药物纳米晶的制备及其口服转运机制研究进展  

Research Progress in the Preparation and Oral Transport Mechanism of Drug Nanocrystals

作　　者：吴帅聪 秦超[1] 韩晓鹏 尹莉芳[1] WU Shuaicong;QIN Chao;HAN Xiaopeng;YIN Lifang(School of Pharmacy,China Pharmaceutical University,Nanjing 211198,China)

机构地区：[1]中国药科大学药学院,江苏南京211198

出　　处：《药学进展》2023年第4期303-311,共9页Progress in Pharmaceutical Sciences

基　　金：“重大新药创制”科技重大专项(No.2017zx09101001-004)。

摘　　要：现阶段提高难溶性药物口服生物利用度是药剂学研究的热点内容,其中药物纳米晶化凭借较高的载药量、较高的口服生物利用度以及易于工业化生产等优点受到广泛关注。药物纳米晶是指采用粉碎法(Top-down法)或纳米沉淀法(Bottom-up法)制备的除稳定剂外无其他药用载体的纳米级微粒。通常认为药物纳米晶口服给药后通过内吞作用吸收入血或通过M细胞介导转运至肠系膜淋巴循环,但目前尚未透彻研究药物纳米晶跨肠道上皮细胞的转运机制。综述系统介绍了纳米晶的定义、制备方法、相关的体外细胞培养模型(Caco-2,MDCK,Caco-2/HT29-MTX,Caco-2/HT29-MTX/Raji-B)以及影响纳米晶跨膜转运的因素,并通过体外细胞培养模型从分子水平上深入分析药物纳米晶跨膜转运机制。Currently,improving the oral bioavailability of poorly soluble drugs is a hot topic in pharmaceutics,with particularly wide attention to nanocrystallization due to its high drug loading,high oral bioavailability and easy industrial production.Drug nanocrystal refers to nanoscale particles prepared by pulverization(Top-down method)or nanoprecipitation(Bottom-up method)with no other pharmaceutical carriers except stabilizer.It is generally believed that nanocrystals are absorbed into blood through endocytosis or transported to the mesenteric lymphatic circulation mediated by M cells after oral administration,but the trans-epithelial mechanism of nanocrystals has not been thoroughly explored.This article systematically introduces the definition of nanocrystals,their preparation methods,some in-vitro cell culture models(Caco-2,MDCK,Caco-2/HT29-MTX,Caco-2/HT29-MTX/Raji-B)and influential factors for the trans-epithelial mechanism of nanocrystals,and analyzes the trans-epithelial mechanism of nanocrystals at molecular level through in-vitro cell culture models.

关 键 词：药物纳米晶 口服吸收 转运机制 细胞培养模型 

分 类 号：R944[医药卫生—药剂学]