Application of aerosol solvent extraction system (ASES) process for preparation of liposomes in a dry and reconstitutable form

Abstract

The aerosol solvent extraction system (ASES) process was applied to prepare liposomes in a dry and reconstitutable form. Dry ASES microparticles containing miconazole (MCZ) as a model drug were prepared by an optimized ASES process with various compositions of spraying solution containing phosphatidylcholine, cholesterol, and Poloxamer 407. The influence of such compositions and the pH of hydration medium on the physico-chemical properties of the produced microparticles were investigated before and after hydration. At optimized conditions, partially crystalline, spherical, and nonporous microparticles associated in aggregates varying from a few microns to 40 μm were produced with the residual content of methylene chloride and methanol lower than 30 and 86 ppm, respectively. The percentage of drug recovered in the produced microparticles was increased with an increase of the drug concentration in the spraying solution. The entrapment efficiency of hydrated MCZ microparticles was improved by increasing the pH of the hydration medium. © 2006 Elsevier B.V. All rights reserved.