淫羊藿苷隐形固体脂质纳米粒冻干粉制备及质量控制

Preparation and quality research of icariin stealth solid lipid nanoparticles lyophilized powder

目的:对淫羊藿苷隐形固体脂质纳米粒的冻干工艺进行优化并考察了其理化性质。方法:以冻干粉末的外观、色泽和再分散性为指标综合评价,优选处方比例;通过测定粒径、外观形态和体外释放度,对比了淫羊藿苷隐形固体脂质纳米粒冻干前后理化性质的变化。结果:制得的淫羊藿苷隐形固体脂质纳米粒冻干粉包封率为(74.00±1.45)%,载药量为(2.95±1.12)%,平均粒径(359.53±6.71)nm,Zeta电位-(33.79±2.96)mV;在生理盐水中,淫羊藿苷隐形固体脂质纳米粒冻干粉16 h累积释放37.48%。结论:优化处方制得隐形固体脂质纳米粒冻干粉具有较高包封率和载药量,体外释药符合Higuchi方程。

OBJECTIVE To optimize the physical and chemical properties of the icariin stealth solid lipid nanoparticles（Ica- SSLN） lyophilized powder and investigate their physical and chemical properties. METHODS The appearance, color and re- dispersibility of lyophilized powder were taken as the comprehensive evaluation indexes, and the prescription proportion was optimized. By measuring the particle size, morphology and in vitro release, the changes of physieochemical properties of icariin stealth solid lipid nanoparticles were compared before and after lyophilization. RESULTS The entrapment efficiency and the ratio of loading drug of Ica-SSLN was （74. 00 ± 1.45） %, and （2. 95 ± 1.12）%, respectively. The average diameter was （359. 53 ± 6. 71）nm and the Zeta potential was - （33.79 ± 2. 96）mV. In normal saline, the in vitro cumulative release rate of the drug from icariin stealth solid lipid nanoparticles lyophilized powder with 16 h was 37.48%. CONCLUSION The applica tion of the uniform design is useful to achieve a high entrapment efficiency and ratio of loading, and the diameter is great saris faction. The in vitro cumulative release was described by Higuchi equation.