叶酸偶联聚合物修饰的紫杉醇纳米脂质载体制备及性质研究  

Studies on Preparation and Properties of Folate-poly(PEG-cyanoacrylate-co-cholesteryl cyanoacrylate) Modified Paclitaxel-loaded Nanostructured Lipid Carriers

作　　者：王晶[1] 

机构地区：[1]辽宁中医药大学附属医院,辽宁沈阳110032

出　　处：《辽宁中医药大学学报》2017年第5期64-67,共4页Journal of Liaoning University of Traditional Chinese Medicine

摘　　要：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 folate-poly（PEG-cyanoacrylate-co-cholesteryl cyanoacrylate）modified paclitaxel-loaded nanostructured lipid carriers,to optimize the fornulation by orthogonal experiment design,and evaluate its in vitro release behavior. Methods：Nanostructured lipid carriers were prepared by film and ultrasonic dispersion method. The particlesize distribution of nanostructured lipid carrierwas examined by laser particle size analyzer. The zetapotential of nanostructured lipid carrier was examined by potential instrument. The encapsulation efficiency of the nanostructured lipid carriers were examined by ultrafiltration method. The property of their release in vitro was investigated,based on the measure of accumulated release ratio and the fitting of release curve. Results：The optimized result showed that the nanostructured lipid carriers were blue with an average diameter of（132±18）nm,zeta potential（-18.8±6.69）mv,encapsulation efficiency of 88.40%,and 24 h-accumulated release ratio of 39.3%,in vitro releasewas in line with Higuchi equation Q=0.0564 t1/2-0.0322（r=0.9719）and Weibul equation Q=0.764 t1/2-2.988（r=0.9965）. Conclusion：This formulation method obtained ideal folate-poly（PEGcyanoacrylate-co-cholesteryl cyanoacrylate）modified paclitaxel-loaded nanostructured lipid carriers,in its vitro release characteristics was in line with property of sustained-released preparation.

关 键 词：药剂学 纳米脂质载体 正交设计 紫杉醇 

分 类 号：R284[医药卫生—中药学]