依托泊苷固体脂质纳米粒的研制

摘要

OBJECTIVE: To prepare Etoposide-loaded solid lipid nanoparticles (ET-SLN) and to investigate the physical and chemical properties. METHODS: Emulsion-ultrasonic dispersion method was used to prepare ET-SLN. The formula was optimized by orthogonal test with amount of glycerin monostearate (A), soy lecithin (B), poloxamer 188 (C), etoposide (D) as factors using encapsulation coefficency as index. The particle size, Zeta potential, encapsulation efficiency and in vitro release of the ET-SLN were investigated. RESULTS: Amounts of A, B, C, D were 0.020 mg, 0.010 mg, 0.015 mg, 0.015 mg. The average particle size was (83 ± 0.5) nm with Zeta potential of (- 23 ± 0.3) mV. The encapsulation coefficency was 81.2%. In vitro release test showed a significant sustained release for 48 h. CONCLUSION: Prepared ET-SLN is in line with requirements of pharmaceutics.%目的:制备依托泊苷固体脂质纳米粒(ET-SLN)并考察其药剂学性质.方法:采用乳化-超声分散法制备ET-SLN,以单硬脂酸甘油酯(A)、大豆磷脂(B)、泊洛沙姆188(C)、依托泊苷(D)的处方用量为考察因素,包封率为指标设计正交试验,筛选最优处方.考察纳米粒的粒径、表面电位、包封率、体外释放情况等.结果:A、B、C、D分别为0.020、0.010、0.015、0.015 mg;所制纳米粒平均粒径(83±0.5) nm,表面电位(-23±0.3)mV,包封率81.2％,可持续48h缓释.结论:所制ET-SLN符合药剂学性质要求.