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COOH 端硅量子点作为一种高效的药物纳米载体用于靶向肿瘤细胞成像。

COOH-Terminated Silicon Quantum Dots as a Highly Efficient Drug Nanocarrier for Targeted Tumor Cell Imaging.

机构信息

School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, 325035, China.

出版信息

J Biomed Nanotechnol. 2021 Sep 1;17(9):1830-1839. doi: 10.1166/jbn.2021.3151.

DOI:10.1166/jbn.2021.3151
PMID:34688328
Abstract

Fluorescent silicon quantum dots (SiQDs) characterized by exceptional photostability and colloidal robustness as well as beneficial biocompatibility are fast becoming new pharmaceutical nanocarriers. With a view to efficiently loading cisplatin (CDDP) onto SiQDs, carboxylate group (COOH) terminated SiQDs were imperative because of chelate formation with CDDP. In this work, we employed a facial microwave irradiation route for rapidly synthesizing high-quality COOH-SiQDs through the use of 3-aminopropyl trimethoxy silane (APTMS) molecules to fulfil the role of silicon precursor and maleic acid (MA) as the agent for facilitating reduction. The SiQDs showed blue fluorescence with an associated photoluminescence quantum yield (PLQY) of 40.2%, the size of which was small at 3.2 ±0.6 nm, and long-lasting stability (an extensive range in pH (4-12) and concentrations of electrolytes reaching 3 Molarity of a solution of sodium chloride). As nanocarriers, carboxylic acids chelation generated a high loading of CDDP onto SiQDs (drug loading capacity, DLC up to 32.2% at pH = 9) and a drug release of CDDP up to 57.6% at pH = 5. Furthermore, the MTT assays demonstrated the non or low cytotoxicity of SiQDs and the role of the controlled release of SiQD-CDDP Finally, the prepared SiQD-CDDP were used for cell imaging, and further targeted labeling of some tumors after folic acid (FA) conjugation. These characteristics allow for the deployment of SiQDs as a highly efficient nanocarrier that facilitate the delivery of clinical drugs for the future.

摘要

荧光硅量子点 (SiQDs) 具有出色的光稳定性和胶体稳定性以及有益的生物相容性,正迅速成为新的药物纳米载体。为了将顺铂 (CDDP) 有效地装载到 SiQDs 上,由于与 CDDP 的螯合形成,需要羧酸盐 (COOH) 封端的 SiQDs。在这项工作中,我们通过使用 3-氨丙基三甲氧基硅烷 (APTMS) 分子作为硅前体和马来酸 (MA) 作为促进还原的试剂,采用简便的微波辐射方法快速合成了高质量的 COOH-SiQDs。SiQDs 显示出蓝色荧光,与之相关的光致发光量子产率 (PLQY) 为 40.2%,其尺寸小至 3.2 ±0.6nm,并且具有长期稳定性(在广泛的 pH 值(4-12)和电解质浓度范围内达到 3 摩尔氯化钠溶液)。作为纳米载体,羧酸螯合生成 SiQDs 上的高 CDDP 负载(药物负载能力,在 pH = 9 时高达 32.2%)和高达 57.6%的 CDDP 释放。此外,MTT 测定表明 SiQDs 的非或低细胞毒性以及 SiQD-CDDP 的控制释放的作用。最后,制备的 SiQD-CDDP 用于细胞成像,并在叶酸 (FA) 缀合后进一步靶向标记一些肿瘤。这些特性使得 SiQDs 能够作为一种高效的纳米载体,用于未来的临床药物输送。

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