Effects of drug-polymer dispersions on solubility and in vitro diffusion of artemisinin across a polydimethylsiloxane membrane

作     者：SHAHZAD Yasser SHAH Syed Nisar Hussain ANSARI Muhammad Tayyab RIAZ Romana SAFDAR Aasma HUSSAIN Talib MALIK Madeeha 

作者机构：Faculty of PharmacyBahauddin Zakariya University Division of Pharmacy and Pharmaceutical SciencesSchool of Applied SciencesUniversity of Huddersfield Hamdard Institute of Pharmaceutical SciencesHamdard University 

出 版 物：《Chinese Science Bulletin》 (Chinese Science Bulletin)

年 卷 期：2012年第57卷第14期

页      面：1685-1692页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 10[医学] 

基　　金：Bahauddin Zakariya University and the Higher Education Comission Pakistan for providing funding (628) to conduct this research 

主　　题：聚合物分散体 溶解度测定 聚硅氧烷 外扩散 青蒿素 药物 傅里叶变换红外光谱 水性高分子 

摘      要：Artemisinin(ART) is a sesquiterpene lactone with an endo-peroxide bridge that is thought to be responsible for its antimalarial *** has low oral bioavailability because of aqueous insolubility,which leads to local toxicity at the site of *** present work focused on increasing its solubility and evaluating its permeation across a model membrane to mimic transdermal delivery that bypasses the hepatic *** this purpose,physical mixtures(PM),solid dispersions(SD) and lyophilized dispersions(LD) with different drug-polymer ratios(1:0.5,1:1,1:2,1:4 and 1:9) were prepared using the hydrophilic polymer polyvinylpyrrolidone(PVP).Drug-polymer dispersions were characterized using X-ray diffraction(XRD) and Fourier transform infrared spectroscopy(FTIR).Solubility was measured in three solvents:de-ionized water,phosphate buffered saline(PBS) and *** toluene-water partition coefficient was evaluated and compared with the literature and calculated logP *** vitro diffusion of ART was studied across a polydimethylsiloxane membrane from a saturated solution of drug-polymer *** patterns showed a gradual decrease in crystallinity of ART with increasing polymer concentration,while FTIR confirmed no interactions between ART and *** was increased up to 4-,5-and 8-fold for LD in water,PBS and methanol,*** logP for toluene-water was 2.65 ± 0.3,which is in good agreement with literature and calculated logP *** was enhanced,which is attributed to the decrease in crystallinity and increase in wettability of the *** ART flux was significantly higher than that of pure ART(0.12 ± 0.01) with increasing PVP concentration for SD and LD *** conclusion,drug-polymer dispersions with PVP improve the pharmaceutical properties of ART in the order LDSDPM.