摘要
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.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2009年第3期272-276,共5页
Chinese Journal of New Drugs
基金
2003年广东省科技计划项目(2003A1070103)
关键词
羟基喜树碱
半固体脂质纳米粒
正交设计
体外释药
hydroxycamptothecin
semisolid lipid nanoparticles （SSLN）
orthogonal design
drug-release in vitro
