Paclitaxel formulation with stable sustained-release behavior and its biological safety evaluation

Abstract

Biological safety and stable sustained-release of the drug are two crucial issues involved in the formulation of paclitaxel. Focusing on these issues, by using the FDA approved polylactide as carrier material, soybean lecithin as surfactant and maltodextrin as thickener, paclitaxel loaded PLA microspheres were simply prepared by solvent evaporation, thus guaranteeing the biological safety. The introduction of maltodextrin as a thickener aided to a stable sustained-release of paclitaxel. Surface morphology, particle size, drug loading rate, encapsulation efficiency and in vitro drug release behavior were investigated. Biological safety evaluations such as acute toxicity, allergies, hemolysis, skin stimulation and genotoxicity test were also carried out. Results showed that the obtained microspheres were biocompatible and could release paclitaxel at a desirable constant rate. Therefore, the simply prepared paclitaxel formulation with good biological safety and desirable release behavior exhibited great potential of local injection of paclitaxel for the clinical use in the future.