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.