presentation to the australasian

OBJ Limited (ACN 056 482 636)
Ground Floor, 284 Oxford Street, Leederville, Western Australia 6007
Phone: +61 9 9443 3011 Fax: +61 9 9443 3866 Email: [email protected]
Tuesday, 6 December 2005
FOR IMMEDIATE RELEASE
PRESENTATION TO THE AUSTRALASIAN
PHARMACEUTICAL SCIENCE ASSOCIATION
ANNUAL SCIENTIFIC MEETING
==============================================
OBJ Limited (ASX:OBJ) is pleased to make available the materials to be
presented by Sarika Namjoshi BSc(Hons) of Curtin University’s Drug
Development Department to the annual scientific meeting of the Australasian
Pharmaceutical Science Association.
The invitation to present was extended jointly by the Australasian
Pharmaceutical Science Association and the Australasian Society of Clinical
and Experimental Pharmacologists and Toxicologists.
The annual meeting commenced in Melbourne on 4 December 2005 and
closes on 7 December 2005.
- END -
Background to the Announcement
OBJ Limited is a drug delivery company, specializing in electronic “drug patch”
technologies that allow drugs, vaccines, therapeutic agents and cosmetic compounds
to be delivered more effectively and more efficiently through-the-skin.
The OBJ Dermaportation system has been shown to manage and control the
transdermal delivery of a broad range of drugs and therapeutic agents ranging from
small difficult molecules such as Caffeine, through to large macro-globular proteins
drugs such as vaccines.
OBJ’s technology has been independently proven in both in-vitro and in-vivo studies
and can manage a broader range of molecular sizes, structures and valencies than
other active or passive drug delivery systems.
OBJ has been successful in
managing the through-the-skin
delivery of drugs used in the
inflammation, pain, cancer and
cosmetic fields.
OBJ’s technology is low cost, and
can be incorporated into reusable
drug patches, (as illustrated)
disposable single use drug patches
and in a range of packaging
systems for OTC and retail use.
Sustainable Benefits
Low cost and controlled through-the-skin delivery of drugs, hormones, vitamins,
vaccines, anti-bodies and anti-aging molecules has long been the desire of the
pharmaceutical industry. It would provide economic, safety and efficacy benefits to the
pharmacology, medical, veterinary and cosmetic industries. Side effects could be
reduced by localized delivery and programmed delivery rates. Needle stick injuries and
needle disposable problems could be eliminated while the reduction in the level of skill
required for application could significantly reduce total cost of many health
programmes. These clear commercial benefits may only be achievable if the skin’s
natural barrier effect can be overcome.
OBJ is the first company to create a broad spectrum through-the-skin delivery system
that is kind to the skin, completely reversible, yet can handle drugs range from the
small difficult molecules up to the largest and most complex proteins and anti-bodies.
OBJ manages an extensive IP portfolio and prosecutes patent applications throughout
the world.
Independence of Results
OBJ contracts its drug and technology testing programs to independent and respected
organisations, such as Western Australian Biomedical Research Institute, Western
Australian Institute for Medical Research, Curtin University of Technology and Murdoch
University. The high level of independence and international accreditation means that
the results attributable to OBJ’s proprietary technology can be published and presented
at major medical and scientific conferences and forums.
For more information:
Jeffrey Edwards
Phone: +61 9 944 33011 Mobile: 041 791 2211 E-mail: [email protected]
HPLC ASSAY FOR HPLC ASSAY FOR
5–AMINOLEVULINIC ACID AMINOLEVULINIC ACID
AND ITS APPLICATION TO AND ITS APPLICATION TO
ASSESSMENT OF SKIN ASSESSMENT OF SKIN
PENETRATION PENETRATION
Sarika Namjoshi Sarika Namjoshi, Rima Caccetta, , Rima Caccetta,
Jeff Edwards and Heather Benson Jeff Edwards and Heather Benson
Structure of human skin Structure of human skin
Background
Transdermal Drug Delivery Transdermal Drug Delivery
���� Painless and patient friendly Painless and patient friendly
���� Avoid first pass metabolism: lower dose Avoid first pass metabolism: lower dose
and reduced side and reduced side-effects effects
���� Controlled release: better control of Controlled release: better control of
symptoms, extended dosing intervals and symptoms, extended dosing intervals and
reduced side reduced side-effects effects
���� Major limitation: skin permeability Major limitation: skin permeability – few few
TDD applications currently available TDD applications currently available
Skin Penetration Enhancement Skin Penetration Enhancement
���� Optimize physicochemical characteristics Optimize physicochemical characteristics
of the drug and/or formulation of the drug and/or formulation
���� Chemical penetration enhancers Chemical penetration enhancers
���� Physical penetration enhancers Physical penetration enhancers
���� Iontophoresis Iontophoresis
���� Electroporation Electroporation
���� Sonophoresis/phonophoresis Sonophoresis/phonophoresis
���� Dermaportation Dermaportation
5 Aminolevulinic acid (ALA) 5 Aminolevulinic acid (ALA)
���� ALA is a delta amino acid ALA is a delta amino acid
���� It is hydrophilic and zwitterionic at It is hydrophilic and zwitterionic at
physiological pH physiological pH
���� Used with PDT in the treatment of BCC. Used with PDT in the treatment of BCC.
���� It is converted into PpIX, precursor of heme It is converted into PpIX, precursor of heme
���� Exogenous administration of ALA results Exogenous administration of ALA results
in PpIX accumulation in PpIX accumulation
���� Light activation (PDT) causes destruction Light activation (PDT) causes destruction
of tumours of tumours
���� Skin permeability of ALA through skin Skin permeability of ALA through skin
lesions is poor lesions is poor
AIM AIM
To assess the impact of Dermaportation on To assess the impact of Dermaportation on
the transdermal delivery of ALA the transdermal delivery of ALA
HPLC Method Development HPLC Method Development
���� ALA does not contain a chromophore therefore ALA does not contain a chromophore therefore
cannot be detected by UV cannot be detected by UV
���� Fluorescence derivitization for developing a HPLC Fluorescence derivitization for developing a HPLC
assay. assay.
-100
0
100
200
300
400
500
600
700
0 2 4 6 8 10 12
Concentration (µg/mL)
Peak area
Methods
0
500
1000
1500
2000
2500
3000
3500
0 10 20 30 40 50 60
Concentration (µg/mL)
Peak area
Standard curve after
derivatization at 1000C
Standard curve after
derivatization with
Fluorescamine at room
temperature
R2 = 0.9475 R2 = 0.9993
HPLC Assay For ALA Detection HPLC Assay For ALA Detection
���� Amine group of ALA targeted by Amine group of ALA targeted by
Fluorescamine Fluorescamine
���� Linearity Linearity R2 = 0.9993 = 0.9993
���� Limits of detection (LOD) = 120 ng mL Limits of detection (LOD) = 120 ng mL−1
���� Limit of quantification (LOQ) = 400 Limit of quantification (LOQ) = 400 ng ng
mL mL−1
���� Accuracy = 99.4% Accuracy = 99.4%
Dermaportation Dermaportation – in vitro in vitro diffusion diffusion
protocol protocol
Donor Phase
Membrane
Dermaportation
Receptor phase
Sampling arm
Dermaportation Dermaportation vs vs passive diffusion of passive diffusion of
ALA across human epidermis ALA across human epidermis
(mean (mean ± sem sem)
0.0
2000.0
4000.0
6000.0
8000.0
10000.0
12000.0
0 60 120 180 240
Time (min)
Cumulative amt ALA (ug/cm2)
Dermaportation
Passive
Dermaportation: ALA flux and Dermaportation: ALA flux and
Enhancement ratios (ER) Enhancement ratios (ER)
3.82 3.82 76.57 76.57 Dermaportation Dermaportation
0.006 0.006 0.12 0.12 Passive Passive
Permeability Permeability
coefficient (cm.h coefficient (cm.h-1)
Flux during Flux during
Dermaportation Dermaportation
(µg.cm g.cm-2.h) .h)
Conclusions Conclusions
���� The HPLC method developed was The HPLC method developed was
accurate and sensitive accurate and sensitive
���� Dermaportation enhanced the Dermaportation enhanced the
transdermal delivery of ALA as transdermal delivery of ALA as
compared to passive diffusion compared to passive diffusion
���� Dermaportation has potential as a skin Dermaportation has potential as a skin
penetration enhancement technology penetration enhancement technology –
further evaluation with small and large further evaluation with small and large
molecules molecules