Nanocomplexes of an insulinotropic drug: optimization, microparticle formation, and antidiabetic activity in rats

Enas Elmowafy, Rihab Osman, Abdel Hameed El-Shamy,&dagger; Gehanne AS AwadDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt&dagger;Abdel Hameed El-Shamy passed away on August 25, 2013Abstract: The aim of the present work was to test...

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Autores principales:	Elmowafy E, Osman R, El-Shamy AH, Awad GAS
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/84d21960c278436cb2a35685b5d73443
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spelling	oai:doaj.org-article:84d21960c278436cb2a35685b5d734432021-12-02T06:31:49ZNanocomplexes of an insulinotropic drug: optimization, microparticle formation, and antidiabetic activity in rats1178-2013https://doaj.org/article/84d21960c278436cb2a35685b5d734432014-09-01T00:00:00Zhttp://www.dovepress.com/nanocomplexes-of-an-insulinotropic-drug-optimization-microparticle-for-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013 Enas Elmowafy, Rihab Osman, Abdel Hameed El-Shamy,&dagger; Gehanne AS AwadDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt&dagger;Abdel Hameed El-Shamy passed away on August 25, 2013Abstract: 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.Keywords: nanocomplexes, microparticles, spray drying, nasal delivery, antidiabetic effectElmowafy EOsman REl-Shamy AHAwad GASDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 4449-4465 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Elmowafy E Osman R El-Shamy AH Awad GAS Nanocomplexes of an insulinotropic drug: optimization, microparticle formation, and antidiabetic activity in rats
description	Enas Elmowafy, Rihab Osman, Abdel Hameed El-Shamy,&dagger; Gehanne AS AwadDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt&dagger;Abdel Hameed El-Shamy passed away on August 25, 2013Abstract: 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.Keywords: nanocomplexes, microparticles, spray drying, nasal delivery, antidiabetic effect
format	article
author	Elmowafy E Osman R El-Shamy AH Awad GAS
author_facet	Elmowafy E Osman R El-Shamy AH Awad GAS
author_sort	Elmowafy E
title	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_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_sort	nanocomplexes of an insulinotropic drug: optimization, microparticle formation, and antidiabetic activity in rats
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/84d21960c278436cb2a35685b5d73443
work_keys_str_mv	AT elmowafye nanocomplexesofaninsulinotropicdrugoptimizationmicroparticleformationandantidiabeticactivityinrats AT osmanr nanocomplexesofaninsulinotropicdrugoptimizationmicroparticleformationandantidiabeticactivityinrats AT elshamyah nanocomplexesofaninsulinotropicdrugoptimizationmicroparticleformationandantidiabeticactivityinrats AT awadgas nanocomplexesofaninsulinotropicdrugoptimizationmicroparticleformationandantidiabeticactivityinrats
_version_	1718399881698082816

Nanocomplexes of an insulinotropic drug: optimization, microparticle formation, and antidiabetic activity in rats

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