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Enhanced hypoglycemic effect of biotin-modified liposomes loading insulin: effect of formulation variables, intracellular trafficking, and cytotoxicity

Xingwang Zhang12, Jianping Qi1*, Yi Lu1, Xiongwei Hu1, Wei He1 and Wei Wu1

Author Affiliations

1 School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery, Ministry of Education and PLA, Shanghai 201203, People's Republic of China

2 Division of Pharmaceutics, College of Pharmacy, Jinan University, Guangzhou 510632, People's Republic of China

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Nanoscale Research Letters 2014, 9:185  doi:10.1186/1556-276X-9-185

Published: 16 April 2014


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.

Insulin; Biotin; Liposomes; Hypoglycemic effect; Oral; Ligand-mediated; Endocytosis; Cytotoxicity