AKVANO® spray delivery system ‘tunable’ for fast or slow release

Lugano, Switzerland; Stockholm, Sweden: – High-tech CDMO Cerbios-Pharma SA (Cerbios) has released new test results on its innovative drug delivery system, AKVANO®, co-developed with Swedish partner Lipidor AB (LIPIDOR). These indicate that AKVANO is even more versatile than previously thought, being ‘tunable’ for fast or slow release.AKVANO technology represents a completely new dosage form that creates a lipid layer on the skin surface for effective topical delivery of drugs and skin care treatment. Formulations consist of selected lipids, with or without active ingredients, which are dissolved in a volatile solvent, formulated as a clear water-free, cutaneous and sprayable liquid. When this formulation is applied to the skin, the solvent evaporates and a non-occlusive lipid layer is formed in an immediate interaction with the skin surface.

Controlling permeation

Earlier studies show that by choosing different lipids in the AKVANO vehicle, the skin barrier could either be strengthened or weakened, evidenced by changes in transepidermal water loss (TEWL).

Now a Lipidor White Paper reports diffusion study results from new in vitro permeation experiments, performed on ketoprofen, diclofenac diethylamine and diclofenac sodium formulations in the AKVANO system.

“These test results show that by adjusting the composition of lipid components in AKVANO vehicles, it is possible to control permeation,” Cerbios reports.

From slow to ultra-fast release

“By using a lipid composition with only barrier strengthening components, the penetration is relatively slow, and a significant part of the active substance is retained in or on the membrane. With a moderate amount of penetration enhancing lipids, the flux increases but registers a prolonged release profile,” says Cerbios.

The tests also showed that AKVANO formulations using higher proportions of the penetration enhancing lipids matched or exceeded the release speeds for active substance through the membrane achieved by currently available commercial products Orudis® gel (2.5 % ketoprofen) and Voltaren® gel (2.3 % diclofenac diethylamine).

Flexible delivery platform

”We are very excited about the results obtained, which confirm the very high flexibility of the AKVANO delivery system, not only in incorporating very different drug substances (from lipophilic to hydrophilic), but also providing a flexible delivery speed from fast to slow”, commented Cerbios CEO Dr. Gabriel Haering.

“This gives very high flexibility for the development and manufacture of topical drugs currently at New Chemical Entities or Life-Cycle-Management stage,” said Dr. Haering.

Wide range of APIs

LIPIDOR CEO Dr. Anders Carlsson added: “I am very pleased with these results which confirm that AKVANO technology has the capacity to control the delivery rate of active components into the skin, and that it is possible to fine-tune the balance between penetration enhancement and strengthening of the protective skin barrier.”

AKVANO is available to companies wishing to innovate, develop or improve new and existing products in areas like pharmaceuticals, biocides, cosmetics and medical devices. So far, more than 80 active ingredients have been successfully incorporated into AKVANO, of which more than 50 are active pharmaceutical ingredients (APIs). AKVANO is designed for local treatment, not for systemic delivery. AKVANO® is a registered trademark of Lipidor AB.

About Cerbios-Pharma

Cerbios is a privately held company located in Lugano, Switzerland, that specializes in the development and manufacture of both chemical and biological APIs for its partners worldwide.

Formed in 1994 by the merger of Bioferment SA (founded in 1976) and Sapec SA (founded in 1979), Cerbios specializes in the development and production of high potency active pharmaceutical ingredients (HPAPIs) in the area of fine chemicals and biologicals.

Exclusive, third party manufacturing services are offered by the Chemical Division for HPAIs and by the Biological Division for monoclonal antibodies, recombinant proteins and pharma probiotics.

About Lipidor

Lipidor AB is a Swedish lipid technology company offering unique lipid based formulation opportunities across dermatology, wound and skin care markets. The company was established in 2009.

Research and development is conducted at Stockholm University and Karolinska Institutet Science Park in Stockholm. Lipidor is owned by its founders, Karolinska Development, AB, Cerbios-Pharma SA, Aurena Laboratories AB and private investors (http://www.lipidor.se/).