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.
Highlights
With the advent of biotech epoch, more and more proteins and peptides become available for clinical treatment, such as growth hormone [1], calcitonin [2], and octreotide [3]
Our previous report has proved that biotin-modified liposomes (BLPs) have ability to improve the oral delivery of insulin, and studied the uptake and transport mechanisms in the gastrointestinal tract [30]
Preparation and characterization of BLPs Formulation variables influence the physicochemical properties of insulin-loaded liposomes such as entrapment efficiency and particle size [32,33]
Summary
With the advent of biotech epoch, more and more proteins and peptides become available for clinical treatment, such as growth hormone [1], calcitonin [2], and octreotide [3]. Problems encountered with insulin injection vitalize the demands to develop alternative delivery systems. To achieve effective oral delivery of insulin, several barriers like instability, gastrointestinal enzymatic degradation, and poor membrane permeability, etc., should. Biotin plays an important role in maintaining the homeostasis of blood glucose [24]. Improved cellular permeability and higher hypoglycemic effect after oral administration of biotinconjugated glucagon-like peptide-1 has been observed [25]. Biotin-modified vehicles have been investigated for nonparenteral delivery of active ingredients [26,27,28,29]. Our previous report has proved that biotin-modified liposomes (BLPs) have ability to improve the oral delivery of insulin, and studied the uptake and transport mechanisms in the gastrointestinal tract [30]. Particular enhanced absorption mechanisms and cytotoxicity of BLPs are not clear enough
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