Preparation and Characterization of Paclitaxel Nanocrystalline Suspensions

OBJECTIVE To optimize the formulation and preparation conditions of paclitaxel nanocrystalline suspensions, describe the physical characterization of paclitaxel nanocrystals, and inspect its in vitro release characteristics. METHODS Single factor experimental method was used to study the formulation composition and preparation procedure of paclitaxel nanocrystals to establish the preparation procedure of the method of high pressure homogenization. Nanocrystalline morphology, particle size distribution was physically characterized. An HPLC method was used to investigate the equilibrium solubility and in vitro release characteristics of paclitaxel nanocrystals. RESULTS The average particle diameter of nanocrystals was (239.5±1.98)nm, polydispersity was 0.111±0.011, Zeta electric potential was -(24.6±1.13)mV. TEM images showed that paclitaxel nanocrystals had a rod-like morphology with a uniform distribution. The equilibrium solubility of nanocrystals in PBS pH7.4 solution was 1 800 times as many as paclitaxel API and 250 times in water. In 0.5% SDS-PBS (pH 7.4) solution, the in vitro cumulative release of paclitaxel nanocrystals reached 91.6% in 5 min, while the cumulative release of physical mixture was 67.7% in 2 h. CONCLUSION The paclitaxel nanoparticles is distributed evenly, and the formulation and preparation method are simple and feasible. Nanocrystals significantly improve solubility and release rate of paclitaxel.