Abstract:

Objective   To prepare docetaxel (DTX)-loaded Pluronic F68 polymeric micelles (DTX-micelles) and evaluate their physicochemical characterization. Methods    The DTXmicelles were prepared by nano-precipitation methods. Based on the results of single factor experiments, the DTX-micelle formulation was optimized by  orthogonal design. The encapsulation efficacy (EE%) and drug loading (DL%) were determined by the RP-HPLC method. The physicochemical characteristics were evaluated, including  surface morphology, particle size and size distribution as well as zeta potential. The in vitro release behaviors of DTX-micelles were carried out by the dynamic membrane dialysis technique. Results   The drug-loading rate and entrapment rate were (0.060±0.003)% and (89.10±1.50)%, respectively. The DTX-micelles were spherical with a mean particle size of (135.1±3.42) nm and a zeta potential of  (-10.56±3.52)mV. The release of DTX from DTX-micelles followed the Weibull equation. Conclusions   DTX-micelles were successfully prepared  and improved the solubility of DTX.

Key words: Docetaxel; Pluronic F68; Polymeric micelles; Nanoprecipitation methods