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Silymarin-laden PVP-PEG polymeric composite for enhanced aqueous solubility and dissolution rate: Preparation and in vitro characterization

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Journal of Pharmaceutical Analysis 2019年第1期9卷 34-39页

作者： Abid Mehmood Yousaf Usman Rashid Malik yasser shahzad Tariq Mahmood Talib Hussain Department of Pharmacy COMSATS University IslamabadLahore Campus Faculty of Pharmacy University of Central Punjab

The aim of this work was to develop, optimize and characterize a silymarin-laden polyvinylpyrrolidone(PVP)-polyethylene glycol(PEG) polymeric composite to resolve low aqueous solubility and dissolution rate problem of the drug. A number of silymarin-laden polymeric formulations were fabricated with different quantities of PVP K-30 and PEG 6000 by the solvent-evaporation method. The effect of PVP K-30 and PEG 6000 on the aqueous solubility and dissolution rate was investigated. The optimized formulation and its constituents were characterized using powder X-ray diffraction(PXRD), differential scanning calorimetry(DSC), scanning electron microscopy(SEM) and Fourier transform infrared spectroscopy(FTIR) techniques. Both the PEG 6000 and PVP K-30 positively affected the aqueous solubility and dissolution rate of the drug. In particular, a formulation consisting of silymarin, PVP K-30 and PEG 6000(0.25/1.5/1.5, w/w/w) furnished the highest solubility(24.3972.95 mg/mL) and an excellent dissolution profile( $100% in 40 min). The solubility enhancement with this formulation was $ 1150-fold as compared to plain silymarin powder. Moreover, all the constituents existed in the amorphous state in this silymarin-laden PVP-PEG polymeric composite. Accordingly, this formulation might be a promising tool to administer silymarin with an enhanced effect via the oral route.

关键词： Silymarin Hydrophilic polymers Inclusion Solid dispersion Aqueous solubility Dissolution rate

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

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Chinese Science Bulletin 2012年第14期57卷 1685-1692页

作者： shahzad yasser SHAH Syed Nisar Hussain ANSARI Muhammad Tayyab RIAZ Romana SAFDAR Aasma HUSSAIN Talib MALIK Madeeha Faculty of Pharmacy Bahauddin Zakariya University Division of Pharmacy and Pharmaceutical Sciences School of Applied SciencesUniversity of Huddersfield Hamdard Institute of Pharmaceutical Sciences Hamdard University

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 LD>SD>PM.

关键词：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

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