RESUMO
OBJECTIVE: To prepare paclitaxel-loaded solid lipid nanoparticles (PTX-SLNs) and evaluate its physicochemical properties, release behavior and antitumor activity in vitro. METHODS: PTX-SLNs were prepared in a rectangular microchannels. The formulation of PTX-SLNs were optimized by the orthogonal design. The particle size distributions was determined by dynamic light scattering(DLS) techniques. The encapsulation efficiency and drug loading content were determined by HPLC. In vitro release behavior and in vitro antitumor activity of the PTX-SLNs were investigated by dialysis and MTT respectively. RESULTS: Transmission electron microscopy (TEM) image showed that the obtained nanoparticles shaped regularly round and dispersed uniformly. The particle size of PTX-SLNs was(129.73 ±2.41) nm, drug loading content and drug encapsulation efficiency were(3.11 ± 1.90)% and(43.67 ± 0.55)% respectively. The in vitro release behavior exhibited that the amount of cumulated paclitaxel released from PTX-SLNs was 87.3% with initial burst release and sustained release in 120 h. In vitro antitumor activity of the PTX-SLNs against human breast cancer MCF-7 indicated that in comparison with paclitaxel solution the minimal inhibitory concentration of paclitaxel-SLNs is remarkably lower. CONCLUSION: PTX-SLNs is easy to prepare in microchannels and its quality is stable. This preparation technique has a very good prospect in the field of pharmaceutics.