同时包载人参3种成分的透明质酸修饰的纳米脂质载体的制备及表征

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。

Preparation and characterization of nanostructured lipid carrier modified by hyaluronic acid loaded with three components in Ginseng Radix

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.