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Int J Pharm ; 571: 118708, 2019 Nov 25.
Article in English | MEDLINE | ID: mdl-31593805

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 ±â€¯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 ±â€¯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.


Subject(s)
Blood Glucose/drug effects , Drug Carriers/chemistry , Hypoglycemic Agents/administration & dosage , Insulin/administration & dosage , Nanoparticles/chemistry , Administration, Oral , Animals , Blood Glucose/analysis , Caco-2 Cells , Chitosan/chemistry , Chitosan/toxicity , Drug Carriers/toxicity , Drug Evaluation, Preclinical , Drug Stability , Folic Acid/chemistry , Folic Acid/toxicity , Humans , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/pharmacokinetics , Hypoglycemic Agents/toxicity , Insulin/chemistry , Insulin/pharmacokinetics , Male , Models, Animal , Nanoparticles/toxicity , Particle Size , Rats , Toxicity Tests
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