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基于介孔二氧化硅的华法林新型给药系统的开发:二氧化硅材料对抗凝剂的吸附特性

Development of novel delivery system for warfarin based on mesoporous silica: adsorption characteristics of silica materials for the anticoagulant.

作者信息

Dolinina Ekaterina S, Vorobyeva Evgeniya V, Parfenyuk Elena V

机构信息

a G.A. Krestov Institute of Solution Chemistry of Russian Academy of Sciences , Ivanovo , Russia.

出版信息

Pharm Dev Technol. 2016 Aug;21(5):546-53. doi: 10.3109/10837450.2015.1098662. Epub 2015 Oct 14.

DOI:10.3109/10837450.2015.1098662
PMID:26465269
Abstract

The adsorption of the anticoagulant warfarin onto unmodified (UMS) and modified (phenyl (PhMS), methyl (MMS), mercaptopropyl (MPMS)) mesoporous silica materials was studied at pH 1.6 and 7.4 and in the temperature range of 293-325 K. The silica materials were prepared by sol-gel method for further characterization by FTIR spectroscopy, N2 adsorption/desorption method, transmission electron microscopy and zeta potential measurements. The effects of medium pH, temperature and surface modification of mesoporous silica material on their adsorption characteristics (adsorption capacity, thermodynamic parameters of adsorption) relative to anticoagulant warfarin were investigated. It was found that medium acid-base properties strongly affect the adsorption of warfarin due to the pH-dependent structural diversity of the drug and ionization state of the silica surfaces. The adsorption capacity of the silica materials at pH 1.6 decreases in the order: MMS > MPMS > UMS > PhMS. The influence of various non-covalent interactions on the adsorption capacity of the silica materials and energy of the drug-silica interactions is discussed. These results may be useful for the development of a novel delivery system of warfarin.

摘要

在pH值为1.6和7.4以及293 - 325 K的温度范围内,研究了抗凝剂华法林在未改性(UMS)和改性(苯基(PhMS)、甲基(MMS)、巯基丙基(MPMS))介孔二氧化硅材料上的吸附情况。通过溶胶 - 凝胶法制备二氧化硅材料,以便通过傅里叶变换红外光谱(FTIR)、N₂吸附/脱附法、透射电子显微镜和zeta电位测量进行进一步表征。研究了介质pH值、温度和介孔二氧化硅材料的表面改性对其相对于抗凝剂华法林的吸附特性(吸附容量、吸附热力学参数)的影响。发现由于药物的pH依赖性结构多样性和二氧化硅表面的电离状态,介质酸碱性质强烈影响华法林的吸附。二氧化硅材料在pH 1.6时的吸附容量顺序为:MMS>MPMS>UMS>PhMS。讨论了各种非共价相互作用对二氧化硅材料吸附容量和药物 - 二氧化硅相互作用能量的影响。这些结果可能有助于开发新型华法林递送系统。

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