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基于氧化石墨烯功能化壳聚糖的聚电解质纳米复合材料用于靶向和 pH 响应型药物传递。

Graphene oxide based functionalized chitosan polyelectrolyte nanocomposite for targeted and pH responsive drug delivery.

机构信息

Department of Chemistry, School of Physical and Mathematical Sciences, University of Kerala, Kariavattom, Trivandrum 695 581, India.

Department of Chemistry, School of Physical and Mathematical Sciences, University of Kerala, Kariavattom, Trivandrum 695 581, India.

出版信息

Int J Biol Macromol. 2020 May 1;150:468-479. doi: 10.1016/j.ijbiomac.2020.02.053. Epub 2020 Feb 7.

DOI:10.1016/j.ijbiomac.2020.02.053
PMID:32044367
Abstract

Graphene oxide (GO) was first modified to amine functionalized GO (AGO) and acts as a cationic polyelectrolyte. Chitosan (CS) was conjugated with folic acid (FA) through N, N´ -Dicyclohexylcarbodiimide coupling to form FA-CS. After this, itaconic acid and acrylic acid monomers are grafted to the hydroxyl group of CS using ethyleneglycol dimethacrylate as cross linker and potassium peroxydisulfate as an initiator to generate -COOH functional groups and forming chemically modified chitosan (CMCS). Further doxorubicin (DOX) loaded into the FA-CMCS/AGO through π-π stacking interactions. The resulting nanocomposite was characterized by FTIR, SEM, TEM, Raman, AFM, DLS and ZP. The drug loading capacity was as high as 95.0% and the drug release rate at pH 5.3 was significantly higher than that under physiological conditions of pH 7.4. Cell viability of L929, HeLa and MCF7 cells was studied. The studies suggest the drug carrier has potential clinical applications for anticancer drug delivery.

摘要

氧化石墨烯(GO)首先被修饰为胺功能化的氧化石墨烯(AGO),并作为阳离子聚电解质。壳聚糖(CS)通过 N,N´-二环己基碳二亚胺偶联与叶酸(FA)结合形成 FA-CS。之后,使用乙二醇二甲基丙烯酸酯作为交联剂,过硫酸钾作为引发剂,将衣康酸和丙烯酸单体接枝到 CS 的羟基上,形成 -COOH 官能团,形成化学改性壳聚糖(CMCS)。进一步通过 π-π 堆积相互作用将阿霉素(DOX)负载到 FA-CMCS/AGO 中。所得纳米复合材料通过傅里叶变换红外光谱(FTIR)、扫描电子显微镜(SEM)、透射电子显微镜(TEM)、拉曼光谱(Raman)、原子力显微镜(AFM)、动态光散射(DLS)和 Zeta 电位(ZP)进行了表征。载药能力高达 95.0%,在 pH 5.3 下的药物释放率明显高于生理条件下 pH 7.4 的药物释放率。研究了 L929、HeLa 和 MCF7 细胞的细胞活力。研究表明,该药物载体具有用于抗癌药物输送的潜在临床应用。

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