羟基喜树碱半固体脂质纳米粒的体外药剂学性质研究

Pharmaceutical characteristics of hydroxycamptothecin semisolid lipid nanoparticles in vitro

目的:制备羟基喜树碱的半固体脂质纳米粒(HCPT-SSLN)。方法:在单因素考察的基础上,通过正交设计优选处方和制备工艺,并对优化条件下制备的HCPT-SSLN进行质量评价。结果:制备的HCPT-SSLN平均粒径为130.5 nm,多分散系数为0.18,载药量为2.51%,包封率为79.19%,Zeta电位为-33.1mV;体外释药规律符合Weibull方程lnln[1/(1-Q)]=0.2633lnt+0.0509(r=0.9485);HCPT-SSLN4℃下放置6个月,纳米粒外观、粒径及包封率无明显变化。结论:所制备的HCPT-SSLN包封率和载药量较高,粒径分布均匀,稳定性良好,体外释药具有缓释特点,为羟基喜树碱的临床应用提供了更广阔的前景。

Objective： To prepare hydroxycamptothecin semisolid lipid nanoparticles （HCPT-SSLN）. Methods：Based on the single-factor experiment, the HCPT-SSLN was prepared by using orthogonal design for optimization of formula and technology. Then the obtained SSLN was also evaluated. Results：The mean particle size of the prepared HCPT-SSLN was 130.5 nm, Polydispersity Index（PI） was 0.18, drug loading（DL） was 2.51% , entrapment efficiency （EE） was 79. 19% , Zeta potential was -33. 1 mV;the release rule in vitro was subject to Weibull equation ： lnln [ 1 / （ 1 - Q） 1 = 0. 263 3 lnt ＋ 0. 050 9 （ r = 0. 948 5 ）. The appearance, particle size and entrapment efficiency of SSLN were all stable at 4 ℃ for 6 months. Conclusion ：The HCPT-SSLN has high entrapment efficiency, drug loading, uniform particle size, good stability, and can retard drug release in vitro, so it provides an extensive prospect for clinical application of HCPT.