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Preparation, Administration, and Assessment of In Vivo Tissue-Specific Cellular Uptake of Fluorescent Dye-Labeled Liposomes
Published on: July 30, 2020
Enhanced hypoglycemic effect of biotin-modified liposomes loading insulin: effect of formulation variables,
Xingwang Zhang1, Jianping Qi2, Yi Lu2
1School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery, Ministry of Education and PLA, Shanghai 201203, People's Republic of China ; Division of Pharmaceutics, College of Pharmacy, Jinan University, Guangzhou 510632, People's Republic of China.
Abstract:
Peroral protein/peptide delivery has been one of the most challenging, but encouraging topics in pharmaceutics. This article was intended to explore the potential of biotin-modified liposomes (BLPs) as oral insulin delivery carriers. By incorporating biotin-DSPE into the lipid bilayer, we prepared BLPs using reverse evaporation/sonication method. We investigated hypoglycemic effects in normal rats after oral administration of BLPs, and the possible absorption mechanism by a series of in vitro tests. The relative pharmacological bioavailability of BLPs was up to 11.04% that was as much as 5.28 folds of conventional liposomes (CLPs). The results showed that the enhanced oral absorption of insulin mainly attributed to biotin ligand-mediated endocytosis. The results provided proof of BLPs as effective carriers for oral insulin delivery.
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