羟基喜树碱脂质体的制备及质量评价研究

目的:制备羟基喜树碱(HCPT)脂质体,并对其质量进行评价.方法:采用薄膜分散-高压乳匀法制备羟基喜树碱脂质体;用激光粒度分析仪测定其Zeta电位、粒径大小;考察其在0.9%NaCl溶液、水、5%葡萄糖溶液中8 h的稳定性;用凝胶柱层析法考察包封率;采用薄膜透析法考察体外释药性质.结果:羟基喜树碱脂质体Zeta电位为(-33.1±1.3) mV,平均粒径(182.5±5.6) nm,8 h内在水、5%葡萄糖溶液中稳定性良好;包封率(91.2±1.2)%;体外释药曲线符合Higuchi方程Q=1.291 6t1/2 0.309 8,r=0.980 3.结论:本试验制备的羟基喜树碱脂质体稳定性好,大小均匀, 包封率高,并具有延缓药物释放的性质.

Preparation and quality evaluation of 10-hydroxycamptothecin nanoliposomes

Objective:To prepare and evaluate the quality of HCPT liposomes. Method: HCPT liposomes were prepared by film dispersion-high-pressure homogenization method. The shape of liposomes, particles size, zeta potential and stability in 0.9%NaCl solution, water, 5% glucose solution for 8 hours were evaluated; Sephadex-G50 column was used to study the entrapment efficiency; dialyzer was used to study the release of HCPT in vitro. Result: The average diameter and zeta potential of HCPT liposomes were (182.5±5.6) nm and (-33.1±1.3) mV, these liposomes were stable in water and 5%glucose solution for 8 hours. The entrapment efficiency was (91.2±1.2) %. The drug release curve accorded with Higuchi equation: Q=1.2916t^1/2+0.3098 (r=0.9803). Conclusion: The HCPT liposomes have good stablity, uniformal size, which could retard drug release prominently in vitro.