Hydrophobic ion pairing of an insulin-sodium deoxycholate complex for oral delivery of insulin

Shaoping Sun1&ndash;3, Na Liang2, Yoshiaki Kawashima3, Dengning Xia2, Fude Cui21School of Chemistry and Material Science, Heilongjiang University, Harbin, 2School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China; 3School of Pharmaceutical Science, Aichi Gakuin University, Nis...

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Autores principales:	Sun S, Liang N, Kawashima Y, Xia D, Cui F
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2011
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/d41b3d584b2849598aa7da8ec663261a
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spelling	oai:doaj.org-article:d41b3d584b2849598aa7da8ec663261a2021-12-02T00:02:39ZHydrophobic ion pairing of an insulin-sodium deoxycholate complex for oral delivery of insulin1176-91141178-2013https://doaj.org/article/d41b3d584b2849598aa7da8ec663261a2011-11-01T00:00:00Zhttp://www.dovepress.com/hydrophobic-ion-pairing-of-an-insulin-sodium-deoxycholate-complex-for--a8748https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Shaoping Sun1&ndash;3, Na Liang2, Yoshiaki Kawashima3, Dengning Xia2, Fude Cui21School of Chemistry and Material Science, Heilongjiang University, Harbin, 2School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China; 3School of Pharmaceutical Science, Aichi Gakuin University, Nissin, JapanAbstract: Insulin was complexed with sodium deoxycholate to form an insulin-sodium deoxycholate complex (Ins-SD-Comp) using an hydrophobic ion pairing method in aqueous phase to enhance the liposolubility of insulin. In order to obtain the maximal complexation efficiency, the molar ratio of sodium deoxycholate to insulin was found. The zeta potential method was used to confirm the optimal ratio for formation of Ins-SD-Comp. The structural characteristics of Ins-SD-Comp were assessed using the Fourier transform infrared method. The apparent partition coefficient of insulin increased upon the formation of Ins-SD-Comp. Based on the preliminary study, Ins-SD-Comp was encapsulated into poly(lactide-co-glycolide) (PLGA) nanoparticles using an emulsion solvent diffusion method. The maximal encapsulation efficiency of Ins-SD-Comp into PLGA nanoparticles was 93.6% &plusmn; 2.81%, drug loading was about 4.8% &plusmn; 0.32%, and the mean diameter of the nanoparticles was 278 &plusmn; 13 nm. Biological activity and in vivo results revealed that the bioactivity of insulin was not destroyed during the preparation process. Ins-SD-Comp-loaded PLGA nanoparticles have the potential to reduce serum glucose levels and increase the oral bioavailability of insulin.Keywords: insulin complex, sodium deoxycholate, nanoparticles, zeta potential, oral bioavailabilitySun SLiang NKawashima YXia DCui FDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2011, Iss default, Pp 3049-3056 (2011)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Sun S Liang N Kawashima Y Xia D Cui F Hydrophobic ion pairing of an insulin-sodium deoxycholate complex for oral delivery of insulin
description	Shaoping Sun1&ndash;3, Na Liang2, Yoshiaki Kawashima3, Dengning Xia2, Fude Cui21School of Chemistry and Material Science, Heilongjiang University, Harbin, 2School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China; 3School of Pharmaceutical Science, Aichi Gakuin University, Nissin, JapanAbstract: Insulin was complexed with sodium deoxycholate to form an insulin-sodium deoxycholate complex (Ins-SD-Comp) using an hydrophobic ion pairing method in aqueous phase to enhance the liposolubility of insulin. In order to obtain the maximal complexation efficiency, the molar ratio of sodium deoxycholate to insulin was found. The zeta potential method was used to confirm the optimal ratio for formation of Ins-SD-Comp. The structural characteristics of Ins-SD-Comp were assessed using the Fourier transform infrared method. The apparent partition coefficient of insulin increased upon the formation of Ins-SD-Comp. Based on the preliminary study, Ins-SD-Comp was encapsulated into poly(lactide-co-glycolide) (PLGA) nanoparticles using an emulsion solvent diffusion method. The maximal encapsulation efficiency of Ins-SD-Comp into PLGA nanoparticles was 93.6% &plusmn; 2.81%, drug loading was about 4.8% &plusmn; 0.32%, and the mean diameter of the nanoparticles was 278 &plusmn; 13 nm. Biological activity and in vivo results revealed that the bioactivity of insulin was not destroyed during the preparation process. Ins-SD-Comp-loaded PLGA nanoparticles have the potential to reduce serum glucose levels and increase the oral bioavailability of insulin.Keywords: insulin complex, sodium deoxycholate, nanoparticles, zeta potential, oral bioavailability
format	article
author	Sun S Liang N Kawashima Y Xia D Cui F
author_facet	Sun S Liang N Kawashima Y Xia D Cui F
author_sort	Sun S
title	Hydrophobic ion pairing of an insulin-sodium deoxycholate complex for oral delivery of insulin
title_short	Hydrophobic ion pairing of an insulin-sodium deoxycholate complex for oral delivery of insulin
title_full	Hydrophobic ion pairing of an insulin-sodium deoxycholate complex for oral delivery of insulin
title_fullStr	Hydrophobic ion pairing of an insulin-sodium deoxycholate complex for oral delivery of insulin
title_full_unstemmed	Hydrophobic ion pairing of an insulin-sodium deoxycholate complex for oral delivery of insulin
title_sort	hydrophobic ion pairing of an insulin-sodium deoxycholate complex for oral delivery of insulin
publisher	Dove Medical Press
publishDate	2011
url	https://doaj.org/article/d41b3d584b2849598aa7da8ec663261a
work_keys_str_mv	AT suns hydrophobicionpairingofaninsulinsodiumdeoxycholatecomplexfororaldeliveryofinsulin AT liangn hydrophobicionpairingofaninsulinsodiumdeoxycholatecomplexfororaldeliveryofinsulin AT kawashimay hydrophobicionpairingofaninsulinsodiumdeoxycholatecomplexfororaldeliveryofinsulin AT xiad hydrophobicionpairingofaninsulinsodiumdeoxycholatecomplexfororaldeliveryofinsulin AT cuif hydrophobicionpairingofaninsulinsodiumdeoxycholatecomplexfororaldeliveryofinsulin
_version_	1718404014857519104

Hydrophobic ion pairing of an insulin-sodium deoxycholate complex for oral delivery of insulin

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