摘要
目的:研制青蒿琥酯-壳聚糖纳米粒(ART-CS-NPs)并进行质量评价。方法:采用离子交联法制备ART-CS-NPs,以包封率和粒径为考察指标,通过单因素、正交设计试验优化制备工艺及处方,通过形貌观察、粒径和电位测定、体外释药考察对其进行质量评价。结果:以优化处方、工艺制备的ART-CS-NPs在透射电镜下呈现圆整、均匀的球形微粒,形态规则完整。粒径为(186.8±12.2)nm,PDI为(0.259±0.004),Zeta电位为(+31.7±1.5)mV,包封率为(69.4±1.4)%,载药量为(19.67±0.32)%。ART-CS-NPs体外释放曲线以Higuchi方程拟合结果最好。结论:离子交联法所制ART-CS-NPs形态规则完整,载药量、包封率较高,体外释放具有缓释作用,稳定性较好。
OBJECTIVE To study the formulation and preparation of artesunate-ehitosan nanoparticles (ART-CS-NPs). METHODS The ART-CS-NPs were prepared by ionic cross-linking. A single factor experiment and orthogonal experiment were used to inspect the effect regularity of various factors on the encapsulation efficiency and particle size. The ART-CS-NPs were evaluated by morphological observation, the particle size and Zeta potential measurement, in vitro release inspection. RE- SULTS AR'r C~%NPs prepared by optimized formulation were approximate to spheres, smooth with almost homogeneous structure. The mean diameter of ART-CS-NPs was (186. 8 + 12. 2) nm, PDI was (0. 259 -+ 0. 004) and Zeta potential was ( + 31.7 + 1.5)mV. The entrapment efficiency and drug-loading efficiency were (69. 4 + l. 4) ~/00 and (19. 67 + 0. 32) % respec- tively. The in vitro profiles of ART CS-NPs could be described by Higuchi equation. CONCLUSION ART-CS-NPs prepared by ionic cross-linking showed smooth surfaces with almost homogeneous structure. The entrapment efficiency and drug-loading ef- ficiency could meet the requirement of pharmaceutical design. Drug release property in vitro and physical stability of ART-CS- NPs was good.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2013年第5期349-355,共7页
Chinese Journal of Hospital Pharmacy
基金
湖北省卫生厅血防项目(编号:XF2010-20)
关键词
青蒿琥酯
壳聚糖
纳米粒
离子交联法
体外释放
artesunate
chitosan
nanoparticles
ionic cross-linking
in vitro release