异补骨脂素纳米结构脂质载体的体外溶出及其抗白癜风活性研究  

In vitro dissolution and anti-vitiligo activity of isopsoralen nanostructured lipid carriers

作　　者：庞建云[1,2] 沈成英[1] 周敏[1] 申宝德[1,3] 刘肖 刘娟[1,2] 许润春[2] 袁海龙[1] PANG Jian-yun;SHEN Cheng-ying;ZHOU Min;SHEN Bao-de;LIU Xiao;LIU Juan;XU Rtm- chun;YUAN Hai-long(Department of Pharmacy, Air Force General Hospital, PLA, Beijing 100142, China;College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China;Key Laboratory of Modern Preparation of Traditional Chinese Medicine, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China)

机构地区：[1]中国人民解放军空军总医院药学部,北京100142 [2]成都中医药大学药学院,四川成都611137 [3]江西中医药大学现代中药制剂教育部重点实验室,江西南昌330004

出　　处：《中草药》2018年第8期1796-1801,共6页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(81573696);全军重大科研计划(BKJ16J025;BKJ16J011)

摘　　要：目的评价异补骨脂素纳米结构脂质载体(IPRN-NLC)的体外溶出行为,并考察其对小鼠黑色素瘤B16F10细胞增殖、黑色素合成及酪氨酸酶活性的影响。方法采用透析袋法测定IPRN-NLC在72 h内的累积溶出量并绘制溶出曲线,MTT法测定B16F10细胞增殖情况,多巴氧化法测定酪氨酸酶活性,GENMED细胞黑色素含量比色法测定黑色素合成。结果在72 h时体外累积溶出量IPRN-NLC为67.31%,IPRN-物理混合物为90.30%,IPRN-DMSO为98.67%,IPRN-混悬液为53.34%。IPRN在一定质量浓度范围内可以促进B16F10细胞增殖,提高酪氨酸酶活性,增加黑色素的合成,且同质量浓度的IPRN-NLC对B16F10的作用显著高于IPRN溶液(P<0.05)。结论 IPRN-NLC不仅具有缓释作用,还可以增加药物的溶解度;在一定质量浓度范围内与细胞具有较好的生物相容性,能显著提高细胞酪氨酸酶活性,促进黑色素合成。Objective To evaluate the in vitro dissolution characteristic of IPRN-NLC and to study its effects on B16 F10 cells proliferation, melanin synthesis, and tyrosinase activity. Methods The dynamic dialysis was employed to compare the in vitrodissolution of IPRN and IPRN-NLC; MTT assay was used to detect the proliferation of B16 F10; The tyrosinase activity was determined by L-DOPA-oxidation; The melain content was determined by GENMED Cell Melanin Quantitative Assay Kit. Results The accumulation dissolution of IPRN-NLC was 67.31% within 72 h, which showed sustained release; While the dissolution of IPRN-suspension, IPRN-physical mixture, and IPRN-DMSO were 53.34%, 90.30%, and 98.67%, respectively. The IPRN-NLC could significantly promote the proliferation, tyrosinase activity and melanin content compared with IPRN DMSO groups（P 0.05） at the same concentration. Conclusion IPRN-NLC could increase the solubility of the drug with sustained release, and showed good cell biology intermiscibility, which could significantly increase the effects on B16 F10 cells.

关 键 词：异补骨脂素 纳米结构脂质载体 体外释放 黑色素瘤B16F10细胞 白癜风 酪氨酸酶 细胞增殖 黑色素 MTT法 多巴氧化法 

分 类 号：R283.6[医药卫生—中药学]