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Pharmacokinetic study of niosome-loaded insulin in diabetic rats

BACKGROUND AND THE PURPOSE OF THE STUDY: Encapsulation of human insulin in lipid vesicular systems such as niosomes was sought as a route to protect this protein against proteolytic enzymes and to improve its oral bioavailability. The purpose of this study was to assess the effect of insulin encapsu...

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Autores principales: Pardakhty, A., Moazeni, E., Varshosaz, J., Hajhashemi, V., Rouholamini Najafabadi, A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Tehran University of Medical Sciences 2011
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3436076/
https://www.ncbi.nlm.nih.gov/pubmed/23008685
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author Pardakhty, A.
Moazeni, E.
Varshosaz, J.
Hajhashemi, V.
Rouholamini Najafabadi, A.
author_facet Pardakhty, A.
Moazeni, E.
Varshosaz, J.
Hajhashemi, V.
Rouholamini Najafabadi, A.
author_sort Pardakhty, A.
collection PubMed
description BACKGROUND AND THE PURPOSE OF THE STUDY: Encapsulation of human insulin in lipid vesicular systems such as niosomes was sought as a route to protect this protein against proteolytic enzymes and to improve its oral bioavailability. The purpose of this study was to assess the effect of insulin encapsulation in niosomes on oral bioavailability in diabetic rats. METHODS: Recombinant human insulin was entrapped in multilamellar niosomes composed of polyoxyethylene alkyl ether surfactants (Brij 52 and Brij 92) or sorbitan monostearate (Span 60) and cholesterol. The amount of insulin released in simulated intestinal fluid (SIF) and simulated gastric fluid (SGF) were measured at 37°C. The protection of entrapped insulin against pepsin, α-chymotrypsin and trypsin were evaluated in comparison with free insulin solution. Diabetes was induced by IP injection of streptozotocin (65 mg/kg) in male wistar rats and effects of orally administered niosomes and subcutaneously injected insulin on hypoglycemia and elevation of insulin levels in serum were compared. RESULTS AND CONCLUSION: The extent and rate of insulin release from Brij 92 and Span 60 vesicles were lower than that of Brij 52 niosomes (P<0.05). Vesicles protected insulin in comparison with free insulin solution against proteolytic enzymes (P<0.05) significantly. Animals treated with oral niosome-encapsulated insulin (100 IU/kg) showed decreased levels of blood glucose and elevated serum insulin, which in the case of Brij 92 niosomes, hypoglycemic effect was significant (P<0.05). Niosomes were also stable in solubilizing bile salt solutions and could effectively prolong the release of insulin in both SGF and SIF. Results of this study showed that niosomes may be utilized as oral carriers of insulin; however, to increase bioavailability of insulin, further studies on the protease inhibitor co-encapsulation in niosomal formulations might be helpful.
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spelling pubmed-34360762012-09-24 Pharmacokinetic study of niosome-loaded insulin in diabetic rats Pardakhty, A. Moazeni, E. Varshosaz, J. Hajhashemi, V. Rouholamini Najafabadi, A. Daru Original Article BACKGROUND AND THE PURPOSE OF THE STUDY: Encapsulation of human insulin in lipid vesicular systems such as niosomes was sought as a route to protect this protein against proteolytic enzymes and to improve its oral bioavailability. The purpose of this study was to assess the effect of insulin encapsulation in niosomes on oral bioavailability in diabetic rats. METHODS: Recombinant human insulin was entrapped in multilamellar niosomes composed of polyoxyethylene alkyl ether surfactants (Brij 52 and Brij 92) or sorbitan monostearate (Span 60) and cholesterol. The amount of insulin released in simulated intestinal fluid (SIF) and simulated gastric fluid (SGF) were measured at 37°C. The protection of entrapped insulin against pepsin, α-chymotrypsin and trypsin were evaluated in comparison with free insulin solution. Diabetes was induced by IP injection of streptozotocin (65 mg/kg) in male wistar rats and effects of orally administered niosomes and subcutaneously injected insulin on hypoglycemia and elevation of insulin levels in serum were compared. RESULTS AND CONCLUSION: The extent and rate of insulin release from Brij 92 and Span 60 vesicles were lower than that of Brij 52 niosomes (P<0.05). Vesicles protected insulin in comparison with free insulin solution against proteolytic enzymes (P<0.05) significantly. Animals treated with oral niosome-encapsulated insulin (100 IU/kg) showed decreased levels of blood glucose and elevated serum insulin, which in the case of Brij 92 niosomes, hypoglycemic effect was significant (P<0.05). Niosomes were also stable in solubilizing bile salt solutions and could effectively prolong the release of insulin in both SGF and SIF. Results of this study showed that niosomes may be utilized as oral carriers of insulin; however, to increase bioavailability of insulin, further studies on the protease inhibitor co-encapsulation in niosomal formulations might be helpful. Tehran University of Medical Sciences 2011 /pmc/articles/PMC3436076/ /pubmed/23008685 Text en © 2011 Tehran University of Medical Sciences http://creativecommons.org/licenses/by-nc/3.0/ This work is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported License which allows users to read, copy, distribute and make derivative works for non-commercial purposes from the material, as long as the author of the original work is cited properly.
spellingShingle Original Article
Pardakhty, A.
Moazeni, E.
Varshosaz, J.
Hajhashemi, V.
Rouholamini Najafabadi, A.
Pharmacokinetic study of niosome-loaded insulin in diabetic rats
title Pharmacokinetic study of niosome-loaded insulin in diabetic rats
title_full Pharmacokinetic study of niosome-loaded insulin in diabetic rats
title_fullStr Pharmacokinetic study of niosome-loaded insulin in diabetic rats
title_full_unstemmed Pharmacokinetic study of niosome-loaded insulin in diabetic rats
title_short Pharmacokinetic study of niosome-loaded insulin in diabetic rats
title_sort pharmacokinetic study of niosome-loaded insulin in diabetic rats
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3436076/
https://www.ncbi.nlm.nih.gov/pubmed/23008685
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