摘要
目的制备表没食子儿茶素没食子酸酯(EGCG)壳聚糖(CS)纳米粒(EGCG-CS-NPs),并初步评价其理化性质。方法采用离子凝胶化法制备EGCG-CS-NPs,通过对处方优化:CS质量浓度(X_1)、三聚磷酸钠(TPP)质量浓度(X_2)、EGCG质量浓度(X_3)为考察对象,以包封率(Y_1,%)、平均粒径(Y_2,nm)为评价指标,利用Box-Behnken设计-效应面法优化EGCG-CS-NPs处方;采用Malvern粒度仪测定EGCG-CS-NPs的粒径分布和Zeta电位,透射电镜考察其形态;并考察EGCGCS-NPs的体外释药行为。结果 EGCG-CS-NPs的最优处方:CS质量浓度为2.6 g/L、TPP质量浓度为1.5 g/L、EGCG质量浓度为2.7 g/L,制备的EGCG-CS-NPs的包封率为(85.8±3.1)%;粒径为(102.2±27.1)nm,Zeta电位为(25.5±4.1)m V;透射电镜显示EGCG-CS-NPs粒径均一,呈球状;EGCG-CS-NPs在24 h内平稳缓慢释药(p H 4.5 PBS)。结论通过对处方的优化,制备得到圆整、释药缓慢的EGCG-CS-NPs,为进一步考察EGCG-CS-NPs在大鼠体内药效学奠定了基础。
Objective To prepare the epigallocatechin-3-gallate (EGCG) chitosan nanoparticles (CS-NPs) and investigate their physicochemical properties. Methods The EGCG-CS-NPs were prepared by ion gelation method. The formulation variables were optimized by Box-Behnken Design (BBD) of response surface methodology (RSM) of CS concentration (X0, sodium tripolyphosphate concentration (X2), and EGCG concentration (X3) as independent variables and encapsulation efficiency (Y1, %) and particle size (Y2, nm) as dependent variables. The optimized CS-NPs were characterized for encapsulation efficiency (EE), particle size, Zeta potential, morphology, and in vitro drug release behavior of EGCG-CS-NPs were studied. Results An optimal EGCG-CS-NPs consisting of CS concentration as 2.6 g/L, sodium tripolyphosphate concentration as 1.5 g/L and EGCG concentration as 2.7 g/L. For EE, particle size, Zeta potential of EGCG-CS-NPs were found to be (85.8 ±3.1)%, (102.2 ± 27.1) nm, and (25.5 ± 4.1) mV, respectively. The CS-NPs were found to be small and spherical as seen in transmission electron microscopy (TEM). The in vitro release data proved that the drug release was steady within 24 h (pH 4.5 PBS). Conclusion Through optimizing the formulation, we obtain the uniform EGCG-CS- NPs with in vitro sustained-release behavior. This work is useful for the further research on pharmacodynamics of EGCG-CS-NPs.
出处
《中草药》
CAS
CSCD
北大核心
2016年第5期741-747,共7页
Chinese Traditional and Herbal Drugs
基金
中国科学院"西部之光"人才培养计划项目资助
陕西省科技新星计划项目(2013KJXX-71)
陕西省中医药管理局中医药科研课题(15-ZY001)