the Caries (tooth decay) field. Highly encouraging ex vivo results encouraged an
expansion of this work and in March the Company announced an expansion of those programmes to include
toothpaste ingredients in other sectors of the oral health.
Other Collaborations
In addition to the those outlined above, the Company maintained close working relationship with a number of
major collaborative partners across the cosmetic, analgesic and pharmaceutical fields.
Internal Products Strategy
The Company has been active in the development of its own product portfolio for some time, as the
commercial flexibly provided by an “own products” initiative may provide an opportunity for earlier cash flow
than partner sponsored programmes.
The Company had previously announced that it had chosen the musculoskeletal and pain patch sectors as the
first product offerings. Development programmes moved another step forward with UK based consumer and
concept research data indicating commercial opportunities for both initiatives. Expanded new product concept
testing was initiated during the period to assist in defining the product needs of the international market.
Technical and Technology
Micro-needles
Prow of the University of Queensland has shown that OBJ’s FIM technology had a substantial effect on the
bioavailability of certain drugs following application by Micro-needles. The results of this work were presented
at the international PPP Drug Delivery Conference in France by Director Dr Chris Quirk.
Surface Care
The Company’s ambitions in industrial, hospital and household hygiene applications continued during the
period with further encouraging results from the University of Bradford (UK) demonstrating the feasibility of
enhanced disinfectant penetration of non-permeable surfaces under the influences of Field in Motion (FIM).
2012 Annual Report
26 July 2012 - seek.com.au - Market Development Manager - Sports Medicine
Australia's leading transdermal patch development company seeks an experienced and motivated Market Development Manager to lead the final development stages and manage the international roll-out of a unique platform of sports and consumer pain and injury management products. This new platform of sports and retail medical products will create a new category in the international professional and amateur sports medicine, rehabilitation and injury treatment markets.
The products are currently being developed by one of the world’s leading transdermal drug delivery companies in conjunction with international sports medical and formulation experts. The unique selling features and benefits provided by the Australian developed transdermal technology will provide new levels of features, functions and performance beyond the capabilities of existing competitor products.
Papers
(The following list of publications cite authors who are collaborating with OBJ Limited, but the work referenced may not neccessarily be affiliated with the company.)
Nanomedicine (Lond) 2012 Apr;7 (4): 541-51. [IF:6.202]
(The following list of publications cite authors who are collaborating with OBJ Limited, but the work referenced may not neccessarily be affiliated with the company.)
Nanomedicine (Lond) 2012 Apr;7 (4): 541-51. [IF:6.202]
High-pressure freezing/freeze substitution and
transmission electron microscopy for characterization of metal oxide
nanoparticles within sunscreens.
Australian Microscopy & Microanalysis Research Facility
& Australian Institute for Bioengineering & Nanotechnology, Cnr College
& Cooper Roads, The University of Queensland, Brisbane, Queensland, 4072,
Australia. m.butler1@uq.edu.au
Abstract
To date, the description of a single, suitable method to observe in detail metal oxide nanoparticles in situ within sunscreens is currently lacking, despite growing concern as to how they interact with humans. This study explores the usefulness of transmission electron microscopy to characterize the nanoparticles in sunscreens. High-pressure freezing then freeze substitution was used to prepare resin-embedded commercial sunscreen samples, and ultrathin sections of these were observed with transmission electron microscopy. Conventional room temperature processing for resin embedding was also trialed. High-pressure frozen/freeze substituted samples provided clear visualization of the size and shape of the nanoparticles and agglomerates and allowed further characterization of the composition and crystal form of the metal oxides, while conventionally processed chemically fixed samples were subject to distribution/agglomeration artifacts. Transmission electron microscopy of high-pressure frozen/freeze substituted samples is an ideal method to completely observe metal oxide nanoparticles in situ in sunscreens.
To date, the description of a single, suitable method to observe in detail metal oxide nanoparticles in situ within sunscreens is currently lacking, despite growing concern as to how they interact with humans. This study explores the usefulness of transmission electron microscopy to characterize the nanoparticles in sunscreens. High-pressure freezing then freeze substitution was used to prepare resin-embedded commercial sunscreen samples, and ultrathin sections of these were observed with transmission electron microscopy. Conventional room temperature processing for resin embedding was also trialed. High-pressure frozen/freeze substituted samples provided clear visualization of the size and shape of the nanoparticles and agglomerates and allowed further characterization of the composition and crystal form of the metal oxides, while conventionally processed chemically fixed samples were subject to distribution/agglomeration artifacts. Transmission electron microscopy of high-pressure frozen/freeze substituted samples is an ideal method to completely observe metal oxide nanoparticles in situ in sunscreens.
PMID: 22394188 [Pubmed - MEDLINE]
__________
Skin
Res Technol 2012 Jun; [IF:1.606]
Enhanced sonophoretic delivery of 5-aminolevulinic acid:
preliminary human ex vivo permeation data.
Curtin Health Innovation Research Institute, School of
Pharmacy, Curtin University, Perth, WA, Australia.
Abstract
BACKGROUND/AIMS: 5-Aminolevulinate (ALA) is an important photodynamic therapy drug for the treatment of actinic keratoses and other non-melanoma skin cancers in cosmetically sensitive areas. One limitation of this drug is a relatively high recurrence rate. Our aim was to evaluate the feasibility of ultrasound augmented ALA delivery in excised human skin. MATERIALS AND METHODS: An ultrasonic delivery device was used to enhance radiolabelled ALA into excised skin. Quantification of ALA was performed after passive and ultrasonic ALA delivery. Transepidermal water loss was used as a measure of barrier function before and after ultrasonic treatment. RESULTS: We found that ultrasonic treatment dramatically increased the mean cumulative amount of ALA to P< 0.0001 from 4 to 8 h when compared to passive ALA treatment. The flux was calculated to be 54.8 ± 8.0 μg/cm(2) h with ultrasound treatment. TEWL increased nearly two-fold, from 12.3 to 21.0, after ultrasound treatment. CONCLUSION: Our study supports the use of ultrasound for improved ALA delivery by showing significant improvements in the cumulative drug load and flux via combined ultrasound and ALA treatment.
BACKGROUND/AIMS: 5-Aminolevulinate (ALA) is an important photodynamic therapy drug for the treatment of actinic keratoses and other non-melanoma skin cancers in cosmetically sensitive areas. One limitation of this drug is a relatively high recurrence rate. Our aim was to evaluate the feasibility of ultrasound augmented ALA delivery in excised human skin. MATERIALS AND METHODS: An ultrasonic delivery device was used to enhance radiolabelled ALA into excised skin. Quantification of ALA was performed after passive and ultrasonic ALA delivery. Transepidermal water loss was used as a measure of barrier function before and after ultrasonic treatment. RESULTS: We found that ultrasonic treatment dramatically increased the mean cumulative amount of ALA to P< 0.0001 from 4 to 8 h when compared to passive ALA treatment. The flux was calculated to be 54.8 ± 8.0 μg/cm(2) h with ultrasound treatment. TEWL increased nearly two-fold, from 12.3 to 21.0, after ultrasound treatment. CONCLUSION: Our study supports the use of ultrasound for improved ALA delivery by showing significant improvements in the cumulative drug load and flux via combined ultrasound and ALA treatment.
PMID: 22672142 [Pubmed - Publisher]
____
Int J
Cosmet Sci 2012 Sep
Predicting skin penetration of actives from complex
cosmetic formulations: An evaluation of inter-formulation and inter-active
effects during formulation optimization for transdermal delivery#
Therapeutics Research Centre, School of Medicine,
University of Queensland, Princess Alexandra Hospital, Woolloongabba, QLD, 4102,
Australia; JW Solutions, Gasthuispolderweg 30, 2807, LL, Gouda, The
Netherlands.
Abstract
Twenty products, containing a radiolabelled form of each active in typical cosmetic formulations, were made and applied to female human epidermal membranes mounted in Franz diffusion cells for 48 hr under 'in use" conditions. The products consisted of combinations of five formulations (a hydro-alcoholic gel, an oil in water emulsion, a water in oil emulsion, a micro-emulsion and an oil) with four model drug actives (testosterone, hydrocortisone, 5-fluorouracil and ketoconazole). Steady state flux appeared to be reached by 8 hr and maintained for all products, other than for the micro-emulsions, consistent with the actives being present in the residual formulation on the skin at saturation. The recovery for each active at the end of the 48 hr study (from a series of stratum corneum tape strips, the remaining skin, cumulative amount penetrating into the receptor solution, product washed from the skin and on the donor chamber cap) ranged from 86.5% to 100.6%. The rank order of the fluxes for the actives from the hydro-alcoholic gel is consistent with the known active molecular size and polarity determinants for maximum epidermal flux. Actives with similar steady state (maximum) fluxes from a range of formulations had retention in the stratum corneum and similar transport rate constants through the stratum corneum. The micro-emulsion formulation significantly enhanced both the stratum corneum steady-state flux and transport rate constant for 5-fluorouracil, hydrocortisone and testosterone. The penetration flux of each active could be related to its size and polarity and appeared maximal when the actives in the different cosmetic formulations applied to the skin under "in use" conditions were likely to remain in the residual product on the skin as a saturated solution after solvent evaporation. Enhanced penetration fluxes can be achieved by formulation selection and an appropriate choice /mix of emollients/adjuvants. The principles described here provide a framework for understanding the delivery of cosmetic ingredients from various formulations. © 2012 Society of Cosmetic Scientists and the Société Française de Cosmétologie.
Twenty products, containing a radiolabelled form of each active in typical cosmetic formulations, were made and applied to female human epidermal membranes mounted in Franz diffusion cells for 48 hr under 'in use" conditions. The products consisted of combinations of five formulations (a hydro-alcoholic gel, an oil in water emulsion, a water in oil emulsion, a micro-emulsion and an oil) with four model drug actives (testosterone, hydrocortisone, 5-fluorouracil and ketoconazole). Steady state flux appeared to be reached by 8 hr and maintained for all products, other than for the micro-emulsions, consistent with the actives being present in the residual formulation on the skin at saturation. The recovery for each active at the end of the 48 hr study (from a series of stratum corneum tape strips, the remaining skin, cumulative amount penetrating into the receptor solution, product washed from the skin and on the donor chamber cap) ranged from 86.5% to 100.6%. The rank order of the fluxes for the actives from the hydro-alcoholic gel is consistent with the known active molecular size and polarity determinants for maximum epidermal flux. Actives with similar steady state (maximum) fluxes from a range of formulations had retention in the stratum corneum and similar transport rate constants through the stratum corneum. The micro-emulsion formulation significantly enhanced both the stratum corneum steady-state flux and transport rate constant for 5-fluorouracil, hydrocortisone and testosterone. The penetration flux of each active could be related to its size and polarity and appeared maximal when the actives in the different cosmetic formulations applied to the skin under "in use" conditions were likely to remain in the residual product on the skin as a saturated solution after solvent evaporation. Enhanced penetration fluxes can be achieved by formulation selection and an appropriate choice /mix of emollients/adjuvants. The principles described here provide a framework for understanding the delivery of cosmetic ingredients from various formulations. © 2012 Society of Cosmetic Scientists and the Société Française de Cosmétologie.
PMID: 22950455 [Pubmed - Publisher]
_____
Br J Dermatol
2012 Aug;167 (2): 270-9. [IF:4.353]
In vivo assessment of chronological ageing and photoageing
in forearm skin using reflectance confocal microscopy.
1Dermatology Research Centre, The University of Queensland,
Brisbane, Qld, Australia Dermatology Unit, First Medical Department, Arcispedale
Santa Maria Nuova, Reggio, Emilia, Italy Department of Dermatology, University
of Modena and Reggio Emilia, Modena, Italy.
Abstract
Background Skin ageing is a complex process due to intrinsic chronological factors (chronoageing) and extrinsic environmental factors. The primary extrinsic factor is cumulative ultraviolet (UV) exposure, and is therefore termed photoageing. The current standards for measuring cumulative sun damage are biopsy histology and skin microtopography. However, skin biopsies are too invasive for population studies and skin replicas render only superficial skin architecture data. Reflectance confocal microscopy (RCM) is a noninvasive imaging tool that allows for in vivo imaging of the skin at quasihistological resolution. Objectives To define and identify RCM features associated with chronological ageing and photoageing on the forearm in two age groups with different skin phototypes and to assess whether these results agree with previous findings. Methods We obtained RCM images of dorsal and volar nonlesional skin of the lower forearm of 75 individuals with skin Fitzpatrick phototypes I-III in two age groups (20-30 years and 50-60 years). From each participant and body site, 21 RCM features were assessed and statistically significant differences between the two age groups and different forearm sites determined. Results RCM enabled identification of changes in architecture, cell morphology and extracellular matrix (collagen) at the level of the epidermis, dermoepidermal junction and papillary dermis. Changes that were correlated with chronological ageing and which were aggravated on the UV-exposed dorsal forearm were: loss of small skin furrows resulting in wider and less intersecting furrows; irregularity of the epidermal honeycomb pattern; irregularly distributed (mottled) pigmented keratinocytes/melanocytes; irregularity of the papillary rings and/or effacement of the rete ridges; and loss of thin collagen fibres and presence of collagen clods. Conclusion We have tested previously reported and new parameters for skin ageing evaluation by RCM, and identified 15 statistically significant RCM features that can be used to quantify ageing and photoageing in forearm skin noninvasively.
Background Skin ageing is a complex process due to intrinsic chronological factors (chronoageing) and extrinsic environmental factors. The primary extrinsic factor is cumulative ultraviolet (UV) exposure, and is therefore termed photoageing. The current standards for measuring cumulative sun damage are biopsy histology and skin microtopography. However, skin biopsies are too invasive for population studies and skin replicas render only superficial skin architecture data. Reflectance confocal microscopy (RCM) is a noninvasive imaging tool that allows for in vivo imaging of the skin at quasihistological resolution. Objectives To define and identify RCM features associated with chronological ageing and photoageing on the forearm in two age groups with different skin phototypes and to assess whether these results agree with previous findings. Methods We obtained RCM images of dorsal and volar nonlesional skin of the lower forearm of 75 individuals with skin Fitzpatrick phototypes I-III in two age groups (20-30 years and 50-60 years). From each participant and body site, 21 RCM features were assessed and statistically significant differences between the two age groups and different forearm sites determined. Results RCM enabled identification of changes in architecture, cell morphology and extracellular matrix (collagen) at the level of the epidermis, dermoepidermal junction and papillary dermis. Changes that were correlated with chronological ageing and which were aggravated on the UV-exposed dorsal forearm were: loss of small skin furrows resulting in wider and less intersecting furrows; irregularity of the epidermal honeycomb pattern; irregularly distributed (mottled) pigmented keratinocytes/melanocytes; irregularity of the papillary rings and/or effacement of the rete ridges; and loss of thin collagen fibres and presence of collagen clods. Conclusion We have tested previously reported and new parameters for skin ageing evaluation by RCM, and identified 15 statistically significant RCM features that can be used to quantify ageing and photoageing in forearm skin noninvasively.
PMID: 22428802 [Pubmed - In-Data-Review]
_____
Int J
Pharm 2012 Oct;435 (1): 93-7. [IF:3.607]
Fluorescence recovery after photo-bleaching as a method to
determine local diffusion coefficient in the stratum corneum.
School of Biomolecular and Physical Sciences, Griffith
University, Qld 4222, Australia.
Abstract
Fluorescence recovery after photo-bleaching experiments were performed in human stratum corneum in vitro. Fluorescence multiphoton tomography was used, which allowed the dimensions of the photobleached volume to be at the micron scale and located fully within the lipid phase of the stratum corneum. Analysis of the fluorescence recovery data with simplified mathematical models yielded the diffusion coefficient of small molecular weight organic fluorescent dye Rhodamine B in the stratum corneum lipid phase of about (3-6)×10(-9)cm(2)s(-1). It was concluded that the presented method can be used for detailed analysis of localised diffusion coefficients in the stratum corneum phases for various fluorescent probes.
Fluorescence recovery after photo-bleaching experiments were performed in human stratum corneum in vitro. Fluorescence multiphoton tomography was used, which allowed the dimensions of the photobleached volume to be at the micron scale and located fully within the lipid phase of the stratum corneum. Analysis of the fluorescence recovery data with simplified mathematical models yielded the diffusion coefficient of small molecular weight organic fluorescent dye Rhodamine B in the stratum corneum lipid phase of about (3-6)×10(-9)cm(2)s(-1). It was concluded that the presented method can be used for detailed analysis of localised diffusion coefficients in the stratum corneum phases for various fluorescent probes.
PMID: 22326252 [Pubmed - In-Data-Review]
Pharm Res 2012 Aug;
[IF:4.456]
Effect of Vehicles on the Maximum Transepidermal Flux of
Similar Size Phenolic Compounds.
School of Pharmacy and Medical Sciences, University of
South Australia, Adelaide, SA, 5001, Australia.
Abstract
PURPOSE: In principle, maximum transepidermal fluxes of solutes should be similar for different vehicles, except when the solute or vehicle modifies the skin. Here we estimated maximum flux, stratum corneum solubility, diffusivity and permeability coefficient for a range of similarly sized phenolic compounds with varying lipophilicity from polar and lipophilic vehicles. METHODS: Maximum flux and other skin transport parameters through human epidermis were obtained from lipophilic vehicles (mineral oil (MO) and isopropyl myristate (IPM)) and compared with values from water and propylene glycol (PG)-water solutions. Solvent uptake and changes in stratum corneum infrared spectroscopy and multiphoton microscopy imaging were also investigated. RESULTS: Maximum fluxes for MO and water were similar but IPM has a higher value for more polar phenols due to a higher diffusivity and PG-water had a higher flux due to higher solubility in the stratum corneum. Whereas maximum flux for various phenols was directly related to solubility in the stratum corneum independent of vehicle, increasing phenol lipophilicity increased and decreased permeability coefficient for aqueous solvents and lipophilic solvents, respectively. CONCLUSION: The maximum fluxes for phenols with a similar molecular size and varying lipophilicity were comparable between water and MO vehicles but higher for IPM and PG-water mixtures.
PURPOSE: In principle, maximum transepidermal fluxes of solutes should be similar for different vehicles, except when the solute or vehicle modifies the skin. Here we estimated maximum flux, stratum corneum solubility, diffusivity and permeability coefficient for a range of similarly sized phenolic compounds with varying lipophilicity from polar and lipophilic vehicles. METHODS: Maximum flux and other skin transport parameters through human epidermis were obtained from lipophilic vehicles (mineral oil (MO) and isopropyl myristate (IPM)) and compared with values from water and propylene glycol (PG)-water solutions. Solvent uptake and changes in stratum corneum infrared spectroscopy and multiphoton microscopy imaging were also investigated. RESULTS: Maximum fluxes for MO and water were similar but IPM has a higher value for more polar phenols due to a higher diffusivity and PG-water had a higher flux due to higher solubility in the stratum corneum. Whereas maximum flux for various phenols was directly related to solubility in the stratum corneum independent of vehicle, increasing phenol lipophilicity increased and decreased permeability coefficient for aqueous solvents and lipophilic solvents, respectively. CONCLUSION: The maximum fluxes for phenols with a similar molecular size and varying lipophilicity were comparable between water and MO vehicles but higher for IPM and PG-water mixtures.
PMID: 22923350 [Pubmed - Publisher]
Biomed Opt Express
2011 Dec;2 (12): 3321-33. 全文索取
Characterization of optical properties of ZnO
nanoparticles for quantitative imaging of transdermal transport.
Abstract
Widespread applications of ZnO nanoparticles (NP) in sun-blocking cosmetic products have raised safety concerns related to their potential transdermal penetration and resultant cytotoxicity. Nonlinear optical microscopy provides means for high-contrast imaging of ZnO NPs lending in vitro and in vivo assessment of the nanoparticle uptake in skin, provided their nonlinear optical properties are characterized. We report on this characterization using ZnO NP commercial product, Zinclear, mean-sized 21 nm. Two-photon action cross-section of this bandgap material (E(bg) = 3.37 eV, λ(bg) = 370 nm) measured by two techniques yielded consistent results of [Formula: see text] = 6.2 ± 0.8 μGM at 795 nm, and 32 ± 6 μGM at 770 nm per unit ZnO crystal cell, with the quantum efficiency of [Formula: see text] = (0.9 ± 0.2) %. In order to demonstrate the quantitative imaging, nonlinear optical microscopy images of the excised human skin topically treated with Zinclear were acquired and processed using [Formula: see text] and [Formula: see text]values yielding nanoparticle concentration map in skin. Accumulations of Zinclear ZnO nanoparticles were detected only on the skin surface and in skin folds reaching concentrations of 800 NPs per μm(3).
Widespread applications of ZnO nanoparticles (NP) in sun-blocking cosmetic products have raised safety concerns related to their potential transdermal penetration and resultant cytotoxicity. Nonlinear optical microscopy provides means for high-contrast imaging of ZnO NPs lending in vitro and in vivo assessment of the nanoparticle uptake in skin, provided their nonlinear optical properties are characterized. We report on this characterization using ZnO NP commercial product, Zinclear, mean-sized 21 nm. Two-photon action cross-section of this bandgap material (E(bg) = 3.37 eV, λ(bg) = 370 nm) measured by two techniques yielded consistent results of [Formula: see text] = 6.2 ± 0.8 μGM at 795 nm, and 32 ± 6 μGM at 770 nm per unit ZnO crystal cell, with the quantum efficiency of [Formula: see text] = (0.9 ± 0.2) %. In order to demonstrate the quantitative imaging, nonlinear optical microscopy images of the excised human skin topically treated with Zinclear were acquired and processed using [Formula: see text] and [Formula: see text]values yielding nanoparticle concentration map in skin. Accumulations of Zinclear ZnO nanoparticles were detected only on the skin surface and in skin folds reaching concentrations of 800 NPs per μm(3).
PMID: 22162822 [Pubmed - PubMed-not-MEDLINE]
FASEB
J 2012 Sep;26 (9): 3901-15. [IF:6.515]
In vivo evidence for a novel pathway of vitamin D3
metabolism initiated by P450scc and modified by CYP27B1.
1Department of Pathology; 930 Madison Ave., RM525; Memphis,
TN 38163, USA. aslominski@uthsc.edu.
Abstract
We define previously unrecognized in vivo pathways of vitamin D(3) (D3) metabolism generating novel D3-hydroxyderivatives different from 25-hydroxyvitamin D(3) [25(OH)D3] and 1,25(OH)(2)D3. Their novel products include 20-hydroxyvitamin D(3) [20(OH)D3], 22(OH)D3, 20,23(OH)(2)D3, 20,22(OH)(2)D3, 1,20(OH)(2)D3, 1,20,23(OH)(3)D3, and 17,20,23(OH)(3)D3 and were produced by placenta, adrenal glands, and epidermal keratinocytes. We detected the predominant metabolite [20(OH)D3] in human serum with a relative concentration ∼20 times lower than 25(OH)D3. Use of inhibitors and studies performed with isolated mitochondria and purified enzymes demonstrated involvement of the steroidogenic enzyme cytochrome P450scc (CYP11A1) as well as CYP27B1 (1α-hydroxylase). In placenta and adrenal glands with high CYP11A1 expression, the predominant pathway was D3 → 20(OH)D3 → 20,23(OH)(2)D3 → 17,20,23(OH)(3)D3 with further 1α-hydroxylation, and minor pathways were D3 → 25(OH)D3 → 1,25(OH)(2)D3 and D3 → 22(OH)D3 → 20,22(OH)(2)D3. In epidermal keratinocytes, we observed higher proportions of 22(OH)D3 and 20,22(OH)(2)D3. We also detected endogenous production of 20(OH)D3, 22(OH) D3, 20,23(OH)(2)D3, 20,22(OH)(2)D3, and 17,20,23(OH)(3)D3 by immortalized human keratinocytes. Thus, we provide in vivo evidence for novel pathways of D3 metabolism initiated by CYP11A1, with the product profile showing organ/cell type specificity and being modified by CYP27B1 activity. These findings define the pathway intermediates as natural products/endogenous bioregulators and break the current dogma that vitamin D is solely activated through the sequence D3 → 25(OH)D3 → 1,25(OH)(2)D3.-Slominski, A. T., Kim, T.-K., Shehabi, H. Z., Semak, I., Tang, E. K. Y., Nguyen, M. N., Benson, H. A. E., Korik, E., Janjetovic, Z., Chen, J., Yates, C. R., Postlethwaite, A., Li, W., Tuckey, R. C. In vivo evidence for a novel pathway of vitamin D(3) metabolism initiated by P450scc and modified by CYP27B1.
We define previously unrecognized in vivo pathways of vitamin D(3) (D3) metabolism generating novel D3-hydroxyderivatives different from 25-hydroxyvitamin D(3) [25(OH)D3] and 1,25(OH)(2)D3. Their novel products include 20-hydroxyvitamin D(3) [20(OH)D3], 22(OH)D3, 20,23(OH)(2)D3, 20,22(OH)(2)D3, 1,20(OH)(2)D3, 1,20,23(OH)(3)D3, and 17,20,23(OH)(3)D3 and were produced by placenta, adrenal glands, and epidermal keratinocytes. We detected the predominant metabolite [20(OH)D3] in human serum with a relative concentration ∼20 times lower than 25(OH)D3. Use of inhibitors and studies performed with isolated mitochondria and purified enzymes demonstrated involvement of the steroidogenic enzyme cytochrome P450scc (CYP11A1) as well as CYP27B1 (1α-hydroxylase). In placenta and adrenal glands with high CYP11A1 expression, the predominant pathway was D3 → 20(OH)D3 → 20,23(OH)(2)D3 → 17,20,23(OH)(3)D3 with further 1α-hydroxylation, and minor pathways were D3 → 25(OH)D3 → 1,25(OH)(2)D3 and D3 → 22(OH)D3 → 20,22(OH)(2)D3. In epidermal keratinocytes, we observed higher proportions of 22(OH)D3 and 20,22(OH)(2)D3. We also detected endogenous production of 20(OH)D3, 22(OH) D3, 20,23(OH)(2)D3, 20,22(OH)(2)D3, and 17,20,23(OH)(3)D3 by immortalized human keratinocytes. Thus, we provide in vivo evidence for novel pathways of D3 metabolism initiated by CYP11A1, with the product profile showing organ/cell type specificity and being modified by CYP27B1 activity. These findings define the pathway intermediates as natural products/endogenous bioregulators and break the current dogma that vitamin D is solely activated through the sequence D3 → 25(OH)D3 → 1,25(OH)(2)D3.-Slominski, A. T., Kim, T.-K., Shehabi, H. Z., Semak, I., Tang, E. K. Y., Nguyen, M. N., Benson, H. A. E., Korik, E., Janjetovic, Z., Chen, J., Yates, C. R., Postlethwaite, A., Li, W., Tuckey, R. C. In vivo evidence for a novel pathway of vitamin D(3) metabolism initiated by P450scc and modified by CYP27B1.
PMID: 22683847 [Pubmed - In-Data-Review]
J Pharm
Sci 2012 Jan;101 (1): 233-44. [IF:3.031]
Enhanced immune response against pertussis toxoid by
IgA-loaded chitosan-dextran sulfate nanoparticles.
School of Pharmacy, CHIRI, Western Australia
Biomedical Research Institute, Curtin University, Perth, Western Australia 6845,
Australia.
Abstract
The objective of the present study was to evaluate immunological activities of chitosan-dextran sulfate (CS-DS) nanoparticle formulation of pertussis toxoid (PTXd) and its combination with a potential immunological adjuvant, immunoglobulin A (IgA). CS-DS nanoparticles were prepared using a complex coacervation (polyelectrolyte complexation) technique. CS-DS nanoparticle formulations with size and zeta potential in a range of 300-350 nm and +40-+55 mV, respectively, were obtained. An entrapment efficiency of more than 90% was obtained for pertussis toxin and IgA in CS-DS nanoparticles. All loaded nanoparticle formulations showed less than 20% of release within 24 h in in vitro release studies. The immunological evaluation of developed formulations in female Balb/c mice groups showed that the CS-DS nanoparticles formulations induced significantly higher serum IgG and IgG1 titers (p < 0.05) as compared with conventional alum-adjuvanted PTXd formulation administered by subcutaneous route. This study indicated the potential of CS-DS nanoparticles to be a simple and effective particulate delivery system with in-built immunological adjuvant property for acellular protein antigens. The study also revealed the potential important role of IgA-loaded CS-DS nanoparticles as a novel immunological adjuvant for vaccine delivery.
The objective of the present study was to evaluate immunological activities of chitosan-dextran sulfate (CS-DS) nanoparticle formulation of pertussis toxoid (PTXd) and its combination with a potential immunological adjuvant, immunoglobulin A (IgA). CS-DS nanoparticles were prepared using a complex coacervation (polyelectrolyte complexation) technique. CS-DS nanoparticle formulations with size and zeta potential in a range of 300-350 nm and +40-+55 mV, respectively, were obtained. An entrapment efficiency of more than 90% was obtained for pertussis toxin and IgA in CS-DS nanoparticles. All loaded nanoparticle formulations showed less than 20% of release within 24 h in in vitro release studies. The immunological evaluation of developed formulations in female Balb/c mice groups showed that the CS-DS nanoparticles formulations induced significantly higher serum IgG and IgG1 titers (p < 0.05) as compared with conventional alum-adjuvanted PTXd formulation administered by subcutaneous route. This study indicated the potential of CS-DS nanoparticles to be a simple and effective particulate delivery system with in-built immunological adjuvant property for acellular protein antigens. The study also revealed the potential important role of IgA-loaded CS-DS nanoparticles as a novel immunological adjuvant for vaccine delivery.
PMID: 21953499 [Pubmed - MEDLINE]
Biopolymers 2011 ;96 (2): 166-71.
[IF:2.572]
Enhanced transdermal delivery of 5-aminolevulinic
acid and a dipeptide by iontophoresis.
Curtin Health Innovation Research Institute, School
of Pharmacy, Curtin University, Perth, Western Australia.
Abstract
Poor skin permeability limits the application of peptides to the skin. Enhanced skin permeation could facilitate the development of new therapies for dermatologic and cosmeceutical applications. The aim of this study was to investigate the application of iontophoresis to the delivery of small peptide model compounds (5-aminolevulinic acid and L-alanine-L-tryptophan) across human skin. Under the conditions tested, iontophoresis increased the in vitro permeability coefficient of ALA.HCl across human epidermis from 7 X 10(-5) cm/h with passive diffusion to 110 x 10(-5) cm/h with iontophoresis. D-Glucose permeation elucidated the iontophoretic electrotransport of ALA.HCl to have contributions of both electrorepulsion and electroosmosis. The L-alanine-L-tryptophan permeability coefficient was increased from 1.5 x 10(-5) cm/h to 35 x 10(-5) cm/h with iontophoretic application. Iontophoretic delivery of the dipeptide increased markedly at lower pH because of an increase in electrorepulsive transport. The study demonstrates that iontophoresis can enhance epidermal permeation of a small peptide and peptide-like drug by up to 15- and 22-fold under the conditions tested.
Poor skin permeability limits the application of peptides to the skin. Enhanced skin permeation could facilitate the development of new therapies for dermatologic and cosmeceutical applications. The aim of this study was to investigate the application of iontophoresis to the delivery of small peptide model compounds (5-aminolevulinic acid and L-alanine-L-tryptophan) across human skin. Under the conditions tested, iontophoresis increased the in vitro permeability coefficient of ALA.HCl across human epidermis from 7 X 10(-5) cm/h with passive diffusion to 110 x 10(-5) cm/h with iontophoresis. D-Glucose permeation elucidated the iontophoretic electrotransport of ALA.HCl to have contributions of both electrorepulsion and electroosmosis. The L-alanine-L-tryptophan permeability coefficient was increased from 1.5 x 10(-5) cm/h to 35 x 10(-5) cm/h with iontophoretic application. Iontophoretic delivery of the dipeptide increased markedly at lower pH because of an increase in electrorepulsive transport. The study demonstrates that iontophoresis can enhance epidermal permeation of a small peptide and peptide-like drug by up to 15- and 22-fold under the conditions tested.
PMID: 20665477 [Pubmed - MEDLINE]
Pubmed: Tarl Prow
A "plug-and-play" approach to the preparation of transparent luminescent hybrid materials based on poly(methyl methacrylate), a calix[4]arene cross-linking agent, and terbium ions.
Driscoll CR, Reid BL, McIldowie MJ, Muzzioli S, Nealon GL, Skelton BW, Stagni S, Brown DH, Massi M, Ogden MI.
Abstract
Abstract
A novel methodology to prepare transparent luminescent hybrid materials is reported. Using a calixarene ionophore as a PMMA cross-linker avoids problems, such as phase segregation, and produces a polymer monolith that can be loaded with the metal ion required for luminescence post-synthesis. This approach is versatile and will simplify the production of such materials.
Interesting to note some recent work with metabotropic glutamate receptors (mGluRs)...
Newly Discovered Scaffold Supports Turning Pain Off
ScienceDaily (July 26, 2012) — Johns Hopkins scientists have discovered a "scaffolding" protein that holds together multiple elements in a complex system responsible for regulating pain, mental illnesses and other complex neurological problems.
Preso1 (green) and mGluR5 (red) appear in the same location inside a neuron.
(Credit: Image courtesy of Johns Hopkins Medicine)
The finding, published in the May 6 issue of Nature Neuroscience, could give researchers a new target for drugs to treat these often-intractable conditions.
The discovery, detailed in a study led by neuroscience professor Paul Worley, M.D., of the Johns Hopkins University School of Medicine, focuses on a family of proteins called group 1 metabotropic glutamate receptors (mGluRs) that lie on the surfaces of nerve cells. When these receptors lock in glutamate, a chemical that neurons use to communicate, it encourages neurons to fire.
Without a way to turn off these receptors, neurons would remain active indefinitely, keeping pain and other responses going long after they're useful. Previous research suggested that these mGluRs need to bind to another protein called Homer to shut down, and that this binding is stronger after other molecules called protein kinases modify the receptors. However, Worley explains, thus far it's been unclear exactly how all these different players come together.
Seeking the mechanism behind this phenomenon, Worley and his colleagues started with a series of experiments to see what other proteins the mGluRs and Homer were binding with in rat brains. Their search turned up a third protein called Preso1, which bound to both mGluRs and Homer. A search in genetic databases shows that the gene responsible for making Preso1 is present in animals ranging from fruit flies to people, highlighting its importance in a wide variety of creatures.
To figure out what Preso1 does, the researchers performed another series of experiments to examine behavior of neurons that produced both mGluRs and Homer. They found that when these neurons also expressed Preso1, the mGluRs bound Homer more efficiently, suggesting that Preso1 might somehow increase modification by protein kinases.
Worley's team received another clue when they found that protein kinases also bind to Preso1.
Genetically modifying mice so that they don't make any Preso1, the researchers found that binding between mGluRs and Homer in these animals' neurons was greatly reduced compared to normal mice.
Additionally, when the researchers injected the modified mice with a chemical that causes pain and inflammation, the animals had a significantly greater and longer-lasting response compared to regular mice. A final experiment showed that neurons taken from the modified animals were significantly more responsive to the neurotransmitter glutamate. When the researchers added Preso1 to the cell cultures, this increased activity disappeared, suggesting that Preso1 is pivotal for mGluRs to signal properly.
Taken together, Worley explains, the findings suggest that Preso1 appears to gather all the important elements in this system -- Homer, protein kinases and mGluRs -- bringing them all together to coordinate the activation and deactivation of the mGluRs.
With Preso1 so pivotal for regulating group 1 mGluR activity, it could prove a useful new target for drugs to treat a variety of health problems in which these receptors are thought to play a role, including chronic pain, schizophrenia, Alzheimer's disease, and fragile X syndrome, Worley says.
"Because mGluRs play so many important roles in the brain for so many different mental and neurological health conditions, knowledge of their regulatory mechanisms is extremely important. But we really don't know how they work in great detail," he says. "You need to know all the players before you can understand the system. Here, we've identified an important player that no one had previously known had existed. Preso1 and Homer appear essential for desensitization of mGluR signaling, much like beta-adrenergic receptor kinase and arrestin are important for desensitization of adrenergic and opiate receptors."
This work was supported by National Institutes of Health grants from the National Institute on Drug Abuse (DA010309), National Institute of Mental Health (MH084020), National Institute of Neurological Disorders and Stroke (NS050274 (P.F.W.); NS054791 and GM087369 (X.D.)), National 973 Basic Research Program of China (20009CB941400; B.X.), and the National Institute on Deafness and Other Communication Disorders Intramural Research Program (R.S.P.).
Sourced from Science Daily
Opportunities Arise in Alternative Delivery for Non-Device-Enabled Pharmaceuticals
The drug industry is facing an unprecedented level of challenges, threatening to crumble even the largest of players. Oral deliveries remain the dominant mode of drug delivery. But with a flagging pipeline, looming patent expiries, and increasing competition from new entrants, device delivery technologies offer new potential to boost safety, efficacy, and sales of today’s top-selling drug products
Currently, $124 billion worth of top-selling drugs rely on devices for delivery, but with innovation increasing in the sector, close to half of these drugs are eligible for an upgrade. With $55 billion currently at stake via basic delivery devices, and billions more up for grabs as orally delivered drugs face a patent meltdown, the advanced drug-delivery-device sector looks increasingly inviting to drug-makers.
This week’s graphic comes from a recent report, in which Lux Research surveys the landscape of top-selling drugs facing patent expiration that are currently not device-enabled or are delivered only by basic devices.
It is difficult for device technologies to compete against oral-based delivery, which comprises the majority of device-based alternatives, on convenience or cost. So other factors become paramount, such as localizing exposure to reduce side effects, increase efficiency, or improve compliance with electronic enablement (e.g. alarms).
As the graphic shows, 64 percent of products delivered without devices or with basic devices – accounting for $127 billion worth of revenues in 2011 – will face patent expiry within these five years. More advanced versions of delivery devices, with their high manipulability and potential to address delivery issues will provide technical as well as consumer value, presenting an optimistic route for the life-cycle extension of products facing patent expiry. This is especially true amidst the trend of increasing patient-centric healthcare. It behooves pharmas, generics, and biotechs, as well as biosimilar producers (with the latter two producing biologics and essentially depending on devices for delivery) to explore delivery technologies to enhance their drug product value. Delivery technologies will help them keep pace with the changing demands of their end users, and potentially rescue and rejuvenate revenue potential.
Source: Lux Research report “Making Space for Innovation in Drug-delivery Devices.”
Market Development Manager - Sports Medicine - July 2012
P&G Newsletter - August 2012
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