Cargando…

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Sun, Shaoping, Liang, Na, Gong, Xianfeng, An, Weiwei, Kawashima, Yoshiaki, Cui, Fude, Yan, Pengfei
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
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
_version_ 1782505760978108416
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
work_keys_str_mv AT sunshaoping multifunctionalcompositemicrocapsulesfororaldeliveryofinsulin
AT liangna multifunctionalcompositemicrocapsulesfororaldeliveryofinsulin
AT gongxianfeng multifunctionalcompositemicrocapsulesfororaldeliveryofinsulin
AT anweiwei multifunctionalcompositemicrocapsulesfororaldeliveryofinsulin
AT kawashimayoshiaki multifunctionalcompositemicrocapsulesfororaldeliveryofinsulin
AT cuifude multifunctionalcompositemicrocapsulesfororaldeliveryofinsulin
AT yanpengfei multifunctionalcompositemicrocapsulesfororaldeliveryofinsulin