[关键词]
[摘要]
目的 制备包载人参3种成分的透明质酸(hyaluronic acid,HA)修饰的纳米脂质载体(HA-OUR-NLC),并对其进行表征。方法 采用纳米脂质体(nanostructured lipid,NLC)包载人参中3种难溶性有效成分齐墩果酸(oleanolic acid,OA)、熊果酸(ursolic acid,UA)、人参皂苷Rg3(ginsenoside Rg3,Rg3)制备纳米脂质载体(OUR-NLC);然后采用HA作为靶向因子,经电荷吸附作用进行修饰。采用动态透析法进行释放度实验。通过流式细胞仪及MTT法考察HA-OUR-NLC对SMMC-7721细胞的细胞摄取及细胞毒性情况。结果 采用溶剂超声分散法制备的OUR-NLC外观呈现淡蓝色乳光。并通过电荷吸附法成功制备了HA-OUR-NLC。其形态圆整,分布均匀。体外释放表明其具有一定的缓释作用。摄取实验表明HA-OUR-NLC能被SMMC-7721细胞所摄取。MTT实验结果表明,HA-OUR-NLC对SMMC-7721细胞增殖具有抑制作用。结论 采用溶剂超声分散法制备的HA-OUR-NLC具有较好的理化性质和稳定性,且具备一定的缓释长效作用。
[Key word]
[Abstract]
Objective To prepare and characterize tri-components nanostructure lipid carrier of Ginseng Radix modified with hyaluronic acid (HA-OUR-NLC). Methods Nanostructured lipid carriers (NLC) was used to wrap mount three difficult soluble active ingredients in Ginseng Radix including oleanolic acid (OA), ursolic acid (UA), and ginsenoside Rg3. Then using hyaluronic acid (HA) as the target factor, NLC was modified by charge-adsorption. The dynamic dialysis method was used to test the release. The cellular uptake and cytotoxicity of HA-OUR-NLC on SMMC-7721 cells were investigated by flow cytometry instrument and MTT assay respectively. Results OUR-NLC was prepared by ultrasonic dispersion of solvent using NLC as carrier material and CTAB as emulsifier, and its appearance was light blue opalescence. Then HA-OUR-NLC was successfully prepared by charge-sorption method with round shape and uniform distribution. In vitro release showed that it had a sustained release effect. Cell uptake experiments showed that HA-OUR-NLC can be taken up by SMMC-7721 cells. MTT assay results showed that HA-OUR-NLC had inhibitory effect on SMMC-7721 cell proliferation. Conclusion HA-OUR-NLC prepared by solvent ultrasonic dispersion not only has good physical and chemical properties, but also has a certain sustained release effect.
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[基金项目]
黑龙江省自然科学基金项目(H2016060);国家自然科学基金面上项目(81373929);黑龙江中医药大学科研基金项目(201408)