Biotinylated liposomes as potential carriers for the oral delivery of insulin

Abstract This study aimed to explore biotinylated liposomes (BLPs) as novel carriers to enhance the oral delivery of insulin. Biotinylation was achieved by incorporating biotin-conjugated phospholipids into the liposome membranes. A significant hypoglycemic effect and enhanced absorption were observ...

Full description

Saved in:
Bibliographic Details
Published in:Nanomedicine 2014, Vol.10 (1), p.167-176
Main Authors: Zhang, Xingwang, PhD, Qi, Jianping, PhD, Lu, Yi, PhD, He, Wei, PhD, Li, Xiaoyang, MSc, Wu, Wei, PhD
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Biotin
Blood Glucose
Diabetes Mellitus - drug therapy
Diabetes Mellitus - pathology
Diabetes Mellitus, Experimental - drug therapy
Drug Carriers
Drug Delivery Systems
Humans
Insulin
Insulin - administration & dosage
Insulin - chemistry
Internal Medicine
Liposomes
Liposomes - administration & dosage
Liposomes - chemistry
Oral delivery
Rats
Receptor-mediated endocytosis
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Abstract This study aimed to explore biotinylated liposomes (BLPs) as novel carriers to enhance the oral delivery of insulin. Biotinylation was achieved by incorporating biotin-conjugated phospholipids into the liposome membranes. A significant hypoglycemic effect and enhanced absorption were observed after treating diabetic rats with the BLPs with a relative bioavailability of 12.09% and 8.23%, based on the measurement of the pharmacologic effect and the blood insulin level, respectively; this achieved bioavailability was approximately double that of conventional liposomes. The significance of the biotinylation was confirmed by the facilitated absorption of the BLPs through receptor-mediated endocytosis, as well as by the improved physical stability of the liposomes. Increased cellular uptake and quick gastrointestinal transport further verified the ability of the BLPs to enhance absorption. These results provide a proof of concept that BLPs can be used as potential carriers for the oral delivery of insulin. From the Clinical Editor Diabetes remains a major source of mortality in the Western world, and advances in its management are expected to have substantial socioeconomic impact. In this paper, biotinylated liposomes were utilized as carriers of insulin for local delivery, demonstrating the feasibility of this approach in a rat model.
ISSN:1549-9634
1549-9642
DOI:10.1016/j.nano.2013.07.011