CONTEXT

Efficient trans-cutaneous delivery of active molecules is still a challenge due to the nature itself of the dermal tissue. The permeabibility of therapeutic agents can be improved by permeability agents but most of the induced delivery mechanisms induce irreversible skin alterations. We present here an original strategy consisting in using the active molecule itself to parcicipate into ist own trans-cutaneous transport, while protecting solubilizing and delivering it to its active site.

TECHNICAL DESCRIPTION

The invention thus proposes to associate a biocompatible amphiphilic acidic transporter with an active principle comprising one or more basic functional groups. This intermolecular association leads to a novel amphiphilic species corresponding to the formation of an acid/base pair bound by electrostatic interactions and stabilized by Van der Waals interactions between the hydrophobic moieties of the two components. The amphiphilic complex thus formed by association can lead, according to its concentration in water as well as the nature of the active principle (volume, hydrophobicity), to a group of self-assembled structures such as micelles or vesicles. The objects thus formed can also be used for self-transport of the active principle.…

BENEFITS

This invention has applications in formulations, in terms of solubilization, protection, conveyance and transcutaneous diffusion of an active principle, wherein the amphiphilic molecule can also play the role of permeabilization agent for transcutaneous conveyance. These formulations, which are simplified and harmless to the skin, thus make it possible to increase the principle active concentration in the skin and to promote its passage through the stratum corneum.

INDUSTRIAL APPLICATIONS

Trans-cutaneous delivery of active molecules: cosmetics, therapeutics…

DEVELOPMENT STAGE

A recent article (ChemPhysChem 2013, 14, 1126 – 1131) presents an original catanionic assembly for antihistamine delivery with sugar-derived bolaamphiphiles. The antihistamine incorporated within the aggregates is not just dissolved in water but is a constitutive entity of the spontaneousself-assembling process. The formation of a drug reservoir with vesicles ensures slower diffusion of the antihistamine through the skin and protection of the antihistamine against UV damage. Finally, these easy-to-prepare bioactive catanionic associations made of biocompatible surfactants are promising dermal delivery systems for promethazine in the course of skin allergic treatments.

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