目的 制备漆黄素固体脂质纳米粒(FIT-SLN),对其进行质量评价并考察其体外释放作用.方法 采用乳化蒸发-低温固化法制备FIT-SLN,利用Box-Behnken设计试验优化处方工艺,并制成冻干粉末.考察其外观、粒径、Zeta电位,并通过差示量热扫描仪判断药物在FIT-SLN冻干粉中的存在状态,透析袋法评价制剂在不同介质中的体外释放行为.结果 FIT-SLN的最佳制备工艺:漆黄素用量3 mg、吐温80用量115μL、双硬脂酸甘油酯(Precirol ATO 5)用量30 mg、卵磷脂用量30 mg.所得FIT-SLN的粒径、Zeta电位、包封率分别为(124.53±2.00)nm、(-21.33±1.69)mV、77.89％,体外释放规律与一级动力学方程相符.结论 成功制备粒径小、包封率高的FIT-SLN,其具有一定的缓释能力.
Preparation and in vivo release of fisetin solid lipid nanoparticles
Objective To prepare fisetin solid lipid nanoparticles(FIT-SLN),evaluate their quality and determine its in vitro release.Methods FIT-SLNs were prepared by emulsion evaporation-cryogenic curing method,and the prescription process was optimized with Box-Behnken design experiment and made into lyophilized powder.The appearance,particle size,and Zeta potential were examined,and the presence of the drug in the lyophilized powder of FIT-SLN was determined by differential scanning calorimetry.The in vitro release behavior of the preparation was evaluated by the dialysis bag method.Results The optimal preparation of FIT-SLN was as follows:3 mg fisetin,115 μL Tween 80,30 mg Precirol ATO 5,and 30 mg lecithin.The particle size,Zeta-potential,and encapsulation rate of FIT-SLN were(124.53±2.00)nm,(-21.33±1.69)mV,and 77.89％,respectively.The in vitro release was in accordance with the first-order kinetics equation.Conclusion FIT-SLN with small particle size and high encapsulation rate are successfully prepared with slowly release.
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