Linker-based lecithin microemulsion delivery vehicles

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/107 (2006.01) A61K 47/12 (2006.01) A61K 47/24 (2006.01) A61K 47/44 (2006.01)

Patent

CA 2673234

The present invention relates to biocompatible microemulsion systems designed for controlled release drug delivery applications formulated with phospholipids such as lecithin (surfactant), a lipophilic additive (linker) containing 9 or more carbons in their alkyl group and hydrophilic-lipophilic balance (HLB) of 5 or less, and a surfactant-like hydrophilic additive (linker) containing between 6 to 9 carbon atoms in their alkyl tail. The combination of linkers and phospholipids produce formulations capable of delivering high concentrations of poorly soluble drugs into epithelial tissue using low surfactant concentrations, with minimum cytotoxic side effects.

La présente invention concerne des systèmes de microémulsions biocompatibles conçus pour des applications d'administration de médicament à libération contrôlée formulés avec des phospholipides tels que la lécithine (tensioactif), un additif lipophile (liant) contenant 9 ou plus de 9 atomes de carbone dans son groupe alkyle et ayant une balance hydrophile-lipophile (HLB) inférieure ou égale à 5 et un additif hydrophile semblable à un tensioactif (liant) contenant entre 6 et 9 atomes de carbone dans sa queue alkylique. L'association des liants et des phospholipides produit des formulations permettant d'administrer des concentrations élevées de médicaments faiblement solubles à un tissu épithélial en utilisant de faibles concentrations en tensioactif, avec un minimum d'effets secondaires cytotoxiques.

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