Selection suitable solvents to prepare paclitaxel-loaded micelles by solvent evaporation method

Abstract

Amphiphilic block copolymer micelle is one of the most important drug delivery systems to improve the water-solubility of lipophilic drugs. Blank micelles were prepared by solvent evaporation method in order to choose the suitable solvents for PBMA-b-PMPC (poly(n-butyl methacrylate)-b-poly(2-methacryloyloxyethyl phosphorylcholine)) copolymer micelles. The selected solvents, which include chloroform/ethanol mixture and ScCO₂, were used to prepare the paclitaxel-loaded micelles. The micelles with high drug encapsulation efficiency and drug-loading content showed both narrow size distribution and regularly spherical shape. In vitro drug release studies indicated that paclitaxel could be slowly and continuously released from the micelles. More than 50% incorporated drug was released within 132 h from the micelles prepared using ScCO₂ as solvent while only 20% was released at the same period from those prepared using chloroform/ethanol mixture. In addition, the environmentally-friendly solvent, ScCO₂, was used for the first time to prepare the paclitaxel-loaded micelles during the solvent evaporation process.

Keywords::

• Drug delivery system
• paclitaxel
• solvent evaporation method
• supercritical dioxide carbon
• morphology
• controlled release