Enhanced oral bioavailability of koumine by complexation with hydroxypropyl-β-cyclodextrin: preparation, optimization, ex vivo and in vivo characterization

Koumine (KME) is an active alkaloid extracted from Gelsemium elegans, and its diverse bioactivities have been studied for decades. However, KME exhibits poor solubility and low oral bioavailability, which hampers its potential therapeutic exploitation. This work aimed to develop optimized inclusion...

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Autores principales:	Qing Hu, Xiaoling Fu, Yanping Su, Yanfang Wang, Sihuan Gao, Xiaoqin Wang, Ying Xu, Changxi Yu
Formato:	article
Lenguaje:	EN
Publicado:	Taylor & Francis Group 2021
Materias:	koumine hydroxypropyl-β-cyclodextrin inclusion complexes permeability bioavailability Therapeutics. Pharmacology RM1-950
Acceso en línea:	https://doaj.org/article/5392fe18b70e4b70993c777e3f1b2311
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spelling	oai:doaj.org-article:5392fe18b70e4b70993c777e3f1b23112021-11-17T14:21:55ZEnhanced oral bioavailability of koumine by complexation with hydroxypropyl-β-cyclodextrin: preparation, optimization, ex vivo and in vivo characterization1071-75441521-046410.1080/10717544.2021.1998248https://doaj.org/article/5392fe18b70e4b70993c777e3f1b23112021-01-01T00:00:00Zhttp://dx.doi.org/10.1080/10717544.2021.1998248https://doaj.org/toc/1071-7544https://doaj.org/toc/1521-0464Koumine (KME) is an active alkaloid extracted from Gelsemium elegans, and its diverse bioactivities have been studied for decades. However, KME exhibits poor solubility and low oral bioavailability, which hampers its potential therapeutic exploitation. This work aimed to develop optimized inclusion complexes to improve the bioavailability of KME. The KME/hydroxypropyl-β-cyclodextrin (KME/HP-β-CD) inclusion complexes were prepared by the solvent evaporation method and later optimized using the Box-Behnken design. The optimal KME/HP-β-CD was characterized by scanning electron microscopy, Fourier transforms infrared spectroscopy, differential scanning calorimetry, and nuclear magnetic resonance spectroscopy. The physicochemical characterization results revealed that the crystalline state of KME was transformed into an amorphous form, forming KME/HP-β-CD inclusion complexes. Compared with KME, the solubility and in vitro release rate of KME/HP-β-CD was significantly enhanced by 52.34- and 1.3-fold, respectively. Further research was performed to investigate the intestinal absorption characteristics and in vivo bioavailability in rats. The optimal KME/HP-β-CD showed enhanced absorptive permeability and relative bioavailability increased more than two-fold compared to that of raw KME. These results indicate that the optimal KME/HP-β-CD can be used as an effective drug carrier to improve the solubility, intestinal absorption, and bioavailability of KME.Qing HuXiaoling FuYanping SuYanfang WangSihuan GaoXiaoqin WangYing XuChangxi YuTaylor & Francis Grouparticlekouminehydroxypropyl-β-cyclodextrininclusion complexespermeabilitybioavailabilityTherapeutics. PharmacologyRM1-950ENDrug Delivery, Vol 28, Iss 1, Pp 2415-2426 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	koumine hydroxypropyl-β-cyclodextrin inclusion complexes permeability bioavailability Therapeutics. Pharmacology RM1-950
spellingShingle	koumine hydroxypropyl-β-cyclodextrin inclusion complexes permeability bioavailability Therapeutics. Pharmacology RM1-950 Qing Hu Xiaoling Fu Yanping Su Yanfang Wang Sihuan Gao Xiaoqin Wang Ying Xu Changxi Yu Enhanced oral bioavailability of koumine by complexation with hydroxypropyl-β-cyclodextrin: preparation, optimization, ex vivo and in vivo characterization
description	Koumine (KME) is an active alkaloid extracted from Gelsemium elegans, and its diverse bioactivities have been studied for decades. However, KME exhibits poor solubility and low oral bioavailability, which hampers its potential therapeutic exploitation. This work aimed to develop optimized inclusion complexes to improve the bioavailability of KME. The KME/hydroxypropyl-β-cyclodextrin (KME/HP-β-CD) inclusion complexes were prepared by the solvent evaporation method and later optimized using the Box-Behnken design. The optimal KME/HP-β-CD was characterized by scanning electron microscopy, Fourier transforms infrared spectroscopy, differential scanning calorimetry, and nuclear magnetic resonance spectroscopy. The physicochemical characterization results revealed that the crystalline state of KME was transformed into an amorphous form, forming KME/HP-β-CD inclusion complexes. Compared with KME, the solubility and in vitro release rate of KME/HP-β-CD was significantly enhanced by 52.34- and 1.3-fold, respectively. Further research was performed to investigate the intestinal absorption characteristics and in vivo bioavailability in rats. The optimal KME/HP-β-CD showed enhanced absorptive permeability and relative bioavailability increased more than two-fold compared to that of raw KME. These results indicate that the optimal KME/HP-β-CD can be used as an effective drug carrier to improve the solubility, intestinal absorption, and bioavailability of KME.
format	article
author	Qing Hu Xiaoling Fu Yanping Su Yanfang Wang Sihuan Gao Xiaoqin Wang Ying Xu Changxi Yu
author_facet	Qing Hu Xiaoling Fu Yanping Su Yanfang Wang Sihuan Gao Xiaoqin Wang Ying Xu Changxi Yu
author_sort	Qing Hu
title	Enhanced oral bioavailability of koumine by complexation with hydroxypropyl-β-cyclodextrin: preparation, optimization, ex vivo and in vivo characterization
title_short	Enhanced oral bioavailability of koumine by complexation with hydroxypropyl-β-cyclodextrin: preparation, optimization, ex vivo and in vivo characterization
title_full	Enhanced oral bioavailability of koumine by complexation with hydroxypropyl-β-cyclodextrin: preparation, optimization, ex vivo and in vivo characterization
title_fullStr	Enhanced oral bioavailability of koumine by complexation with hydroxypropyl-β-cyclodextrin: preparation, optimization, ex vivo and in vivo characterization
title_full_unstemmed	Enhanced oral bioavailability of koumine by complexation with hydroxypropyl-β-cyclodextrin: preparation, optimization, ex vivo and in vivo characterization
title_sort	enhanced oral bioavailability of koumine by complexation with hydroxypropyl-β-cyclodextrin: preparation, optimization, ex vivo and in vivo characterization
publisher	Taylor & Francis Group
publishDate	2021
url	https://doaj.org/article/5392fe18b70e4b70993c777e3f1b2311
work_keys_str_mv	AT qinghu enhancedoralbioavailabilityofkouminebycomplexationwithhydroxypropylbcyclodextrinpreparationoptimizationexvivoandinvivocharacterization AT xiaolingfu enhancedoralbioavailabilityofkouminebycomplexationwithhydroxypropylbcyclodextrinpreparationoptimizationexvivoandinvivocharacterization AT yanpingsu enhancedoralbioavailabilityofkouminebycomplexationwithhydroxypropylbcyclodextrinpreparationoptimizationexvivoandinvivocharacterization AT yanfangwang enhancedoralbioavailabilityofkouminebycomplexationwithhydroxypropylbcyclodextrinpreparationoptimizationexvivoandinvivocharacterization AT sihuangao enhancedoralbioavailabilityofkouminebycomplexationwithhydroxypropylbcyclodextrinpreparationoptimizationexvivoandinvivocharacterization AT xiaoqinwang enhancedoralbioavailabilityofkouminebycomplexationwithhydroxypropylbcyclodextrinpreparationoptimizationexvivoandinvivocharacterization AT yingxu enhancedoralbioavailabilityofkouminebycomplexationwithhydroxypropylbcyclodextrinpreparationoptimizationexvivoandinvivocharacterization AT changxiyu enhancedoralbioavailabilityofkouminebycomplexationwithhydroxypropylbcyclodextrinpreparationoptimizationexvivoandinvivocharacterization
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Enhanced oral bioavailability of koumine by complexation with hydroxypropyl-β-cyclodextrin: preparation, optimization, ex vivo and in vivo characterization

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