Preparation and in vitro activity of liposome encapsulated opioids

Abstract

Four opiate molecules: morphine, naloxone, meperidine and codeine have been encapsulated in liposomes. the encapsulation efficiency has been studied as a function of the following parameters: liposome preparation method, lipid composition and opioid molecule hydrophobicity. the most important parameter as far as the entrapment efficiency is concerned is the liposome preparation method.

The opioid activity of these molecules in vitro (Guinea Pig Ileum preparation) has been determined. No differences in the IC₅₀ values could be found between encapsulated and free drug molecules.