微孔沸石中 5-氟尿嘧啶的控制释放。
Controlled release of 5-fluorouracil from microporous zeolites.
机构信息
Aristotle University of Thessaloniki, School of Pharmacy, Department of Pharmacology, Thessaloniki, Greece.
Department of Materials Science, University of Patras, Rio, Patras, Greece; Foundation for Research and Technology, Hellas-Institute of Chemical Engineering Sciences-FORTH/ICE-HT, Patras, Greece.
出版信息
Nanomedicine. 2014 Jan;10(1):197-205. doi: 10.1016/j.nano.2013.06.016. Epub 2013 Aug 3.
UNLABELLED
Zeolite particles with different pore diameter and particle size were loaded with the model anticancer drug 5-fluorouracil. The loaded zeolites were characterized by means of SEM, XRD, DSC, XPS, N2 physisorption and FT-IR. Higher loading of 5-FU was observed for NaX-FAU than BEA. Release studies were carried out in HCl 0.1N. Release of 5-FU from NaX-FAU showed exponential-type behaviour with the drug fully released within 10 min. In the case of BEA, the kinetics of 5-FU shows a multi-step profile with prolonged release over time. Molecular dynamics simulations showed that diffusion of the drug molecule through the BEA framework is lower than for NaX-FAU due to increased van der Waals interaction between the drug and the framework. The effect of zeolitic particles on the viability of Caco-2 monolayers showed that the NaX-FAU particles cause a reduction of cell viability in a more pronounced way compared with the BEA particles.
FROM THE CLINICAL EDITOR
This article describes zeolite-based nanoparticles in generating time-controlled release of 5-FU from zeolite preparations for anti-cancer therapy.
未加标签
用不同孔径和粒径的沸石颗粒负载模型抗癌药物 5-氟尿嘧啶。通过 SEM、XRD、DSC、XPS、N2 物理吸附和 FT-IR 对负载沸石进行了表征。与 BEA 相比，NaX-FAU 的 5-FU 负载量更高。在 0.1N HCl 中进行了释放研究。NaX-FAU 中 5-FU 的释放呈指数型行为，药物在 10 分钟内完全释放。对于 BEA，5-FU 的动力学呈现多步轮廓，随着时间的延长释放时间延长。分子动力学模拟表明，由于药物与骨架之间的范德华相互作用增加，药物分子通过 BEA 骨架的扩散低于 NaX-FAU。沸石颗粒对 Caco-2 单层细胞活力的影响表明，与 BEA 颗粒相比，NaX-FAU 颗粒更明显地降低细胞活力。
临床编辑
本文描述了基于沸石的纳米颗粒如何在沸石制剂中产生时间控制的 5-FU 释放，用于抗癌治疗。
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