Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailability

To improve the stability and oral bioavailability of Z-ligustilide (LIG), the inclusion complex of LIG with hydroxypropyl- β-cyclodextrin (HP-β-CD) was prepared by the kneading method and characterized by UV-Vis spectroscopy, differential thermal analysis (DTA) and Fourier transform infrared (FTIR)...

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Main Authors: Lu Yapeng, Liu Siyuan, Zhao Yu, Zhu Li, Yu Shuqin
Format: Article
Language:English
Published: Sciendo 2014-06-01
Series:Acta Pharmaceutica
Subjects:
Online Access:http://www.degruyter.com/view/j/acph.2014.64.issue-2/acph-2014-0012/acph-2014-0012.xml?format=INT
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author Lu Yapeng
Liu Siyuan
Zhao Yu
Zhu Li
Yu Shuqin
author_facet Lu Yapeng
Liu Siyuan
Zhao Yu
Zhu Li
Yu Shuqin
author_sort Lu Yapeng
collection DOAJ
description To improve the stability and oral bioavailability of Z-ligustilide (LIG), the inclusion complex of LIG with hydroxypropyl- β-cyclodextrin (HP-β-CD) was prepared by the kneading method and characterized by UV-Vis spectroscopy, differential thermal analysis (DTA) and Fourier transform infrared (FTIR) spectroscopy. LIG is capable of forming an inclusion complex with HP-b-CD and the stoichiometry of the complex was 1:1. Stability of the inclusion complex against temperature and light was greatly enhanced compared to that of free LIG. Further, oral bioavailability of LIG and the inclusion complex in rats were studied and the plasma drug concentration-time curves fitted well with the non-compartment model to estimate the absolute bioavailability, which was 7.5 and 35.9 %, respectively. In conclusion, these results show that LIG/HP-β-CD complexation can be of great use for increasing the stability and biological efficacy of LIG
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spelling doaj.art-32a9d5ee84d84303bca9ae3fee5333b42022-12-21T18:19:20ZengSciendoActa Pharmaceutica1330-00751846-95582014-06-0164221122210.2478/acph-2014-0012acph-2014-0012Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailabilityLu Yapeng0Liu Siyuan1Zhao Yu2Zhu Li3Yu Shuqin4Institute of Nautical Medicine, Nantong University, Nantong 226001, ChinaSchool of Life Sciences, Nantong University, Nantong 226007, ChinaInstitute of Nautical Medicine, Nantong University, Nantong 226001, ChinaInstitute of Nautical Medicine, Nantong University, Nantong 226001, ChinaJiangsu Key Laboratory for Supramolecular Medicinal Materials and Applications College of Life Sciences, Nanjing Normal University, Nanjing 210046, ChinaTo improve the stability and oral bioavailability of Z-ligustilide (LIG), the inclusion complex of LIG with hydroxypropyl- β-cyclodextrin (HP-β-CD) was prepared by the kneading method and characterized by UV-Vis spectroscopy, differential thermal analysis (DTA) and Fourier transform infrared (FTIR) spectroscopy. LIG is capable of forming an inclusion complex with HP-b-CD and the stoichiometry of the complex was 1:1. Stability of the inclusion complex against temperature and light was greatly enhanced compared to that of free LIG. Further, oral bioavailability of LIG and the inclusion complex in rats were studied and the plasma drug concentration-time curves fitted well with the non-compartment model to estimate the absolute bioavailability, which was 7.5 and 35.9 %, respectively. In conclusion, these results show that LIG/HP-β-CD complexation can be of great use for increasing the stability and biological efficacy of LIGhttp://www.degruyter.com/view/j/acph.2014.64.issue-2/acph-2014-0012/acph-2014-0012.xml?format=INTZ-ligustilidehydroxypropyl-β-cyclodextrininclusion complexstabilitybioavailability
spellingShingle Lu Yapeng
Liu Siyuan
Zhao Yu
Zhu Li
Yu Shuqin
Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailability
Acta Pharmaceutica
Z-ligustilide
hydroxypropyl-β-cyclodextrin
inclusion complex
stability
bioavailability
title Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailability
title_full Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailability
title_fullStr Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailability
title_full_unstemmed Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailability
title_short Complexation of Z-ligustilide with hydroxypropyl-β-cyclodextrin to improve stability and oral bioavailability
title_sort complexation of z ligustilide with hydroxypropyl β cyclodextrin to improve stability and oral bioavailability
topic Z-ligustilide
hydroxypropyl-β-cyclodextrin
inclusion complex
stability
bioavailability
url http://www.degruyter.com/view/j/acph.2014.64.issue-2/acph-2014-0012/acph-2014-0012.xml?format=INT
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AT zhaoyu complexationofzligustilidewithhydroxypropylbcyclodextrintoimprovestabilityandoralbioavailability
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