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纳米结构载甲硝唑HPC/氧化物干凝胶复合材料的设计:配方参数对体外表征的影响

The Design of Nanostructured Metronidazole-Loaded HPC/Oxide Xerogel Composites: Influence of the Formulation Parameters on In Vitro Characterisation.

作者信息

Czarnobaj Katarzyna

机构信息

Department of Physical Chemistry, Medical University of Gdańsk, al. Gen. J. Hallera 107, 80-416, Gdańsk, Poland.

出版信息

AAPS PharmSciTech. 2015 Oct;16(5):1160-8. doi: 10.1208/s12249-015-0310-4. Epub 2015 Feb 26.

Abstract

In this study, oxide and polymer/oxide xerogels with metronidazole were prepared and examined as carriers of drug for the local application to the bone. The nanoporous SiO2-CaO-P2O5 and HPC-SiO2-CaO-P2O5 xerogel materials with different amounts of the polymer [hydroxypropyl cellulose (HPC)] were prepared using the sol-gel technology, and their physicochemical properties were characterised with respect to chemical structure [by Fourier transform infrared spectroscopy (FTIR)], porosity and the specific surface area of solids (BET), crystallinity [by X-ray powder diffraction (XRD)], morphology [by scanning electron microscope (SEM)] and the in vitro release of the metronidazole over time (by UV-vis spectroscopy, in the ultraviolet light region). HPC-modified oxide xerogels as the carriers of drug showed slower release of metronidazole, due to the structure and stronger interactions with drug as compared with the pure oxide xerogel. Kinetic analysis indicated diffusional mechanism of drug release from all xerogel carriers. HPC addition to the oxide material resulted in a decrease in the porosity and improved the bioactive properties of xerogels. Obtained results for xerogel composites suggest that the metronidazole-loaded xerogels could be attractive candidates for local delivery systems particularly to a bone.

摘要

在本研究中,制备了含有甲硝唑的氧化物和聚合物/氧化物干凝胶,并将其作为药物载体用于局部骨应用进行研究。采用溶胶 - 凝胶技术制备了具有不同聚合物[羟丙基纤维素(HPC)]含量的纳米多孔SiO₂ - CaO - P₂O₅和HPC - SiO₂ - CaO - P₂O₅干凝胶材料,并通过傅里叶变换红外光谱(FTIR)表征其化学结构、通过BET法表征其孔隙率和固体比表面积、通过X射线粉末衍射(XRD)表征其结晶度、通过扫描电子显微镜(SEM)表征其形态以及通过紫外可见光谱(在紫外光区域)表征甲硝唑随时间的体外释放情况。作为药物载体的HPC改性氧化物干凝胶显示出甲硝唑的释放较慢,这是由于其结构以及与药物相比纯氧化物干凝胶具有更强的相互作用。动力学分析表明药物从所有干凝胶载体中释放的扩散机制。向氧化物材料中添加HPC导致孔隙率降低,并改善了干凝胶的生物活性。所得干凝胶复合材料的结果表明,负载甲硝唑的干凝胶可能是局部给药系统特别是骨局部给药系统的有吸引力的候选材料。

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