期刊
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
卷 69, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.jddst.2022.103141
关键词
Insulin; Liposomes; Vitamin B12; Oral delivery
资金
- Nanotechnology Research Center, Mashhad University of Medical Sciences (MUMS) , Mashhad, Iran [951706]
This study prepared B12-targeted PEGylated liposomal insulin to improve the stability and absorption of orally administered insulin. The results showed that B12-targeted liposomes were more stable than non-functionalized liposomes in the gastrointestinal environment and exhibited enhanced cellular uptake and insulin accumulation. This suggests that B12-targeted liposomes could be an effective formulation for oral delivery of insulin.
Orally administered Insulin have to survive the harsh gastrointestinal tract condition, penetrate the enteric epithelia barrier and bypass first pass effect before reaching the bloodstream. To address this problem, PEGylated liposomal insulin was prepared and modified with B12 to improve stability and absorption of insulin in gastro intestinal environment. Liposomes were prepared by film method plus extrusion, linked to B12 and characterized for their particle size, zeta potential, encapsulation efficiency (EE%). The release profile in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) was evaluated.& nbsp;The results indicated that B12 targeted PEGylated liposomes were more stable than non-functionalized-LipPEG in SGF and SIF. In vitro results showed significantly enhanced cellular uptake of B12 targeted PEGylated liposomes in Caco-2 cells compared to non-targeted liposomes. In the meantime, they had no toxicity on Caco-2 cells. In BALB/c mice, B12 targeted PEGylated liposomes showed higher insulin accumulation in intestine and liver. In diabetic rats B12 targeted PEGylated liposomes provided higher insulin bioavailability compared with other formulations. These findings suggest that B12-targeted liposomes could be an effective formulation for oral delivery of insulin and merits further investigations.
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