目的 优化雷公藤内酯醇纳米脂质体(TP-NLS)的处方及制备工艺。方法 采用高压均质法制备TP-NLS。依据均匀设计U₇(7³) 实验方法,以两种脂类基质a与b的配比(A)、泊洛沙姆188的用量(B)和均质压力(C)为考察因素,以包封率、平均粒径和Zeta电位为考察标准,优选TP-NLS的处方及制备工艺。结果 最优处方为A₁B₅C₇,即按制备600 mL TP-NLS溶液,所取脂类基质a为1.2 g,b为0.2 g,泊洛沙姆188的用量为1.3 g,均质压力70 MPa,均质乳匀15 min。制备的TP-NLS溶液外观好,平均包封率为83.52%,平均粒径117 nm,Zeta电位31.7 mV。所得TP-NLS溶液置于4 ℃,避光环境下保存30 d,包封率、粒径、电位等基本保持不变,稳定性良好。结论 优化后的TP-NLS制备工艺简单易行,为其进一步研究奠定了基础。

Objective: To optimize the preparation method of triptolide-nano-liposomes (TP-NLS). Methods High pressure homogeneous method was used to prepare TP-SLN. According to even design U₇(7³), the preparation method of TP-SLN was optimized with the factors including weight ratio of phosphorlipid and cholesterol (A), quantity of Poloxamer 188 (B), and homogeneous pressure (C), using the encapsulation efficiency (EE), particle size, and Zeta potential of NLS as indexes. Results The optimum prescription of TP-NLS was A₁B₅C₇, i.g. lipid matrix a : b was 6 : 1, the dosage of Poloxamer 188 was 1.3 g, and the homogeneous pressure was 70 MPa, high pressure homogeneous method for 15 min. The TP-NLS prepared with the optimal method had good appearance. The EE was 83.52%, the average particle size was 117 nm, and the Zeta potential was 31.7 mV. TP-NLS solution was kept in avoiding light environment at 4 ℃ for 30 d, and the preservation stability was good. Conclusion The formula is reasonable and the preparation method of TP-NLS is feasible, which is valuable to further study.

国家卫生与计划生育委员会科研基金课题(WKJ-FJ-15);福建省省属公益类科研院所基本科研专项(2015R1031-4,2014R1031-3);福建省科技计划社会发展引导性(重点)项目(2014Y0051);福建省卫生厅中医药科研项目(wzze201306)