Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China.
Colloids Surf B Biointerfaces. 2013 Oct 1;110:138-47. doi: 10.1016/j.colsurfb.2013.04.009. Epub 2013 Apr 20.
In this study, a targeting drug delivery system based on mesoporous silica nanoparticle (MSN) was successfully developed for anti-cancer drug delivery and bioimaging. Carboxyl functionalized MSN (MSN/COOH) was firstly prepared and then modified with folate as the cancer targeting moiety and a near infrared fluorescent dye as labeling segment. Folate was conjugated to MSN/COOH via functional polyethyleneglycol (PEG), constructing the vector MSN/COOH-PEG-FA. The functionalization with carboxyl caused the pore surface of the nanocarrier more negative than native MSN, which could provide attractive forces between the nanoparticles and positively charged doxorubicin hydrochloride (DOX). Meanwhile, the folate modification significantly enhanced the cellular uptake of the delivery system compared to unmodified counterparts. Furthermore, the introduction of PEG increased the water dispersibility. Besides, the modification with the near infrared fluorescent dye Cy5 made the system effective for live cell and in vivo imaging. Therefore, the Cy5-MSN/COOH-PEG-FA system could be a promising nanocarrier for simultaneous diagnosis and treatment of diseases.
在这项研究中，成功开发了一种基于介孔硅纳米粒子（MSN）的靶向药物传递系统，用于抗癌药物输送和生物成像。首先制备了羧基功能化的 MSN（MSN/COOH），然后通过功能化聚乙二醇（PEG）将叶酸作为癌症靶向部分和近红外荧光染料作为标记部分进行修饰。叶酸通过功能化聚乙二醇（PEG）与 MSN/COOH 偶联，构建载体 MSN/COOH-PEG-FA。羧基的功能化使纳米载体的孔表面比天然 MSN 更负，这可以在纳米颗粒和带正电荷的盐酸多柔比星（DOX）之间提供吸引力。同时，与未修饰的相比，叶酸修饰显著提高了递药系统的细胞摄取。此外，PEG 的引入增加了水的分散性。此外，近红外荧光染料 Cy5 的修饰使该系统能够有效地用于活细胞和体内成像。因此，Cy5-MSN/COOH-PEG-FA 系统可能是一种很有前途的用于疾病同时诊断和治疗的纳米载体。
