Preparation, Characterization, and Bioactivity of Temsirolimus-In- Phospholipids-Cholesterol-In-Liposome

Preparation, characterization, and in vitro bioactivity of temsirolimus liposomes (TL) were investigated. TL was prepared with film dispersion-ultrasonic method, and the effective factors of TL were screened and optimized with response surface methodology (RSM). Under the optimal preparation conditions, i.e. ratio of phospholipids to drug (w/w) 20: 1, ratio of phospholipids to cholesterol (w/w) 14: 1, and the concentration of phospholipids (w/v) 3%, the experimental entrapment efficiency of TL was 83.0 +/- 1.2%, which was close to the predicted value. The mean particle size was 122.4 +/- 0.45 nm, and kept stable after that TL was freeze-dried with sucrose or lactose as cryoprotectant. The data of bioactivity showed that TL could increase obviously antitumor activity in HepG2 tumor cells compared to free temsirolimus. The novel temsirolimus formulation was easy to push industrialization forward and might be a potential carrier for temsirolimus delivery in tumor chemotherapy.