青蒿琥酯-壳聚糖纳米粒的制备及质量评价

Preparation and quality assessment of artesunate-chitosan nanoparticles

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.