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目的:制备叶酸偶联聚合物修饰的紫杉醇纳米脂质载体,并对处方工艺进行优化,考察其体外释放。方法:采用超声分散法制备纳米脂质载体,采用正交设计优化处方,透射电镜观察微观形态,激光粒度分析仪测定粒径及分布,电位仪测定Zeta电位,应用超滤法测定纳米脂质载体的包封率;以累积释药百分率为指标,通过方程拟合释药曲线,考察制剂的体外释药特性。结果:优化处方制得的脂质载体的平均粒径(132±18)nm,Zeta电位(-18.8±6.69)m V,包封率88.40%,制剂24 h体外累积释药百分率为39.3%,体外释放符合Higuchi方程Q=0.090t1/2-0.034(r=0.9975)和Weibull方程Q=0.764 t1/2-2.988(r=0.9965)。结论:本实验获得了较理想的叶酸偶联聚合物修饰的紫杉醇纳米脂质载体,其体外释放特性符合缓释制剂特征。
OBJECTIVE: To prepare the folate conjugated polymer modified paclitaxel nano-lipid carrier and to optimize the formulation process to investigate its in vitro release. Methods: The nano-lipid carrier was prepared by ultrasonic dispersion method. The orthogonal design was used to optimize the prescription. The morphology was observed by transmission electron microscopy. The particle size and distribution were determined by laser particle size analyzer. Zeta potential was measured by potentiometer. Of the encapsulation efficiency; cumulative release rate as an indicator, through the equation fitting release curve, study formulations in vitro release characteristics. RESULTS: The average diameter of lipid carrier prepared by optimized formulation was (132 ± 18) nm, the Zeta potential was (-18.8 ± 6.69) mV, the entrapment efficiency was 88.40%. The cumulative drug release percentage was 39.3% In vitro release was in accordance with the Higuchi equation Q = 0.090t1 / 2-0.034 (r = 0.9975) and Weibull equation Q = 0.764 t1 / 2-2.988 (r = 0.9965). Conclusion: In this study, the ideal folate conjugated polymer modified paclitaxel nano-lipid carrier, in vitro release characteristics in line with the characteristics of sustained-release preparations.