【摘要】 目的 制备脱氧胆酸修饰的脂质体，进一步提高姜黄素的胃肠道稳定性和口服吸收。方法 采用薄膜分散结合超声法制备姜黄素脂质体（Cur-L）,后采用静电吸附法将脱氧胆酸壳聚糖结合物（deoxycholic acid-modified chitosan, DCS）吸附在Cur-L表面制成DCS修饰的姜黄素脂质体（Cur-DL）,采用傅里叶变换红外光谱和核磁共振氢谱表征合成的DCS,采用动态光散射法测定各脂质体的粒径及Zeta电位，采用透射电镜观察脂质体的形态，采用动态透析法进行体外释放实验，以大鼠为实验动物研究体内药物动力学并采用小动物活体成像技术研究体内分布。结果 Cur-DL的平均粒径为（138.70±5.50）nm, PDI为0.14±0.02。Cur-L和Cur-DL在胃pH模拟液中2 h释药分别为30.81%和15.03%,大鼠体内药物动力学实验结果表明Cur-DL的AUC_0-∞是姜黄素混悬液（Cur-Sus）组的5.78倍，是Cur-L组的2.18倍。给药24 h后的组织分布实验结果表明，Cur-DL组的各器官平均荧光强度值均比其他组高，Cur在肝和肾中分布最多。结论 Cur-DL能够明显增强姜黄素的胃肠道稳定性和口服吸收。更多还原

【Abstract】 Objective Preparation of deoxycholic acid modified liposomes to further improve the gastrointestinal stability and oral absorption of curcumin.Methods Curcumin liposomes（Cur-L） were prepared by thin film dispersion combined with ultrasonication, followed by electrostatic adsorption of deoxycholate chitosan conjugate（DCS） on the surface of Cur-L to produce DCS-modified curcumin liposomes（Cur-DL）.In vitro release experiments were performed using dynamic dialysis, in vivo pharmacokinetics in rats and in vivo distribution using small animal imaging.Results The mean particle size of Cur-DL was（138.70±5.50） nm and the PDI was 0.14±0.02.The 2 h drug release percentages in the stomach were 30.81% and 15.03% for Cur-L and Cur-DL,respectively.And the results of in vivo pharmacokinetic experiments in rats showed that the AUC_0-∞ of Cur-DL was 5.78 times higher than that of the curcumin suspension（Cur-Sus） group and 2.18 times higher than that of the Cur-L group.The results of tissue distribution experiments at 24 h after administration showed that the mean fluorescence intensity of all organs was greater in the Cur-DL group than in the other groups, with curcumin being most distributed in the liver and kidney.Conclusion Cur-DL significantly enhances the gastrointestinal stability and oral absorption of curcumin.更多还原