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用于药物递送的新型溶胶-凝胶有机-无机杂化材料

Novel sol-gel organic-inorganic hybrid materials for drug delivery.

作者信息

Catauro Michelina, Verardi Duilio, Melisi Daniela, Belotti Federico, Mustarelli Piercarlo

机构信息

Department of Mechanical and Aerospace Engineering, Second University of Naples, Aversa, Italy.

出版信息

J Appl Biomater Biomech. 2010 Jan-Apr;8(1):42-51.

Abstract

PURPOSE

The aim of the present study was to synthetize and characterize novel sol-gel organic-inorganic hybrid materials to be used for controlled drug delivery application.

MATERIALS AND METHODS

Organic-inorganic hybrid class I materials based on poly(epsilon-caprolactone) (PCL 6, 12, 24 and 50 wt%) and zirconia-yttria (ZrO2-5%Y2O3) were synthesized by a sol-gel method, from a multicomponent solution containing zirconium propoxide [Zr(OC2H7)4], yttrium chloride (YCl3), PCL, water and chloroform (CHCl3). The structure of the hybrids was obtained by means of hydrogen bonds between the Zr-OH group (H-donor) in the sol-gel intermediate species and the carboxylic group (H-acceptor) in the repeating units of the polymer.

RESULTS

The presence of hydrogen bonds between organic-inorganic components of the hybrid materials was suggested by Fourier transform infrared (FTIR) analysis, and strongly supported by solid-state NMR. A single-step, sol-gel process was then used to precipitate microspheres containing ketoprofen or indomethacin for controlled drug delivery applications. Release kinetics in a simulated body fluid (SBF) were subsequently investigated. The amount of drug released was detected by UV-VIS spectroscopy. Pure anti-inflammatory agents exhibited linear release with time, in contrast drugs entrapped in the organic-inorganic hybrids were released with a logarithmic time dependence, starting with an initial burst effect followed by a gradual decrease.

CONCLUSIONS

The synthesis of amorphous materials containing drugs, obtained by sol-gel methods, helps to devise new strategies for controlled drug delivery system design.

摘要

目的

本研究的目的是合成并表征用于控释药物应用的新型溶胶 - 凝胶有机 - 无机杂化材料。

材料与方法

基于聚(ε - 己内酯)(PCL,含量分别为6%、12%、24%和50%重量)和氧化锆 - 氧化钇(ZrO₂ - 5%Y₂O₃)的I类有机 - 无机杂化材料通过溶胶 - 凝胶法合成,原料为包含丙醇锆[Zr(OC₂H₇)₄]、氯化钇(YCl₃)、PCL、水和氯仿(CHCl₃)的多组分溶液。杂化材料的结构是通过溶胶 - 凝胶中间物种中的Zr - OH基团(氢供体)与聚合物重复单元中的羧基(氢受体)之间的氢键形成的。

结果

傅里叶变换红外(FTIR)分析表明杂化材料的有机 - 无机成分之间存在氢键,固态核磁共振(NMR)提供了有力支持。然后采用单步溶胶 - 凝胶工艺沉淀含酮洛芬或吲哚美辛的微球用于控释药物应用。随后研究了在模拟体液(SBF)中的释放动力学。通过紫外 - 可见光谱法检测药物释放量。纯抗炎剂表现出随时间的线性释放,相比之下,包裹在有机 - 无机杂化材料中的药物释放呈现对数时间依赖性,开始时有初始突释效应,随后逐渐减少。

结论

通过溶胶 - 凝胶法合成含药物的无定形材料有助于设计控释药物递送系统的新策略。

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