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多功能介孔硅纳米粒子中小分子药物(布洛芬和对乙酰氨基酚)的比较释放动力学。

Comparative release kinetics of small drugs (ibuprofen and acetaminophen) from multifunctional mesoporous silica nanoparticles.

机构信息

Department of Chemical and Biological Engineering, Gachon University, 1342 Seongnamdaero, Seongnam-si 13120, Republic of Korea.

出版信息

J Mater Chem B. 2020 Mar 11;8(10):2096-2106. doi: 10.1039/c9tb02494h.

Abstract

Multifunctional mesoporous silica nanoparticles (MSNs) can confer dynamically varied release kinetics depending on the intermolecular interactions between model drugs and functional decorations on the MSNs. Herein, brush-like fluorescent conjugates were grafted on the pore walls of pristine MSNs for high drug loading and to impart fluorescence properties. The fluorescent MSNs (FMSNs) were further coated with polydopamine (PDA) and graphene oxide (GO) double layer, designated FMSNs@PDA and FMSNs@PDA@GO, respectively. The FMSNs@PDA@GO exhibited highly consistent drug release over one week (∼7 days) because of the consolidated PDA/GO double layer at neutral pH (7.4). However, the release rate of FMSN-Ibu@PDA@GO was increased at acidic pH (5.5) because the PDA/GO double layer was partially disrupted due to weakened π-π stacking and electrostatic interactions. The release kinetics of the FMSNs-based NPs (FMSNs, FMSNs@PDA, and FMSNs@PDA@GO) were systematically investigated using negatively charged hydrophobic ibuprofen and neutral hydrophilic acetaminophen at pH 7.4. In the FMSN-drug system, the release rate of acetaminophen was higher than that of ibuprofen because of the higher solubility of acetaminophen in aqueous solution. In addition, ibuprofen has a bulky molecular structure compared to acetaminophen, leading to its slower transmission through the porous channels of FMSNs. In the FMSNs-drug@PDA system, acetaminophen exhibited a slower release rate than ibuprofen, owing to the π-π stacking interactions in the transmission of neutral acetaminophen by the PDA coating layer. On the other hand, the FMSNs-drug@PDA@GO exhibited a slower ibuprofen release rate than acetaminophen, owing to the electrostatic repulsion effect of the negative GO layer. Our drug delivery system was demonstrated as an advanced delivery platform, in which the transmission rate is controlled by intermolecular interactions between the diffusing drugs and functional decorations on the nanocarrier.

摘要

多功能介孔硅纳米粒子(MSNs)可以根据模型药物与 MSNs 上的功能修饰之间的分子间相互作用,赋予其动态变化的释放动力学特性。在此,刷状荧光偶联物被接枝到原始 MSNs 的孔壁上,以实现高药物负载并赋予荧光性质。这些荧光 MSNs(FMSNs)进一步用聚多巴胺(PDA)和氧化石墨烯(GO)双层包覆,分别命名为 FMSNs@PDA 和 FMSNs@PDA@GO。由于在中性 pH(7.4)下 PDA/GO 双层的稳固存在,FMSNs@PDA@GO 在一周(约 7 天)内表现出高度一致的药物释放。然而,由于 PDA/GO 双层由于π-π 堆积和静电相互作用减弱而部分破坏,在酸性 pH(5.5)下,FMSN-Ibu@PDA@GO 的释放速率增加。FMSNs 基纳米粒子(FMSNs、FMSNs@PDA 和 FMSNs@PDA@GO)的释放动力学系统地研究了在 pH 7.4 下使用带负电荷的疏水性布洛芬和中性亲水性对乙酰氨基酚。在 FMSN-药物系统中,由于对乙酰氨基酚在水溶液中的溶解度较高,对乙酰氨基酚的释放速率高于布洛芬。此外,与对乙酰氨基酚相比,布洛芬具有较大的分子结构,导致其通过 FMSNs 的多孔通道的传输速度较慢。在 FMSNs-药物@PDA 系统中,由于 PDA 涂层层中中性对乙酰氨基酚的π-π 堆积相互作用,对乙酰氨基酚的释放速率比布洛芬慢。另一方面,FMSNs-药物@PDA@GO 中布洛芬的释放速率比对乙酰氨基酚慢,这是由于负 GO 层的静电排斥作用。我们的药物输送系统被证明是一种先进的输送平台,其中传输速率由扩散药物与纳米载体上的功能修饰之间的分子间相互作用控制。

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