Ethypharm has extended its technological portfolio beyond oral delivery to new drug delivery systems, mainly in the field of delivery of biomolecules.
These applications address new areas for pharmaceutical industries.
Organogels
This patented process is based on the specific physico-chemical properties of an innovative composition consisting of a hydrophilic organic substance and an organo-gelling substance derived from amine acids susceptible to trap a particular active substance for sustained delivery over a period of time.
A hydrophilic organic reagent introduced by injection vies in competition with the organo-gelling molecules by creating gentle links with these molecules (hydrogen bridges, Van der Waals forces) preventing gel formation. After injection, the diffusion of the hydrophilic substance in the surrounding environment will then lead to the self-assembling of the molecules of the organo-gelling substance. This self-assembling phenomenon, by the creation of a structured network, will permit the retention of the hydrophile organic liquid causing passage from a liquid state to a gelled state and thus providing a simple process and easy administration of spontaneous in situ gelling.
By means of a controlled process of diffusion and biodegradation the organogel thus formed serves as a sustained release support for bioactive substances in the organism.
Lipidic Nanocapsules
In cooperation with Angers University, Ethypharm is also working on a new generation of nanovectors – lipidic nanocapsules (LNCs). Nanoparticles permit to improve the oral bioavailability of certain molecules. LNCs are prepared in accordance with a simple phase inversion process – a method which has the advantage of not requiring the use of solvents. This new colloidal system consists of a lipidic core constituted of medium link triglycerides surrounded by phospholipids and hydrophilic polymers. This proprietary technique permits the encapsulation of lipophilic molecules.
There are numerous factors which can limit the bioavailability of medicines. Their solubility, their degradation with the digestive tract or their efflux by cellular pumps, are all obstacles against the absorption of medicines by the oral route. Encapsulation of the active substance contained in LNCs permits protection of the molecules against degradation in the gastro-intestinal environment. It also permits augmentation of intestinal permeability. Notably, LNCs possess the propriety of inhibiting P-gp activity, a protein responsible for the efflux of numerous molecules. These diverse properties permit augmentation of oral bioavailability.
