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

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• 作者：Xingwang Zhang (24) (25)
  Jianping Qi (24)
  Yi Lu (24)
  Xiongwei Hu (24)
  Wei He (24)
  Wei Wu (24)
  
  24. School of Pharmacy ; Key Laboratory of Smart Drug Delivery ; Fudan University ; ; Ministry of Education and PLA ; Shanghai ; 201203 ; People鈥檚 Republic of China
  25. Division of Pharmaceutics ; College of Pharmacy ; Jinan University ; Guangzhou ; 510632 ; People鈥檚 Republic of China
  
• 关键词：Insulin ; Biotin ; Liposomes ; Hypoglycemic effect ; Oral ; Ligand ; mediated ; Endocytosis ; Cytotoxicity
• 刊名：Nanoscale Research Letters
• 出版年：2014
• 出版时间：December 2014
• 年：2014
• 卷：9
• 期：1
• 全文大小：1,089 KB
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• 刊物主题：Nanotechnology; Nanotechnology and Microengineering; Nanoscale Science and Technology; Nanochemistry; Molecular Medicine;
• 出版者：Springer US
• ISSN：1556-276X

文摘

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.