丹参酮ⅡA纳米结构脂质载体的制备及体外评价

摘要

目的：以丹参酮ⅡA为模型药物，制备丹参酮ⅡA纳米结构脂质载体，进行处方优化，并进行体外评价。方法采用乳化－超声分散法制备丹参酮ⅡA–NLC，以包封率为评价指标，并进行方法学验证。采用正交试验筛选丹参酮ⅡA－NLC的最优处方。通过测定丹参酮ⅡA －NLC的形态与粒径、包封率、载药量、Zeta电位对其进行体外评价。结果最优处方为模型药物用量0.5mg、脂质浓度为3％、乳化剂比为1：1、固液脂质比为1：4。制备的丹参酮ⅡA–NLC包封率为（76.83±1.701）％、载药量为（0.5564±1.113）％、粒径分布均匀、Zeta电位为－（26.6±0.87）mV。结论通过乳化－超声分散法制备出的丹参酮ⅡA–NLC，粒径分布均匀，多分布在100～200nm之间，包封率和稳定性良好。%Objective To prepare TanshinoneⅡA loaded nanostructured lipid carriers , formulation optimization was conducted , and then evaluate its quality in vitro.Methods TanshinoneⅡA was prepared by emulsion -ultrasonic dispersion method.With encap-sulation efficiency as index and UV -visible spectrophotometry as method validation.Using orthogonal test to choose the optimal pre-scription for TanshinoneⅡA-NLC.and evaluate TanshinoneⅡA-NLC in uitro by measuring the shape and particle size , encapsula-tion efficiency , drug loading and zeta potential.Results Optimum preparation technology was as following:the amount of drug 10 mg, lipid concentration 3%, emulsifier ratio 1:1, and the solid -liquid lipid ratio 1:4.The encapsulation efficiency was (76.83 ± 1.701)%, drug loading (0.5564 ±1.113)%, particle size distributed uniform and zeta potential was -26.6 ±0.87mV with Tan-shinoneⅡA-NLC.Conclusion This prepared TanshinoneⅡA-NLC had uniform particle size distribution , high encapsulation effi-ciency and stability.