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具有末端β-环糊精分子的光致发光糖树状大分子的合成作为一种生物相容性的 pH 敏感载体用于阿霉素的递送。

Synthesis of photoluminescent glycodendrimer with terminal β-cyclodextrin molecules as a biocompatible pH-sensitive carrier for doxorubicin delivery.

机构信息

Research Laboratory of Dendrimers and Nano-Biopolymers, Faculty of Chemistry, University of Tabriz, P.O. Box 51666, Tabriz, Iran.

Research Laboratory of Dendrimers and Nano-Biopolymers, Faculty of Chemistry, University of Tabriz, P.O. Box 51666, Tabriz, Iran; Research Center for Pharmaceutical Nanotechnology (RCPN), Tabriz University of Medical Science, Tabriz, Iran.

出版信息

Carbohydr Polym. 2020 Oct 15;246:116658. doi: 10.1016/j.carbpol.2020.116658. Epub 2020 Jun 17.

DOI:10.1016/j.carbpol.2020.116658
PMID:32747290
Abstract

In the present research, we prepared new glycodendrimer containing β-cyclodextrin (β-CD) in three steps. At first, graphene quantum dots (GQDs) synthesized through pyrolysis of the citric acid (CA). Then the polyamidoamine (PAMAM) dendrimer was grown from the surface of the modified GQDs (GQDs-PAMAM). Finally, the prepared GQDs-PAMAM was functionalized with β-CD to obtain the glycodendrimer (GQDs-PAMAM-β-CD). The synthesized glycodendrimer characterized using several techniques. The phenol-sulfuric acid test obtained the amount of the β-CD about 30.37 %. 61.2 % of doxorubicin (DOX) was loaded in the prepared glycodendrimer. DOX@GQDs-PAMAM-β-CD displayed the pH-sensitive drug release profile, which fitted the Higuchi kinetic model. The biological test outcomes showed that the GQDs-PAMAM-β-CD is a safe carrier with good capability in penetration to the cancer cells. Moreover, DOX@GQDs-PAMAM-β-CD exhibited more efficiency in the killing of the cancer cells compared to neat DOX. Obtained results suggested that prepared glycodendrimer could be a potential nanosystem for breast cancer treatment.

摘要

在本研究中,我们分三步制备了含有β-环糊精(β-CD)的新型糖基树枝状大分子。首先,通过柠檬酸(CA)的热解合成了石墨烯量子点(GQDs)。然后,多胺树枝状大分子(PAMAM)从修饰后的 GQDs(GQDs-PAMAM)表面生长。最后,将制备的 GQDs-PAMAM 用β-CD 功能化得到糖基树枝状大分子(GQDs-PAMAM-β-CD)。使用多种技术对合成的糖基树枝状大分子进行了表征。苯酚-硫酸试验得到β-CD 的量约为 30.37%。在制备的糖基树枝状大分子中负载了 61.2%的阿霉素(DOX)。DOX@GQDs-PAMAM-β-CD 显示出 pH 敏感的药物释放特性,符合 Higuchi 动力学模型。生物学测试结果表明,GQDs-PAMAM-β-CD 是一种安全的载体,具有良好的穿透癌细胞的能力。此外,与单纯的 DOX 相比,DOX@GQDs-PAMAM-β-CD 对癌细胞的杀伤效率更高。结果表明,所制备的糖基树枝状大分子可能是一种用于乳腺癌治疗的潜在纳米系统。

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