羟基喜树碱半固体脂质纳米粒制备工艺研究

Study on the Preparation Technology of Hydroxycamptothecin Semisolid Lipid Nanoparticles

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纳米溶液进行质量评价。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%,ξ电位为-33.1mV;纳米溶液4℃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,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 orthogonal design for optimization of formulation and technology. Then the obtained SSLN was evaluated. Results The mean particle size of the prepared HCPT -SSLN was 130.5nm, Polydispersity index（PI） was 0.18, drug loading（DL） was 2.51% , entrapment efficiency（EE） was 79.19% , ξ potential was - 33. lmV; Placed at 4℃ for 6 months, the appearance, particle size and entrapment efficiency of SSLN were all stable. Conclusion The HCPT- SSLN has high entrapment efficiency and drug loading, uniform particle size, good stability, which provides an extensive prospect for clinical application of HCPT.