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介孔硅纳米粒子(MSNs)药物释放动力学控制的显著定位效应。

A prominent anchoring effect on the kinetic control of drug release from mesoporous silica nanoparticles (MSNs).

机构信息

Department of Chemical and Biochemical Engineering, Gachon University, San 65, Bokjeong-Dong, Sujeong-Gu, Seongnam City 461-701, South Korea.

Department of Chemical and Biochemical Engineering, Gachon University, San 65, Bokjeong-Dong, Sujeong-Gu, Seongnam City 461-701, South Korea.

出版信息

J Colloid Interface Sci. 2018 Jan 15;510:345-356. doi: 10.1016/j.jcis.2017.09.072. Epub 2017 Sep 21.

Abstract

This work demonstrated kinetically controlled release of model drugs (ibuprofen, FITC) from well-tailored mesoporous silica nanoparticles (MSNs) depending on the surface charges and molecular sizes of the drugs. The molecular interactions between entrapped drugs and the pore walls of MSNs controlled the release of the drugs through the pore channels of MSNs. Also, polydopamine (PDA) layer-coated MSNs (MSNs@PDA) was quite effective to retard the release of large FITC, in contrast to a slight retardation effect on relatively small Ibuprofen. Of all things, FITC (Fluorescein isothiocyanate)-labeled APTMS (3-aminopropyltrimethoxysilane) (APTMS-FITC conjugates) grafted onto the MSNs generate a pinch-effect on the pore channel (so-called a prominent anchoring effect), which was highly effective in trapping (or blocking) drug molecules at the pore mouth of the MSNs. The anchored APTMS-FITC conjugates provided not only tortuous pathways to the diffusing molecules, but also sustained release of the ibuprofen over a long period of time (∼7days). The fast release kinetics was predicted by an exponential equation based on Fick's law, while the slow release kinetics was predicted by Higuchi model.

摘要

这项工作展示了根据药物的表面电荷和分子大小,通过精心设计的介孔硅纳米粒子(MSNs)实现模型药物(布洛芬、FITC)的动力学控制释放。包埋药物与 MSNs 孔壁之间的分子相互作用通过 MSNs 的孔道控制药物的释放。此外,聚多巴胺(PDA)层包覆的 MSNs(MSNs@PDA)对大分子 FITC 的释放有很好的延迟作用,而对相对较小的布洛芬则只有轻微的延迟作用。在所有情况下,接枝到 MSNs 上的 FITC(异硫氰酸荧光素)标记的 APTMS(3-氨丙基三甲氧基硅烷)(APTMS-FITC 缀合物)在孔道上产生了一种夹挤效应(所谓的突出锚固效应),这对 MSNs 孔口处的药物分子具有很高的捕获(或阻断)作用。锚固的 APTMS-FITC 缀合物不仅为扩散分子提供了曲折的途径,而且还可以长时间(约 7 天)持续释放布洛芬。快速释放动力学由基于菲克定律的指数方程预测,而缓慢释放动力学由 Higuchi 模型预测。

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