期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 587, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2020.119682
关键词
Liposomes; Doxorubicin; In vivo fate; Oral delivery; Fluorescence resonance energy transfer
资金
- National Natural Science Foundation of China [81872826]
- Science and Technology Commission of Shanghai Municipality [18ZR1404100]
- Shanghai Pujiang Program [18PJD001]
- school of pharmacy and Pudong hospital in Fudan University [RHJJ2017-06]
Liposomes have been broadly used in pharmaceutical field to overcome oral absorption barriers, such as gastric acid, tenacious mucus or intestinal epithelia. However, the concrete in vivo absorption mechanisms of liposomes are still indistinct. This study aims to visually elucidate the effect of particle size and surface characteristics on in vivo translocation of oral liposomes by fluorescence resonance energy transfer (FRET) effect. We fabricated liposomes of various sizes (100 nm, 200 nm and 500 nm) and surface characteristics (anionic, cationic and PEGylated) which are also labeled with FRET probes for discriminating the intact liposomes. We then investigated the in vivo fate of those different liposomes upon oral administration. Results showed that smaller conventional liposomes, cationic and PEGylated liposomes had longer retention time in digestive tract. Few intact liposomes were taken up by intestinal epithelial cells and none were found in circulation. In vivo pharmacokinetics revealed that the smaller, cationic or PEGylated liposomes had higher relative bioavailability. Similar retention time of various liposomes in blood circulation to control solution indicated that liposomes improved oral drug absorption by either prolonging contact time with gastrointestinal tract or increasing penetration ability through mucus barrier, instead of being absorbed integrally into circulation. This study offered new insight into developing highly effective liposomes for oral delivery.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据