叶酸-壳聚糖修饰胡椒碱纳米结构脂质载体的制备及其体外释放研究

Preparation and in Vitro Release Study of Folic Acid-Chitosan Modified Piperine Nanostructured Lipid Carriers

目的制备叶酸-壳聚糖修饰的胡椒碱纳米结构脂质载体(FA-CS-PIP-NLC),并评价其体外释放性能。方法通过叶酸与壳聚糖反应、纯化后得叶酸-壳聚糖复合物(FA-CS),以胡椒碱为模型药物,采用溶剂注入法制备胡椒碱纳米结构脂质载体(PIP-NLC),采用电荷吸附法制备FA-CS-PIP-NLC,并考察其形态特征、粒径、分散系数、Zeta电位、包封率、载药量,以及在不同pH介质中的体外释药特性。结果制备的FA-CS-PIP-NLC呈球形或近球形,粒径为(130.6±3.7)nm,分散系数为0.26±0.01,Zeta电位为(2.9±1.2)mV,包封率为(89.63±2.07)%,载药量为(1.28±0.33)%,在pH 7.4和pH 5.5磷酸盐缓冲液中48 h的胡椒碱累计释放率分别为65.42%和69.73%。结论所制备的FA-CS-PIP-NLC粒径小,稳定性好,包封率高,缓释性能良好。

Objective To prepare folic acid-chitosan modified piperine nanostructured lipid carrier(FA-CS-PIP-NLC),and to evaluate its in vitro release properties.Methods Folic acid-chitosan complex(FA-CS)was prepared by reacting and purifying folic acid with chitosan.Piperine was used as a model drug to prepare piperine nanostructured lipid carrier(PIP-NLC)by solvent injection method.FA-CS-PPI-NLC was prepared by the charge adsorption method,and its morphological characteristics,particle size,dispersion coefficient,Zeta potential,encapsulation efficiency,drug loading capacity,and in vitro release characteristics in different pH release media were investigated.Results The prepared FA-CS-PPI-NLC was spherical or nearly spherical,with a particle size of(130.6±3.7)nm,a dispersion coefficient of 0.26±0.01,a Zeta potential of(2.9±1.2)mV,an encapsulation efficiency of(89.63±2.07)%,and a drug loading capacity of(1.28±0.33)%.The cumulative release rates of FA-CS-PIP-NLC in phosphate buffer solutions(pH 7.4 and pH 5.5)release medium for 48 h were 65.42%and 69.73%,respectively.Conclusion The prepared FA-CS-PPI-NLC has a small particle size,good stability,high encapsulation efficiency,and good sustained release properties.