载龙胆苦苷和齐墩果酸的红细胞载药体系的肝靶向性评价  

Evaluation of erythrocyte drug delivery system containing gentiopicroside and oleanolic acid of liver targeting

作　　者：冯宇飞[1] 秦国昭 FENG Yu-fei;QIN Guo-zhao(College of Pharmacy,Heilongjiang University of Chinese Medicine,Harbin 150040,China)

机构地区：[1]黑龙江中医药大学药学院,黑龙江哈尔滨150040

出　　处：《时珍国医国药》2020年第11期2617-2619,共3页Lishizhen Medicine and Materia Medica Research

基　　金：国家自然科学基金青年基金(81703944);黑龙江省自然科学基金优秀青年项目(YQ2019H031);黑龙江中医药大学博士创新基金项目(2017bs10);黑龙江中医药大学“优秀创新人才支持计划”项目(2018年)。

摘　　要：目的评价载龙胆苦苷和齐墩果酸红细胞载药体系的肝靶向效应。方法利用改良低渗预膨胀法制备载龙胆苦苷和齐墩果酸红细胞载药体系,采用HPLC法测定龙胆苦苷和齐墩果酸的包载率,并对其细胞形态及体内分布情况进行评估。结果从血液中收集的红细胞的形态与正常红细胞相比,装载药物并重封后,部分红细胞被破坏,形态发生明显变化,得到载药红细胞中齐墩果酸包封率为(67.95±7.46)%,龙胆苦苷包封率为(28.26±4.23)%,总包封率为48.11%。对所制备的载龙胆苦苷和齐墩果酸红细胞载药体系进行体内分布研究,结果表明,4h后药物在肝脏富集量最大。与齐墩果酸生理盐水组相比,载药红细胞的肝脏靶向指数(DTI)在0.5h时是前者的1.63倍,而给药后1h内对肝脏外其他脏器及血液的大部分DTI小于1,与龙胆苦苷生理盐水组相比,载药红细胞的肝脏靶向指数(DTI)在0.5h时是前者的3.17倍。结论制成载药红细胞后,提高了齐墩果酸和龙胆苦苷在肝组织中的分布,更好地起到肝靶向的作用。为其它中药多成分新给药系统的开发应用提供实践参考。Objective To evaluate the function of gentianin and oleanolic red blood cell drug delivery system. Methods The modified hypotonic pre-expansion method was used to prepare borneol and oleanolic red blood cell drug-loading system. The drug loading and entrapment rate of gentiopicroside and oleanolic acid were determined by HPLC and the cells were used. Morphology, drug loading and tissue distribution were assessed. Results The morphology of red blood cells collected from the blood were concave and spherical which is the same as in the literature. and the morphology did not change significantly after loading the drug and resealing. The encapsulation efficiency of oleanolic acid in drug-loaded red blood cells was(67.95±7.46) %, the encapsulation efficiency of gentiopicroside was(28.26±4.23) %, and the total encapsulation efficiency was 48.11%. The results of targeted studies on the prepared gentamicin and oleanolic red blood cell drug delivery system showed that the liver targeting index(DTI) of drug-loaded red blood cells was 0.5 compared with the oleanolic acid saline group 0.5 h is 1.63 times of the former, and most DTIs of other organs and blood outside the liver are less than 1 within 1 h after administration, and the liver targeting index of drug-loaded red blood cells(DTI) compared with the gentiopicroside physiological saline group 0.5 h is 3.17 times the former at 0.5 h. Conclusion The above experiments show that the distribution of oleanolic acid and gentiopicroside in liver tissue is improved after liver drug-loading, and it plays a better role in liver targeting. Provide practical reference for the development and application of other traditional Chinese medicine multi-component new drug delivery systems.

关 键 词：红细胞载体 龙胆苦苷 齐墩果酸 肝靶向 

分 类 号：R962[医药卫生—药理学]