Controlled Release of Griseofulvin from Coprecipitates with Phospholipids

Abstract

The release of griseofulvin from griseofulvin: phospholipid coprecipitates has been studied as a function of 1) the fatty ester chain length of phosphatidylcholine, 2) the choice of solvent in forming coprecipitates, and 3) the ratio of phospholipid: cholesterol in the lipid component. Only coprecipitates containing 95%w/w and 80%w/w griseofulvin were examined. The release kinetics and total release after 60 min correlates with the phase transition temperatures of the various phosphatidylcholines. The addition of cholesterol diminishes the initial release rates but increases the total amount released after 60 min when the phospholipid:cholesterol mole ratio is greater than unity. The role of chloroform as an enhancer of the release process and the phospholipid as a solubilizer of griseofulvin is demonstrated.