葛根素纳米粒的制备工艺研究

Investigation on the Prescription and Preparation Technology of Puerarin Nanoparticles

目的:考察苯硼酸化壳聚糖载葛根素纳米粒(PBACS-TPP-Pur-NPs)的处方及其制备工艺。方法:采用离子凝胶化法制备PBACS-TPP-Pur-NPs,以粒径、PDI、电位、包封率、载药量为评价指标,考察的因素主要包括3-羧基苯硼酸化壳聚糖(PBACS)的取代度、PBACS的浓度、三聚磷酸钠(TPP)的浓度、PBACS的pH、搅拌转速和搅拌时间。筛选出最优处方工艺,并对优化所得纳米粒的基本性质和体外释药性能进行表征评价。结果:制备PBACS-TPP-Pur-NPs的最佳处方工艺为PBACS浓度为1.5 mg/mL,TPP浓度为1.4 mg/mL,PBACS的pH为5.5,搅拌转速为390.0 r/min,搅拌时间为30 min。优化所得的PBACS-TPP-Pur-NPs粒径适中均一、载药能力强、稳定性良好、具有明显的缓释特征。结论:该方法有效可行,适用于优化葛根素纳米粒的处方与制备工艺,为葛根素纳米制剂的开发提供稳定基础。

Objective:To investigate the formulation and preparation process of phenyl borated chitosan-loaded Puerarin nanoparticles(PBACS-TPP-Pur-NPs).Methods:PBACS-TPP-Pur-NPs were prepared by ion gelation method.With the particle size,PDI,potential,encapsulation efficiency and drug loading rate as evaluation indicators.The factors investigated mainly included:degree of substitution of 3-carboxyphenyl borated chitosan(PBACS),concentration of PBACS,concentration of sodium tripolyphosphate(TPP),pH of PBACS,stirring speed and stirring time.The optimal formulation process was screened out,and the basic properties and in vitro drug release performance of the optimized nanoparticles were characterized and evaluated.Results:The optimized PBACS-TPP-Pur-NPs had moderate and uniform formulation process for preparing PBACS-TPP-Pur-NPs was as follows:the concentration of PBACS was 1.5 mg/mL,the concentration of TPP was 1.4 mg/mL,the pH of modified chitosan was 5.5,the stirring speed was 390.0 r/min,and the stirring time was 30 min.The prepared PBACS-TPP-Pur-NPs have moderate and uniform particle size,strong drug loading capacity,good stability,and obvious slow-release characteristics.Conclusion:The method is effective and feasible,which is suitable for optimizing the formulation and preparation process of Puerarin loaded nanoparticles,and provides a stable basis for the development of Puerarin nanoparticles.