Folate-chitosan nanoparticles triggered insulin cellular uptake and improved in vivo hypoglycemic activity

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Date

2019

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Volume Title

Type

Article

Publisher

Elsevier B.V.

Series Info

International Journal of Pharmaceutics
571

Abstract

The aim of this study was to prove a prolonged control of glucose levels, in rats, by the oral use of insulin folate-chitosan nanoparticles (FA-CS NPs). It was possible to prepare positively charged NPs with an average particle size of 288 � 5.11 nm and >80% entrapment efficiency. The system was able to enhance the stability of insulin in presence of GIT enzymes, with less than 10% release at pH 1.2 and an 8 hr released amount of 38.92 � 4.52% in PBS pH 7.4. A 5 fold enhancement in insulin intestinal permeability and cellular uptake over insulin solution was proven. The cellular uptake pathways was found to occur by several mechanisms. Besides, cell compatibility and absence of histopathological alterations was also demonstrated. Finally, a controlled blood glucose level for 8 h in rats. These results anticipated FA-CS NPs as a promising oral insulin candidate. � 2019 Elsevier B.V.

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Keywords

Cellular uptake, Chitosan, Controlled blood glucose, Folic acid, Insulin, Oral delivery, antidiabetic agent, chitosan nanoparticle, folate chitosan nanoparticle, folic acid, glucose, insulin, unclassified drug, animal experiment, animal model, antidiabetic activity, Article, Caco-2 cell line, cell viability, controlled study, cytotoxicity, enzymatic degradation, glucose blood level, histopathology, human, human cell, in vivo study, insulin blood level, insulin release, internalization, intestine mucosa permeability, male, mean residence time, nonhuman, particle size, pH, priority journal, rat, zeta potential

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