摘要
目的 制备白藜芦醇纳米结构脂质载体(Res-NLCs),并对其进行理化性质和体外释放特性的考察.方法 采用乳化蒸发-高压均质法制备Res-NLCs,通过正交试验得出最优处方,并对最优处方制得的Res-NLCs进行理化性质考察;通过HPLC建立白藜芦醇体外释放方法学,采用动态透析法对Res-NLCs的体外释药特性进行考察.结果 Res-NLCs的最优处方为:双硬脂酸甘油酯用量为0.0356g,大豆磷脂用量为0.3918g,Tween-80的质量浓度为4.25％,辛酸癸酸聚乙二醇甘油酯用量为0.0475 g.经透射电镜观察Res-NLCs呈规则圆球状,分散均匀.测得Res-NLCs的平均粒径为(81.87±0.14)nm,多分散系数为(0.099±0.02),Zeta 电位为(-8.09±0.75)mV,包封率为(98.43±0.07)％,载药量为I(11.04±0.14)％.体外释放结果显示,白藜芦醇溶液在8h释放97.31％,而Res-NLCs则缓慢持续释放,并在48 h后达到释放平台,累计释放的白藜芦醇为80.69％.结论 通过乳化蒸发-高压均质法制备的Res-NLCs粒径小,分散均匀,具有较高的包封率及载药量,并可显著延长白藜芦醇释放的时间,具有良好的缓释效果.
Abstract
Objective To prepare resveratrol nanostructured lipid carriers(Res-NLCs)and comprehensively assess their physical and chemical attributes,as well as in vitro release characteristics.Methods Res-NLCs were formulated with the emulsification evaporation-high-pressure homogenization method.An orthogonal experimental design was used to optimize the formulation.The physical and chemical properties of Res-NLCs were meticulously analyzed.An HPLC method was established to quantify the in vitro resveratrol release,while forward dynamic membrane dialysis was used to evaluate drug release kinetics.Results The optimal Res-NLC formulation consisted of 0.0356 g glycerol stearate,0.3918 g soybean phospholipid,a 4.25％mass concentration of Tween-80,and 0.0475 g polyethylene glycol caproate.Transmission electron microscopy revealed that Res-NLCs were spherical and well-dispersed.Res-NLC particles had an average size of(81.87±0.14)nm,a polydispersity coefficient of(0.099±0.02),and a Zeta potential of(-8.09±0.75)mV.These Res-NLCs exhibited high encapsulation efficiency(98.43±0.07)％and drug loading(11.04±0.14)％.In vitro release studies indicated that the resveratrol solution released 97.31％at 8 hours,while Res-NLCs released sustainably.Subsequently,Res-NLCs reached a release plateau after 48 h,with a cumulative release of 80.69％.Conclusion Res-NLCs prepared via emulsification evaporation-high-pressure homogenization,exhibit small and uniformly distributed particles,high encapsulation efficiency,and substantial drug loading capacity.Extension of the release duration of resveratrol,demonstrate an effective sustained release profile.
基金项目
哈尔滨医科大学药学院杰出青年人才基金(2019-JQ-03)
维普
万方数据