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Nanocomplexes of an insulinotropic drug: optimization, microparticle formation, and antidiabetic activity in rats
The aim of the present work was to test the ability of two non-diabetogenic carbohydrates to intranasally deliver the insulinotropic drug repaglinide (REP) for controlling blood glucose level. REP was loaded onto chitosan/alginate nanocomplexes (NCs) suitable for mucosal delivery and uptake. Improve...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Dove Medical Press
2014
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4173756/ https://www.ncbi.nlm.nih.gov/pubmed/25258534 http://dx.doi.org/10.2147/IJN.S66876 |
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author | Elmowafy, Enas Osman, Rihab El-Shamy, Abdel Hameed Awad, Gehanne AS |
author_facet | Elmowafy, Enas Osman, Rihab El-Shamy, Abdel Hameed Awad, Gehanne AS |
author_sort | Elmowafy, Enas |
collection | PubMed |
description | The aim of the present work was to test the ability of two non-diabetogenic carbohydrates to intranasally deliver the insulinotropic drug repaglinide (REP) for controlling blood glucose level. REP was loaded onto chitosan/alginate nanocomplexes (NCs) suitable for mucosal delivery and uptake. Improved stability and delivery characteristics were obtained by spray drying the selected NCs, yielding microparticles. A statistical experimental design was adopted to investigate the effects of the formulations’ variables on two critical responses: NC size and drug entrapment efficiency. Physicochemical characterizations of the network’s structures were done, and in vitro cytotoxicity and histopathological studies were conducted. The potential of the developed system to prolong the drug effect was tested on diabetic rats. The results showed that to attain particles suitable for nasal delivery, alginate should be used at its lowest level used in this study (0.6 mg/mL). A low level of chitosan (0.5 mg/mL) was needed when the drug was cation-loaded, while the high chitosan level (1 mg/mL) was more suitable when REP was anion-loaded. The best entrapment efficiency was achieved at a theoretical drug loading of 0.025 mg/mL. Discrete NCs could be rapidly recovered from the spray-dried microparticles. The cytotoxicity and histopathological studies indicated that such formulations were well tolerated. The antihyperglycemic activity of the nasally administered formulae was gradual but was significantly sustained over 24 hours, suggesting NC mucosal uptake. Nasal delivery of such dry powders achieved better glycemic control compared with the conventional oral tablets. |
format | Online Article Text |
id | pubmed-4173756 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | Dove Medical Press |
record_format | MEDLINE/PubMed |
spelling | pubmed-41737562014-09-25 Nanocomplexes of an insulinotropic drug: optimization, microparticle formation, and antidiabetic activity in rats Elmowafy, Enas Osman, Rihab El-Shamy, Abdel Hameed Awad, Gehanne AS Int J Nanomedicine Original Research The aim of the present work was to test the ability of two non-diabetogenic carbohydrates to intranasally deliver the insulinotropic drug repaglinide (REP) for controlling blood glucose level. REP was loaded onto chitosan/alginate nanocomplexes (NCs) suitable for mucosal delivery and uptake. Improved stability and delivery characteristics were obtained by spray drying the selected NCs, yielding microparticles. A statistical experimental design was adopted to investigate the effects of the formulations’ variables on two critical responses: NC size and drug entrapment efficiency. Physicochemical characterizations of the network’s structures were done, and in vitro cytotoxicity and histopathological studies were conducted. The potential of the developed system to prolong the drug effect was tested on diabetic rats. The results showed that to attain particles suitable for nasal delivery, alginate should be used at its lowest level used in this study (0.6 mg/mL). A low level of chitosan (0.5 mg/mL) was needed when the drug was cation-loaded, while the high chitosan level (1 mg/mL) was more suitable when REP was anion-loaded. The best entrapment efficiency was achieved at a theoretical drug loading of 0.025 mg/mL. Discrete NCs could be rapidly recovered from the spray-dried microparticles. The cytotoxicity and histopathological studies indicated that such formulations were well tolerated. The antihyperglycemic activity of the nasally administered formulae was gradual but was significantly sustained over 24 hours, suggesting NC mucosal uptake. Nasal delivery of such dry powders achieved better glycemic control compared with the conventional oral tablets. Dove Medical Press 2014-09-18 /pmc/articles/PMC4173756/ /pubmed/25258534 http://dx.doi.org/10.2147/IJN.S66876 Text en © 2014 Elmowafy et al. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. |
spellingShingle | Original Research Elmowafy, Enas Osman, Rihab El-Shamy, Abdel Hameed Awad, Gehanne AS Nanocomplexes of an insulinotropic drug: optimization, microparticle formation, and antidiabetic activity in rats |
title | Nanocomplexes of an insulinotropic drug: optimization, microparticle formation, and antidiabetic activity in rats |
title_full | Nanocomplexes of an insulinotropic drug: optimization, microparticle formation, and antidiabetic activity in rats |
title_fullStr | Nanocomplexes of an insulinotropic drug: optimization, microparticle formation, and antidiabetic activity in rats |
title_full_unstemmed | Nanocomplexes of an insulinotropic drug: optimization, microparticle formation, and antidiabetic activity in rats |
title_short | Nanocomplexes of an insulinotropic drug: optimization, microparticle formation, and antidiabetic activity in rats |
title_sort | nanocomplexes of an insulinotropic drug: optimization, microparticle formation, and antidiabetic activity in rats |
topic | Original Research |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4173756/ https://www.ncbi.nlm.nih.gov/pubmed/25258534 http://dx.doi.org/10.2147/IJN.S66876 |
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