脑靶向银杏内酯聚氰基丙烯酸正丁酯纳米球的制备方法比较_药学论文.docVIP

脑靶向银杏内酯聚氰基丙烯酸正丁酯纳米球的制备方法比较_药学论文 脑靶向银杏内酯聚氰基丙烯酸正丁酯纳米球的制备方法比较_药学论文 【摘要】 　　目的比较中药银杏内酯A(GA)聚氰基丙烯酸正丁酯纳米球（PBCA-NP）的两种不同制备方法，同时考察稳定剂右旋糖酐-70对纳米球制备的影响。方法以稳定剂右旋糖酐-70作对比实验，采用乳化聚合法和界面缩聚法制备GA-PBCA-NP。在透射电镜下观察其形态，用高效液相－蒸发光散射检测器（HPLC-ELSD）测定各自的包封率和载药量，并观察GA-PBCA-NP的稳定性。结果未添加稳定剂的纳米球表面粘连团聚现象严重，难以成球；乳化聚合法制备的GA-PBCA-NP在透射电镜下观察表面圆整光滑，粒子之间不团聚，不黏连，粒径范围在90～600 nm，包封率为60.49%，载药量为18.15%；界面缩聚法制得的纳米粒表面圆整光滑，粒子之间不团聚，不黏连，粒径大小均匀，都在200 nm左右，包封率为73.87%，载药量为22.23%，两种方法制备的稳定性都较好。结论制备纳米粒过程中需加入适量稳定剂；界面缩聚法制备GA-PBCA-NP具有粒径均匀、载药量和包封率高的特点，优于乳化聚合法。 【关键词】 银杏内酯； 聚氰基丙烯酸； 正丁酯； 纳米球； 乳化聚合法； 界面缩聚法 　　Abstract：ObjectiveTo compare the ginkgolide A(GA) polybutylcyanoacrylate nanoparticles(PBCA-NP) produced by the two methods so as to investigate the effect of stabilizer dextran 70 on preparation.MethodsGA was incorporated into PBCA-NP by emulsification polymerization and interfacial polymerization methods separately.The effect of dextran 70 on preparation wasinvestigated.Transmission electron microscopy was employed to study the shape.The bedding ratio and drug loading were determined with HPLC-ELSD.The stability of GA-PBCA-NP was also studied.ResultsDue to the agglomerationg of nanoparticles with no stabilizer,it was difficult to preparate.GA-PBCA-NP produced by the two methods both had spheric and smooth outer appearance,uniform distribution,nonadherence and stability.The diameter,ebeding ratio and drug loading in GA-PBCA-NP produced by emulsification polymerization and interfacial polymerization methods were 90～600 nm and 200 nm,60.49% and 73.87%,18.15% and 22.23%,respectively.ConclusionIt is important to add dextran 70 in preparation.The interfacial polymerization method which is better than emulsification polymerization method is an effective method to produce the GA-PBCA-NP. 　　Key words：Ginkgolide; Polybutylcyanoacrylate; Nanoparticles; Emulsification; Polymerization method; Interfacial polymerization method 纳米球(nanospheres, NP)是一类以天然或合成高分子材料为载体的固态胶体微粒，粒径大约在10～1 000 nm。NP是一种控释的胶体给药系统［1］，与其它微粒给药系统比较，NP具有更多优点，比如生