Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: characterization, lyophilization and in-vivo evaluation

Jahanzeb Mudassir1,2, Yusrida Darwis,1 Suriani Muhamad,1 Arshad Ali Khan1,31Discipline of Pharmaceutical Technology, School of Pharmaceutical Sciences, Universiti Sains, Malaysia, 11800, Penang Malaysia; 2Department of Pharmaceutics, Faculty of Pharmacy, Bahanuddin Zakariya, Multan, Pakistan; 3Facul...

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Autores principales:	Mudassir J, Darwis Y, Muhamad S, Khan AA
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	acrylic monomers peptides self assembly lyophilization hypoglycemic effect polymeric nanogels Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/45170065504c4022aea2b8f595474e3a
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spelling	oai:doaj.org-article:45170065504c4022aea2b8f595474e3a2021-12-02T01:05:05ZSelf-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: characterization, lyophilization and in-vivo evaluation1178-2013https://doaj.org/article/45170065504c4022aea2b8f595474e3a2019-07-01T00:00:00Zhttps://www.dovepress.com/self-assembled-insulin-and-nanogels-polyelectrolyte-complex-insngs-pec-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Jahanzeb Mudassir1,2, Yusrida Darwis,1 Suriani Muhamad,1 Arshad Ali Khan1,31Discipline of Pharmaceutical Technology, School of Pharmaceutical Sciences, Universiti Sains, Malaysia, 11800, Penang Malaysia; 2Department of Pharmaceutics, Faculty of Pharmacy, Bahanuddin Zakariya, Multan, Pakistan; 3Faculty of Engineering Technology, Universiti Malaysia Pahang, Kuantan, Pahang, MalaysiaIntroduction: Insulin is given by injection, because when administered orally, it would be destroyed by enzymes in the digestive system, hence only about 0.1% reaches blood circulation. The purpose of the present study was to use pH sensitive polyelectrolyte methyl methacrylate (MMA)/itaconic acid (IA) nanogels as carriers in an attempt to improve absorption of insulin administered orally.Methods: Insulin (Ins) was incorporated into the MMA/IA nanogels (NGs) using the polyelectrolyte complexation (PEC) method to form Ins/NGs-PEC. Several parameters, including Ins:NGs ratio, pH, incubation time and stirring rate were optimized during preparation of InsNGs-PEC. The prepared formulations were characterized in terms of particle size (PS), polydispersity index (PdI), zeta potential (ZP) and percent entrapment efficiency (% EE).Results: The optimized InF12 nanogels had a PS, PdI, ZP and %EE of 190.43 nm, 0.186, −16.70 mV and 85.20%, respectively. The InF12 nanogels were lyophilized in the presence of different concentrations of trehalose as cryoprotectant. The lyophilized InF12 containing 2%w/v trahalose (InF12-Tre2 nanogels) was chosen as final formulation which had a PS, PdI, ZP and %EE of 430.50 nm, 0.588, −16.50 mv and 82.10, respectively. The in vitro release of insulin from InF12-Tre2 nanogels in the SGF and SIF were 28.71% and 96.53%, respectively. The stability study conducted at 5±3°C for 3 months showed that lnF12-Tre2 nanogels were stable. The SDS-PAGE assay indicated that the primary structure of insulin in the lnF12-Tre2 nanogels was intact. The in-vivo study in the diabetic rats following oral administration of InF12-Tre2 nanogels at a dose of 100 IU/kg body weight reduced blood glucose level significantly to 51.10% after 6 hours compared to the control groups.Conclusions: The pH sensitive MMA/IA nanogels are potential carriers for oral delivery of insulin as they enhanced the absorption of the drug.Keywords: acrylic monomers, peptides self assembly, lyophilization, hypoglycemic effect, polymeric nanogelsMudassir JDarwis YMuhamad SKhan AADove Medical Pressarticleacrylic monomerspeptides self assemblylyophilizationhypoglycemic effectpolymeric nanogelsMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 4895-4909 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	acrylic monomers peptides self assembly lyophilization hypoglycemic effect polymeric nanogels Medicine (General) R5-920
spellingShingle	acrylic monomers peptides self assembly lyophilization hypoglycemic effect polymeric nanogels Medicine (General) R5-920 Mudassir J Darwis Y Muhamad S Khan AA Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: characterization, lyophilization and in-vivo evaluation
description	Jahanzeb Mudassir1,2, Yusrida Darwis,1 Suriani Muhamad,1 Arshad Ali Khan1,31Discipline of Pharmaceutical Technology, School of Pharmaceutical Sciences, Universiti Sains, Malaysia, 11800, Penang Malaysia; 2Department of Pharmaceutics, Faculty of Pharmacy, Bahanuddin Zakariya, Multan, Pakistan; 3Faculty of Engineering Technology, Universiti Malaysia Pahang, Kuantan, Pahang, MalaysiaIntroduction: Insulin is given by injection, because when administered orally, it would be destroyed by enzymes in the digestive system, hence only about 0.1% reaches blood circulation. The purpose of the present study was to use pH sensitive polyelectrolyte methyl methacrylate (MMA)/itaconic acid (IA) nanogels as carriers in an attempt to improve absorption of insulin administered orally.Methods: Insulin (Ins) was incorporated into the MMA/IA nanogels (NGs) using the polyelectrolyte complexation (PEC) method to form Ins/NGs-PEC. Several parameters, including Ins:NGs ratio, pH, incubation time and stirring rate were optimized during preparation of InsNGs-PEC. The prepared formulations were characterized in terms of particle size (PS), polydispersity index (PdI), zeta potential (ZP) and percent entrapment efficiency (% EE).Results: The optimized InF12 nanogels had a PS, PdI, ZP and %EE of 190.43 nm, 0.186, −16.70 mV and 85.20%, respectively. The InF12 nanogels were lyophilized in the presence of different concentrations of trehalose as cryoprotectant. The lyophilized InF12 containing 2%w/v trahalose (InF12-Tre2 nanogels) was chosen as final formulation which had a PS, PdI, ZP and %EE of 430.50 nm, 0.588, −16.50 mv and 82.10, respectively. The in vitro release of insulin from InF12-Tre2 nanogels in the SGF and SIF were 28.71% and 96.53%, respectively. The stability study conducted at 5±3°C for 3 months showed that lnF12-Tre2 nanogels were stable. The SDS-PAGE assay indicated that the primary structure of insulin in the lnF12-Tre2 nanogels was intact. The in-vivo study in the diabetic rats following oral administration of InF12-Tre2 nanogels at a dose of 100 IU/kg body weight reduced blood glucose level significantly to 51.10% after 6 hours compared to the control groups.Conclusions: The pH sensitive MMA/IA nanogels are potential carriers for oral delivery of insulin as they enhanced the absorption of the drug.Keywords: acrylic monomers, peptides self assembly, lyophilization, hypoglycemic effect, polymeric nanogels
format	article
author	Mudassir J Darwis Y Muhamad S Khan AA
author_facet	Mudassir J Darwis Y Muhamad S Khan AA
author_sort	Mudassir J
title	Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: characterization, lyophilization and in-vivo evaluation
title_short	Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: characterization, lyophilization and in-vivo evaluation
title_full	Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: characterization, lyophilization and in-vivo evaluation
title_fullStr	Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: characterization, lyophilization and in-vivo evaluation
title_full_unstemmed	Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: characterization, lyophilization and in-vivo evaluation
title_sort	self-assembled insulin and nanogels polyelectrolyte complex (ins/ngs-pec) for oral insulin delivery: characterization, lyophilization and in-vivo evaluation
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/45170065504c4022aea2b8f595474e3a
work_keys_str_mv	AT mudassirj selfassembledinsulinandnanogelspolyelectrolytecomplexinsngspecfororalinsulindeliverycharacterizationlyophilizationandinvivoevaluation AT darwisy selfassembledinsulinandnanogelspolyelectrolytecomplexinsngspecfororalinsulindeliverycharacterizationlyophilizationandinvivoevaluation AT muhamads selfassembledinsulinandnanogelspolyelectrolytecomplexinsngspecfororalinsulindeliverycharacterizationlyophilizationandinvivoevaluation AT khanaa selfassembledinsulinandnanogelspolyelectrolytecomplexinsngspecfororalinsulindeliverycharacterizationlyophilizationandinvivoevaluation
_version_	1718403311355297792

Self-assembled insulin and nanogels polyelectrolyte complex (Ins/NGs-PEC) for oral insulin delivery: characterization, lyophilization and in-vivo evaluation

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