Product Opportunities

-> Significance of Drug Delivery
-> Transdermal Transport Systems (TTS)
-> Targeted Drug Delivery Through the Skin
-> IDEA' s Product Portfolio
-> Patents

Significance of Drug Delivery

Pharmaceutical companies are realising more and more that the return on investment for the improved delivery of approved (marketed) compounds is typically greater than the return on developing related new chemical entities. Many major corporations have also found that from thousands of product candidates only those agents which are "packaged" and delivered properly into the body will flourish on the market. This is accomplished by drug delivery groups which, more often than not, reside outside the big-pharma companies.

Transdermal Transport Systems (TTS)

Conventional TTS that deliver drugs to the whole body have been known and used for decades. They constitute a worldwide annual market in excess 2 billion dollars; if one includes analgesic patches for regional therapy, the market exceeds 3 billion US dollars.

 
Effect of molecular weight and lipophilicity on the rate of transdermal transport in case of permeation (upper and lower green curve for the more or less lipophilic substances, respectively) or of the Transfersome® mediated penetration (blue line and bullets). Green bullets represent the commercial drugs in transdermal patches (click to enlarge).

Historically, the main reason for the success of transdermal delivery was the avoidance of first-pass metabolism. This increases drug bioavailability in comparison to oral formulations. Transdermal formulations also deliver drugs with a steady rate (first order kinetics), which is an additional advantage. However, transdermal drug delivery methods have their drawbacks. Most important are the unwanted local side effects (skin irritation/toxicity) and the fact that conventional TTS technology is only suited for delivering relatively small drugs across the skin. The green symbols in the figure above define all important drugs in TTS devices that are used to date.

New transdermal drug delivery methods are therefore required to drive future growth in transdermal product markets. Biological products would also profit greatly from new, non-invasive delivery. The original players in the transdermal field failed to introduce such improvements, which were then introduced by a number of innovator companies, including IDEA.

Broadly speaking, two different new approaches for transdermal drug delivery are currently being pursued:
- nanoporation/minimum abrasion;
- nanocarriers.
Sonoporation, thermoporation or use of very fine and short needles belong to the former; ultradeformable carriers (Transfersome® vesicles or, their typically less advanced kin, such as Ethosomes® or fluid liposomes) exemplify the latter. Any of these can deliver small or large molecules across the skin, but only Transfersome® carriers can provide control over local drug deposition as well.

Targeted Drug Delivery Through the Skin

The therapeutics applied to the skin in a conventional fashion, e.g. using gel or a patch, all rely on the drug’s concentration gradient (chemical “force”) to drive molecular diffusion through the stratum corneum. A drug molecule that has overcome this primary skin barrier continues to diffuse below the stratum corneum driven by the same, but unavoidably smaller force. A drug molecule that has crossed the deeper skin layers may ultimately reach subcutaneous tissues, such as fat deposits and muscles. However, to do so the drug molecule must also avoid the skin microvessels, which form an extensive secondary skin barrier. The free drug concentration thus declines very steeply from the skin surface towards deep subcutaneous tissue.
A drug must be prevented from entering into cutaneous blood vessels to overcome the problem of its local clearance. Until recently, this could only be done by injecting a suitable drug depot formulation below the skin. With IDEA’s products designed for targeted drug deposition into peripheral tissue the same goal is achieved by using Transfersome® carriers. The latter are water—rather than drug—concentration driven and deformable enough to overcome the primary skin barrier and too large to be taken-up by cutaneous blood microvasculature; Transfersome®-drug association then also precludes rapid drug dissipation. Such carriers consequently promote drug accumulation and retention at the chosen subcutaneous site, by way of controlled vesicle deposition at such a site and prolongation of the duration of drug-carrier association. This is a major—and therapeutically much needed—advantage of Transfersome® mediated drug transport into target peripheral tissue, unmatched by any conventional drug delivery method.
The depth and extent of the carrier-mediated drug deposition is chiefly controlled by the applied Transfersome® dose per area, and not by the total drug amount used, owing to the fact that the carrier transport across the skin is osmotically rather than chemically driven. This unmatched feature of Transfersome® technology is highlighted in the table below:


IDEA’s technology is therefore ideally suited for controlling the depth and rate of drug delivery, and for improving drug accumulation in deep subcutaneous tissues, such as muscles and joints below the local application site, whilst minimising systemic drug exposure.

IDEA's Product Portfolio

IDEA's non-invasive drug delivery system, the proprietary Transfersome® carriers, is the method of choice for administering various therapeutic agents into and across the skin barrier in a controlled fashion. The concept has been proven in vivo for a number of drugs in Transfersome® formulation prototypes.

IDEA's long term focus is the development of novel dermatological products. Currently, the Company is using Transfersome® cariers to transport the established low molecular weight drugs selectively into the skin and, in particular, the underlying deep tissues. Such regional delivery generally can be safer, more convenient, and more efficient than conventional topical applications. Furthermore, Transfersome®-mediated drug delivery can provide good control over the depth of deposition of the active ingredient and/or kinetics of drug release.

The Company is pursuing the commercial opportunities of several such products listed in the table above.

The Targeted Analgesic IDEA-033

Dermatics
- Topical drug delivery into the skin

Regio-selective therapeutics
- Delivery to deep skin and underlying muscles/joints

Systemic therapeutics
- Delivery to the whole body

Patents

IDEA holds close to 60 issued patents from 9 international (PCT) patent families for the Transfersome® technology and its transdermal, transnasal applications, incl. vaccination, in the major pharmaceutical markets. These patents cover the composition of matter, methods of use, carrier manufacturing, loading with drugs, and other relevant technological aspects.

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