羟基红花黄色素A固体脂质纳米粒制备及质量评价

Preparation and quality evaluation of hydroxysafflor yellow A solid lipid nanoparticles

目的优化羟基红花黄色素A固体脂质纳米粒的处方和制备工艺,并对其质量进行评价。方法以羟丙基甲基纤维素为脂质材料,单硬脂酸甘油酯为乳化剂,利用热熔乳化超声-低温法制备羟基红花黄色素A固体脂质纳米粒;选用包封率为指标,以羟丙基甲基纤维素、纯净水、单硬脂酸甘油酯、吐温80水溶液(1%)用量为考察因素,利用正交设计法优化处方和制备工艺,透析法测定包封率;通过透射扫描电镜观察纳米粒形态和均匀度,纳米粒度仪测定其粒径、分散指数及Zeta电位;以累积释药百分率为指标,评价羟基红花黄色素A的体外释药特性。结果最佳工艺条件为5 mg羟丙基甲基纤维素、0.2 ml纯净水、100 mg单硬脂酸甘油酯、1.8 ml吐温80水溶液(1%);制备的固体脂质纳米粒为近圆球状,粒径分布较均匀,纳米粒的平均粒径(99.85±3.04)nm,多分散指数(0.390±0.021),Zeta电位(-27.63±2.12)mV,包封率为(63.35±2.65)%,8 h释放率为(44.35±0.49)%。结论羟基红花黄色素A固体脂质纳米粒具有较好的均匀度及良好的缓释性能。

Objective To optimize the formulation and preparation technology of hydroxy safflower yellow A solid lipid nanoparticles and evaluate its quality.Metheds Hydroxy safflower yellow A solid lipid nanoparticles were prepared by the method of hot melt emulsification ultrasonic-low temperature using hydroxypropyl methylcellulose as a lipid material and glyceryl monostearate as an emulsifier.Using entrapment efficiency as indexes,the amount of hydroxypropyl methylcellulose,purified water,glyceryl monostearate,and Tween 80 aqueous solution(1%)as factors,orthogonal test was applied to optimize the formulation and preparation technology.Dialysis method was used to measure encapsulation efficiency.The morphology and uniformity of the nanoparticles were observed by transmission scanning electron microscopy.The particle size,polydispersion index and Zeta potential were determined by nano-particle size analyzer.And hydroxy safflower yellow A solid lipid nanoparticles sustained releasing characteristics was evaluated by the percentage of cumulative drug release.Results The optimal process of prepared hydroxy safflower yellow A solid lipid nanoparticles was 5 mg of hydroxypropyl methylcellulose,0.2 ml of purified water,100 mg of glyceryl monostearate,and 1.8 ml of Tween 80 aqueous solution(1%).The size of the prepared nanoparticles was uniform and spherical.And the average particle size were(99.85±3.04)nm,polydispersion index were(0.390±0.021),Zeta potential were(-27.63±2.12)mV,and the encapsulation efficiency of the hydroxy safflower yellow A solid lipid nanoparticles were(63.35±2.65)%.The release rate of the nanoparticles was(44.35±0.49)%.Conclusions The prepared hydroxy safflower yellow A solid lipid nanoparticles have good uniformity and good sustained release properties.