Amphiphilic N-(2,3-dihydroxypropyl)-chitosan-cholic acid micelles for paclitaxel delivery.

Self-assembled amphiphilic N-(2,3-dihydroxypropyl)-chitosan-cholic acid (DHP-CS-CHO) micelle was prepared as a carrier for paclitaxel. DHP-CS-CHO was synthesized by grafted small molecules cholic acid and glycidol onto primary amine group of chitosan, respectively. The DHP-CS-CHO formed uniform micelles (size=212.4±3.1 nm) with a low critical micelle concentration (0.024 mg/ml) in PBS. Hydrophobic anticancer drug, paclitaxel (PTX), was easily encapsulated into chitosan derivative micelles by a dialysis method with loading efficiency up to 80%. The PTX loaded micelles released the drug in a sustained manner more than a week in PBS containing 0.1% (w/v) Tween 80 at 37°C. In vitro antitumor experiment demonstrated that PTX loaded chitosan derivative micelles could inhibit MCF-7 cell growth and induce its apoptosis. These results suggested that DHP-CS-CHO may be a promising carrier for the anticancer drug PTX.