白藜芦醇脂质体凝胶的制备及其药效学考察  

The preparation and pharmacodynamics of resveratrol nanopreparations

作　　者：钟玮 张玉洁 时庆泽 王中彦[2] ZHONG Wei;ZHANG Yujie;SHI Qingze;WANG Zhongyan(School of Traditional Chinese Materia Medica,Shenyang Pharmaceutical University,Shenyang 110016,China;School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]沈阳药科大学中药学院,辽宁沈阳110016 [2]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2024年第8期1087-1096,共10页Journal of Shenyang Pharmaceutical University

摘　　要：目的将白藜芦醇制备成柔性脂质体后再制备为脂质体凝胶,并考察其白藜芦醇脂质体凝胶体外特性和治疗黄褐斑效果。方法将白藜芦醇制备成柔性脂质体,与凝胶结合制备成脂质体凝胶,对两种制剂进行体外释放、体外透皮、初步药效学、皮肤刺激性考察。结果制备得到的白藜芦醇脂质体凝胶粒径为(148.27±2.90)nm,PDI为0.132±0.01,属于剪切变稀的非牛顿流体。体外释放结果表明,白藜芦醇乙醇溶液释放速度相对较快,4 h时释放量为75.99%,达到释放平衡;而白藜芦醇柔性脂质体与脂质体凝胶在8 h时释放量分别为59.99%和40.30%,可显著延缓药物的释放,维持较长的释放周期。体外透皮试验结果表明,白藜芦醇柔性脂质体的透过量大于脂质体凝胶,但滞留量低于脂质体凝胶。白藜芦醇柔性脂质体与脂质体凝胶均无皮肤刺激性,且能够减少皮肤组织中紫外线照射引起的黑色素含量,与空白组相似,显著低于造模组。结论白藜芦醇纳米制剂在皮肤中都有较好的滞留,不仅可以有效治疗黄褐斑,还能增强抗氧化能力,减少局部损伤。Objective To prepare flexible liposomes and liposome gel from resveratrol,and investigate their in vitro characteristics and the therapeutic effect of melasma.Methods Resveratrol was prepared into flexible liposomes and.combined with gel to prepare liposome gel.The in vitro release,in vitro transdermal delivery,pharmacodynamics and skin irritation of the two preparations were investigated.Results The obtained resveratrol liposome gel had a particle size of(148.27±2.90) nm and a PDI of(0.132±0.01),which belong to shear thinning non-Newtonian fluid.The in vitro release results showed that the release rate of resveratrol ethanol solution was relatively fast,and the release amount reached 75.99% at 4 h,which reached the release equilibrium.The release amount of resveratrol flexible liposome and liposome gel were 59.99% and 40.30% respectively at 8 h,which could significantly delay the release of the drug and maintain a long release cycle.In vitro transdermal test results showed that the permeability of resveratrol flexible liposome was higher than that of liposome gel,but the retention was lower than that of liposome gel.Both resveratrol flexible liposome and liposome gel had no skin irritation,and could reduce the content of melanin caused by ultraviolet irradiation in skin tissue,which was similar to blank group and significantly lower than that of the modeling group.Conclusions Resveratrol nano-preparation has good retention in the skin,which can not only effectively treat melasma,but also enhance antioxidant capacity and reduce local damage.

关 键 词：白藜芦醇 脂质体 脂质体凝胶 黑色素 

分 类 号：R94[医药卫生—药剂学]