[关键词]
[摘要]
目的 以离子凝胶法制备黄芩苷-血根碱离子对壳聚糖纳米粒(BSI-CS-NPs)。方法 以单因素为主要考察方法,筛选最佳处方和制备工艺;采用透射电子显微镜(TEM)观察BSI-CS-NPs的形态,激光粒度分析仪测定粒径大小和Zeta电位,HPLC法检测包封率和载药量。结果 所制BSI-CS-NPs外观圆整,粒度分布均匀,平均粒径为326.4 nm,Zeta电位为45.7 mV,包封率为68.73%,载药量为26.68%。相比黄芩苷-血根碱离子对原料药,BSI-CS-NPs 2 h的药物累积释放率减少了约36.51%,12 h累积释放率为92.29%。结论 离子凝胶法适用于BSI-CS-NPs的制备,且具有缓释性能。
[Key word]
[Abstract]
Objective To prepare chitosan nanoparticles loading baicalin-sanguinarine ion-pair (BSI-CS-NPs) by ionic gelation method. Methods Based on the results of single factor experiments, four factors affecting the formulation were optimized by orthogonal design. The diameters and the Zeta potentials were measured by laser particle size analyzer. Transmission electron microscope (TEM) was used to observe the particle shapes, and HPLC was used to determine the entrapment efficiency and loading rate. Results The mean particle size was found to be 326.4 nm with a narrow particles distribution of polydispersity index. The Zeta potential of the optimized method-loaded chitosan nanoparticles was 45.7 mV, the drug entrapment efficiency was 26.68%, and the loading rate was 68.73%. The drug release degree of BSI-CS-NPs decreased about 36.51% in 2 h compared with BSI solution and the total drug release degree in 12 h was 92.29% with the sustained releasing behavior. Conclusion The method of ionic gelation is appropriate for the preparation of BSI-CS-NPs, and the BSI-CS-NPs have sustained releasing effect.
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[基金项目]
中比药物植物资源利用与作物病虫害防控新技术合作研究(2010DFA 32810)