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Multifunctional Composite Microcapsules for Oral Delivery of Insulin
In this study, we designed and developed a new drug delivery system of multifunctional composite microcapsules for oral administration of insulin. Firstly, in order to enhance the encapsulation efficiency, insulin was complexed with functional sodium deoxycholate to form insulin-sodium deoxycholate...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2016
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5297689/ https://www.ncbi.nlm.nih.gov/pubmed/28036045 http://dx.doi.org/10.3390/ijms18010054 |
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author | Sun, Shaoping Liang, Na Gong, Xianfeng An, Weiwei Kawashima, Yoshiaki Cui, Fude Yan, Pengfei |
author_facet | Sun, Shaoping Liang, Na Gong, Xianfeng An, Weiwei Kawashima, Yoshiaki Cui, Fude Yan, Pengfei |
author_sort | Sun, Shaoping |
collection | PubMed |
description | In this study, we designed and developed a new drug delivery system of multifunctional composite microcapsules for oral administration of insulin. Firstly, in order to enhance the encapsulation efficiency, insulin was complexed with functional sodium deoxycholate to form insulin-sodium deoxycholate complex using hydrophobic ion pairing method. Then the complex was encapsulated into poly(lactide-co-glycolide) (PLGA) nanoparticles by emulsion solvent diffusion method. The PLGA nanoparticles have a mean size of 168 nm and a zeta potential of −29.2 mV. The encapsulation efficiency was increased to 94.2% for the complex. In order to deliver insulin to specific gastrointestinal regions and reduce the burst release of insulin from PLGA nanoparticles, hence enhancing the bioavailability of insulin, enteric targeting multifunctional composite microcapsules were further prepared by encapsulating PLGA nanoparticles into pH-sensitive hydroxypropyl methyl cellulose phthalate (HP55) using organic spray-drying method. A pH-dependent insulin release profile was observed for this drug delivery system in vitro. All these strategies help to enhance the encapsulation efficiency, control the drug release, and protect insulin from degradation. In diabetic fasted rats, administration of the composite microcapsules produced a great enhancement in the relative bioavailability, which illustrated that this formulation was an effective candidate for oral insulin delivery. |
format | Online Article Text |
id | pubmed-5297689 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-52976892017-02-10 Multifunctional Composite Microcapsules for Oral Delivery of Insulin Sun, Shaoping Liang, Na Gong, Xianfeng An, Weiwei Kawashima, Yoshiaki Cui, Fude Yan, Pengfei Int J Mol Sci Article In this study, we designed and developed a new drug delivery system of multifunctional composite microcapsules for oral administration of insulin. Firstly, in order to enhance the encapsulation efficiency, insulin was complexed with functional sodium deoxycholate to form insulin-sodium deoxycholate complex using hydrophobic ion pairing method. Then the complex was encapsulated into poly(lactide-co-glycolide) (PLGA) nanoparticles by emulsion solvent diffusion method. The PLGA nanoparticles have a mean size of 168 nm and a zeta potential of −29.2 mV. The encapsulation efficiency was increased to 94.2% for the complex. In order to deliver insulin to specific gastrointestinal regions and reduce the burst release of insulin from PLGA nanoparticles, hence enhancing the bioavailability of insulin, enteric targeting multifunctional composite microcapsules were further prepared by encapsulating PLGA nanoparticles into pH-sensitive hydroxypropyl methyl cellulose phthalate (HP55) using organic spray-drying method. A pH-dependent insulin release profile was observed for this drug delivery system in vitro. All these strategies help to enhance the encapsulation efficiency, control the drug release, and protect insulin from degradation. In diabetic fasted rats, administration of the composite microcapsules produced a great enhancement in the relative bioavailability, which illustrated that this formulation was an effective candidate for oral insulin delivery. MDPI 2016-12-28 /pmc/articles/PMC5297689/ /pubmed/28036045 http://dx.doi.org/10.3390/ijms18010054 Text en © 2016 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Sun, Shaoping Liang, Na Gong, Xianfeng An, Weiwei Kawashima, Yoshiaki Cui, Fude Yan, Pengfei Multifunctional Composite Microcapsules for Oral Delivery of Insulin |
title | Multifunctional Composite Microcapsules for Oral Delivery of Insulin |
title_full | Multifunctional Composite Microcapsules for Oral Delivery of Insulin |
title_fullStr | Multifunctional Composite Microcapsules for Oral Delivery of Insulin |
title_full_unstemmed | Multifunctional Composite Microcapsules for Oral Delivery of Insulin |
title_short | Multifunctional Composite Microcapsules for Oral Delivery of Insulin |
title_sort | multifunctional composite microcapsules for oral delivery of insulin |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5297689/ https://www.ncbi.nlm.nih.gov/pubmed/28036045 http://dx.doi.org/10.3390/ijms18010054 |
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