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作 者:李晓珊 李凯童 金三娣 胡巧红 LI Xiaoshan;LI Kaitong;JIN Sandi;HU Qiaohong(School of Pharmacy,Guangdong Pharmaceutical University/Guangdong Engineering&Technology Research Center of Local Precision Drug Delivery System,Guangzhou 510006,China)
机构地区:[1]广东药科大学药学院/广东省局部精准药物递药制剂工程技术研究中心,广州510006
出 处:《中国药房》2021年第19期2383-2387,共5页China Pharmacy
摘 要:目的:优化姜黄素(CUR)醇传递体(CUR-TEs)的处方。方法:采用高效液相色谱法测定CUR-TEs中CUR的含量。采用注入法制备CUR-TEs,并以包封率和载药量的综合评分为指标,在单因素实验的基础上,采用Box-Behnken设计-响应面法对其处方进行优化及验证,然后考察以最优处方制得的CUR-TEs的性质。结果:CUR-TEs的最优处方为卵磷脂用量4%、CUR用量0.13%、1,2-丙二醇用量25%、聚山梨酯80用量1%。最优处方的验证实验结果显示,CUR-TEs包封率和载药量的综合评分为93.04±2.16,与预测值(91.19)的相对误差为2.03%。以最优处方所制得的CUR-TEs的包封率为(91.17±1.35)%、载药量为(0.94±0.02)%、粒径为(190.64±15.97)nm、多分散系数(PDI)为0.086±0.007、Zeta电位为(-12.74±1.60)mV。结论:优化后的CUR-TEs处方稳定性良好,具有可行性和可重复性;所制得的CUR-TEs具有较好的稳定性。OBJECTIVE:To optimize the formulation of Curcumin(CUR)transethosomes(CUR-TEs).METHODS:The contents of CUR in CUR-TEs were determined by HPLC.CUR-TEs were prepared by injection method.Using comprehensive score of encapsulation efficiency and drug loading as index,based on signal factor test,Box-Behnken design-response surface method was used to optimize and validate the formulation.The property of CUR-TEs prepared by the optimal formulation was investigated.RESULTS:The optimal formulation of CUR-TEs was as follows as lecithin of 4%,CUR of 0.13%,1,2-propylene glycol of25%,tween-80 of 1%.Results of validation test of optimal formulation showed that comprehensive score of encapsulation efficiency and drug loading of CUR-TEs was 93.04±2.16,relative error of which to predicted value(91.19)was 2.03%.The encapsulation efficiency of CUR-TEs prepared by optimal formulation was(91.17±1.35)%,and its drug loading was(0.94±0.02)%.The particle size was(190.64±15.97)nm with polydispersity index of 0.086±0.007,and Zeta potential was(-12.74±1.60)mV.CONCLUSIONS:The optimized formulation of CUR-TEs is stable,feasible and repeatable,with good stability.
关 键 词:姜黄素 醇传递体 高效液相色谱法 Box-Behnken设计-响应面法 处方优化
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