Abstract:
OBJECTIVE To prepare the paclitaxel nano-liposomes gels, detect the particle size, particle diameter, the entrapment efficiency, the release and transdermal diffusion characteristics in vitro. METHODS Paclitaxel nano-liposomes were prepared using thin film evaporation high pressure microfluidization, added carbomer to prepare the paclitaxel nano-liposomes gels, and the optimal method was determined by the orthogonal test. The particle size, particle diameter of the modified liposomes was detected by nanoparticle size analyzer. The entrapment efficiency was determined by low-speed combination method with HPLC. The release study adopting membrane diffusion method. Using Franz diffusion cell and rats skin to investigate transdermal diffusion characteristics of the modified nano-liposomes gels in vitro. RESULTS The optimal formulation and preparing conditions were as the following: the content of lecithin was 2%, drug∶lecithin=1∶30, lecithin∶cholesterin=10∶1. The particle size of the liposome prepared was 81.8 nm. The particle size distribution coefficient was 0.180. The average entrapment efficiency of the liposomes was up to 73.2%. The release amount of nano-liposomes gels was 79.04% at 72 h and the cumulative penetration amount per unit area was 429.68 μg·cm
-2 at 48 h. CONCLUSION This preparation is prepared with simple technology and the entrapment efficiency of the paclitaxel is high. The particle sizes are small and uniform. Nano-liposomes gels feature a sustained release in vitro, the nano-liposomes can increase diffusion rate of paclitaxel through the skin of rats.