Key Laboratory of Functional Inorganic Materials Chemistry (Ministry of Education), School of Chemistry and Material Science, Heilongjiang University, Harbin 150080, China.
College of Chemistry & Chemical Engineering, Harbin Normal University, Harbin 150025, China.
Carbohydr Polym. 2021 Oct 1;269:118327. doi: 10.1016/j.carbpol.2021.118327. Epub 2021 Jun 10.
In this study, a novel polymer based on aggregation-induced emission (AIE) fluorogen, biotin and disulfide bonds modified chitosan (TPE-bi(SS-CS-Bio)) was designed and synthesized. The polymer could self-assemble into micelles in aqueous media and encapsulate paclitaxel (PTX) into the core with high drug loading. Fluorescence study indicated that the micelles exhibited excellent AIE feature with intense blue fluorescence emitted. In vitro drug release study indicated that the micelles could disassemble rapidly in the presence of high level of glutathione. The modification by biotin could enhance the cellular uptake of the micelles. The drug-loaded micelles possessed remarkable cytotoxicity against MCF-7 cells, and their distribution in the cells could be traced due to the excellent AIE feature. In vivo antitumor efficacy study demonstrated the superior antitumor activity of the PTX-loaded TPE-bi(SS-CS-Bio) micelles. These results indicated that TPE-bi(SS-CS-Bio) has the ability of biological imaging and can be used as a potential carrier for PTX.
在这项研究中，设计和合成了一种基于聚集诱导发射（AIE）荧光团、生物素和二硫键修饰壳聚糖（TPE-bi（SS-CS-Bio）的新型聚合物。该聚合物在水介质中可以自组装成胶束，并将紫杉醇（PTX）包埋在核心中，具有较高的载药量。荧光研究表明，胶束表现出优异的 AIE 特性，发出强烈的蓝色荧光。体外药物释放研究表明，在高浓度谷胱甘肽存在下，胶束可以迅速解体。生物素的修饰可以增强胶束的细胞摄取。载药胶束对 MCF-7 细胞具有显著的细胞毒性，由于其优异的 AIE 特性，可以追踪其在细胞内的分布。体内抗肿瘤疗效研究表明，载药 TPE-bi（SS-CS-Bio）胶束具有优异的抗肿瘤活性。这些结果表明，TPE-bi（SS-CS-Bio）具有生物成像的能力，并可用作 PTX 的潜在载体。
