Pharmacokinetic Study and Optimal Formulation of New Anti-Parkinson Natural Compound Schisantherin A

Our recent studies showed that schisantherin A (StA) is a promising candidate for PD treatment, but the pharmacokinetic profile of StA is largely unknown. The effects of different formulations on the pharmacokinetics and bioavailability of StA were investigated by HPLC equipped with a vacuum degasse...

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Main Authors: Fei Sa, Bao Jian Guo, Sai Li, Zai Jun Zhang, Hok Man Chan, Ying Zheng, Simon Ming Yuen Lee
Format: Article
Language:English
Published: Hindawi Limited 2015-01-01
Series:Parkinson's Disease
Online Access:http://dx.doi.org/10.1155/2015/951361
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spelling doaj-459ab3a265c54cf1841f73a2ed5d9f632020-11-24T22:49:50ZengHindawi LimitedParkinson's Disease2090-80832042-00802015-01-01201510.1155/2015/951361951361Pharmacokinetic Study and Optimal Formulation of New Anti-Parkinson Natural Compound Schisantherin AFei Sa0Bao Jian Guo1Sai Li2Zai Jun Zhang3Hok Man Chan4Ying Zheng5Simon Ming Yuen Lee6State Key Laboratory of Quality Research of Chinese Medicine and Institute of Chinese Medical Sciences, University of Macau, Taipa, MacauInstitute of New Drug Research, Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine & New Drug Research, College of Pharmacy, Jinan University, Guangdong, ChinaInstitute of New Drug Research, Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine & New Drug Research, College of Pharmacy, Jinan University, Guangdong, ChinaState Key Laboratory of Quality Research of Chinese Medicine and Institute of Chinese Medical Sciences, University of Macau, Taipa, MacauState Key Laboratory of Quality Research of Chinese Medicine and Institute of Chinese Medical Sciences, University of Macau, Taipa, MacauState Key Laboratory of Quality Research of Chinese Medicine and Institute of Chinese Medical Sciences, University of Macau, Taipa, MacauState Key Laboratory of Quality Research of Chinese Medicine and Institute of Chinese Medical Sciences, University of Macau, Taipa, MacauOur recent studies showed that schisantherin A (StA) is a promising candidate for PD treatment, but the pharmacokinetic profile of StA is largely unknown. The effects of different formulations on the pharmacokinetics and bioavailability of StA were investigated by HPLC equipped with a vacuum degasser, a quaternary pump, a manual sampler, and an ultraviolet detector. The absolute bioavailability of StA in nanoemulsion formulation was significantly increased from 4.3% to 47.3%. To the best of our knowledge, this is the first report of absolute bioavailability for StA in rats and successful increase of bioavailability of StA by nanoemulsion formulation. The pharmacokinetic profiles of StA could be significantly improved by a safe nanoemulsion formulation. This study provides a successful example of advanced delivery system for improving the bioavailability of potential central nervous system (CNS) drug candidate with poor solubility. This novel approach could be an effective alternative solution to overcome the shortcomings of conventional poor drug delivery of CNS drugs. The results of present study not only indicate that StA has potential to be developed as a promising oral therapeutic agent for the management of PD but also shed light on novel way to improve bioavailability of PD drugs.http://dx.doi.org/10.1155/2015/951361
collection DOAJ
language English
format Article
sources DOAJ
author Fei Sa
Bao Jian Guo
Sai Li
Zai Jun Zhang
Hok Man Chan
Ying Zheng
Simon Ming Yuen Lee
spellingShingle Fei Sa
Bao Jian Guo
Sai Li
Zai Jun Zhang
Hok Man Chan
Ying Zheng
Simon Ming Yuen Lee
Pharmacokinetic Study and Optimal Formulation of New Anti-Parkinson Natural Compound Schisantherin A
Parkinson's Disease
author_facet Fei Sa
Bao Jian Guo
Sai Li
Zai Jun Zhang
Hok Man Chan
Ying Zheng
Simon Ming Yuen Lee
author_sort Fei Sa
title Pharmacokinetic Study and Optimal Formulation of New Anti-Parkinson Natural Compound Schisantherin A
title_short Pharmacokinetic Study and Optimal Formulation of New Anti-Parkinson Natural Compound Schisantherin A
title_full Pharmacokinetic Study and Optimal Formulation of New Anti-Parkinson Natural Compound Schisantherin A
title_fullStr Pharmacokinetic Study and Optimal Formulation of New Anti-Parkinson Natural Compound Schisantherin A
title_full_unstemmed Pharmacokinetic Study and Optimal Formulation of New Anti-Parkinson Natural Compound Schisantherin A
title_sort pharmacokinetic study and optimal formulation of new anti-parkinson natural compound schisantherin a
publisher Hindawi Limited
series Parkinson's Disease
issn 2090-8083
2042-0080
publishDate 2015-01-01
description Our recent studies showed that schisantherin A (StA) is a promising candidate for PD treatment, but the pharmacokinetic profile of StA is largely unknown. The effects of different formulations on the pharmacokinetics and bioavailability of StA were investigated by HPLC equipped with a vacuum degasser, a quaternary pump, a manual sampler, and an ultraviolet detector. The absolute bioavailability of StA in nanoemulsion formulation was significantly increased from 4.3% to 47.3%. To the best of our knowledge, this is the first report of absolute bioavailability for StA in rats and successful increase of bioavailability of StA by nanoemulsion formulation. The pharmacokinetic profiles of StA could be significantly improved by a safe nanoemulsion formulation. This study provides a successful example of advanced delivery system for improving the bioavailability of potential central nervous system (CNS) drug candidate with poor solubility. This novel approach could be an effective alternative solution to overcome the shortcomings of conventional poor drug delivery of CNS drugs. The results of present study not only indicate that StA has potential to be developed as a promising oral therapeutic agent for the management of PD but also shed light on novel way to improve bioavailability of PD drugs.
url http://dx.doi.org/10.1155/2015/951361
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