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具有肝靶向和 pH 响应释放功能的介孔硅纳米粒子用于肝癌治疗中的靶向药物递送。

Mesoporous Silicon Nanoparticles with Liver-Targeting and pH-Response-Release Function Are Used for Targeted Drug Delivery in Liver Cancer Treatment.

机构信息

Guangdong Provincial University Engineering Technology Research Center of Natural Products and Drugs, Guangdong Pharmaceutical University, Guangzhou 510006, China.

Guangdong Metabolic Disease Research Center of Integrated Chinese and Western Medicine, Guangdong Pharmaceutical University, Guangzhou 510006, China.

出版信息

Int J Mol Sci. 2024 Feb 21;25(5):2525. doi: 10.3390/ijms25052525.

DOI:10.3390/ijms25052525
PMID:38473773
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10931546/
Abstract

This article aims to develop an aspirin-loaded double-modified nano-delivery system for the treatment of hepatocellular carcinoma. In this paper, mesoporous silica nanoparticles (MSN) were prepared by the "one-pot two-phase layering method", and polydopamine (PDA) was formed by the self-polymerization of dopamine as a pH-sensitive coating. Gal-modified PDA-modified nanoparticles (Gal-PDA-MSN) were synthesized by linking galactosamine (Gal) with actively targeted galactosamine (Gal) to PDA-coated MSN by a Michael addition reaction. The size, particle size distribution, surface morphology, BET surface area, mesoporous size, and pore volume of the prepared nanoparticles were characterized, and their drug load and drug release behavior in vitro were investigated. Gal-PDA-MSN is pH sensitive and targeted. MSN@Asp is different from the release curves of PDA-MSN@Asp and Gal-PDA-MSN@Asp, the drug release of PDA-MSN@Asp and Gal-PDA-MSN@Asp accelerates with increasing acidity. In vitro experiments showed that the toxicity and inhibitory effects of the three nanodrugs on human liver cancer HepG2 cells were higher than those of free Asp. This drug delivery system facilitates controlled release and targeted therapy.

摘要

本文旨在开发一种载阿司匹林的双修饰纳米递药系统用于治疗肝细胞癌。本文采用“一锅两相反相分层法”制备介孔硅纳米粒（MSN），并通过多巴胺的自聚合作用形成聚多巴胺（PDA）作为 pH 敏感的涂层。通过迈克尔加成反应将半乳糖胺（Gal）与主动靶向半乳糖胺（Gal）连接到 PDA 修饰的 MSN 上，合成 Gal-PDA- MSN。对制备的纳米粒的粒径、粒径分布、表面形态、BET 比表面积、介孔尺寸和孔体积进行了表征，并研究了其体外载药和药物释放行为。Gal-PDA-MSN 具有 pH 敏感性和靶向性。与 PDA-MSN@Asp 和 Gal-PDA-MSN@Asp 的释放曲线不同，随着酸度的增加，PDA-MSN@Asp 和 Gal-PDA-MSN@Asp 的药物释放加速。体外实验表明，三种纳米药物对人肝癌 HepG2 细胞的毒性和抑制作用均高于游离 Asp。该递药系统有利于控制释放和靶向治疗。

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