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琥珀酸α-生育酚修饰的右旋糖酐胶束作为潜在药物载体的制备、表征及评价

Preparation, Characterization and Evaluation of α-Tocopherol Succinate-Modified Dextran Micelles as Potential Drug Carriers.

作者信息

Yu Jingmou, Zhou Yufeng, Chen Wencong, Ren Jin, Zhang Lifang, Lu Lu, Luo Gan, Huang Hao

机构信息

School of Pharmacy and Life Sciences, Jiujiang University, 320 Xunyang East Road, Jiujiang 332000, China.

School of Chemical and Biological Engneering, Yichun University, 576 Xuefu Road, Yichun 336000, China.

出版信息

Materials (Basel). 2015 Sep 28;8(10):6685-6696. doi: 10.3390/ma8105332.

Abstract

In the present study, α-tocopherol succinate (TOS) conjugated dextran (Dex-TOS) was synthesized and characterized by fourier transform infrared (FT-IR) spectroscopy, ¹H nuclear magnetic resonance (¹H NMR), dynamic light scattering (DLS) and fluorescence spectroscopy. Dex-TOS could form nanoscaled micelles in aqueous medium. The critical micelle concentration (CMC) is 0.0034 mg/mL. Doxorubicin (Dox) was selected as a model drug. Dox-loaded Dex-TOS (Dex-TOS/Dox) micelles were prepared by a dialysis method. The size of Dex-TOS/Dox micelles increased from 295 to 325 nm with the Dox-loading content increasing from 4.21% to 8.12%. The Dex-TOS/Dox micelles were almost spherical in shape, as determined by transmission electron microscopy (TEM). release demonstrated that Dox release from the micelles was in a sustained manner for up to 96 h. The cellular uptake of Dex-TOS/Dox micelles in human nasopharyngeal epidermoid carcinoma (KB) cells is an endocytic process determined by confocal laser scanning microscopy (CLSM). Moreover, Dex-TOS/Dox micelles exhibited comparable cytotoxicity in contrast with doxorubicin hydrochloride. These results suggested that Dex-TOS micelles could be a promising carrier for drug delivery.

摘要

在本研究中,合成了α-生育酚琥珀酸酯(TOS)共轭葡聚糖(Dex-TOS),并通过傅里叶变换红外光谱(FT-IR)、¹H核磁共振(¹H NMR)、动态光散射(DLS)和荧光光谱对其进行了表征。Dex-TOS可在水性介质中形成纳米级胶束。临界胶束浓度(CMC)为0.0034 mg/mL。选择阿霉素(Dox)作为模型药物。通过透析法制备了载有Dox的Dex-TOS(Dex-TOS/Dox)胶束。随着Dox负载量从4.21%增加到8.12%,Dex-TOS/Dox胶束的尺寸从295 nm增加到325 nm。通过透射电子显微镜(TEM)测定,Dex-TOS/Dox胶束几乎呈球形。释放研究表明,Dox从胶束中的释放持续长达96小时。通过共聚焦激光扫描显微镜(CLSM)确定,人鼻咽表皮样癌(KB)细胞对Dex-TOS/Dox胶束的细胞摄取是一个内吞过程。此外,与盐酸阿霉素相比,Dex-TOS/Dox胶束表现出相当的细胞毒性。这些结果表明,Dex-TOS胶束可能是一种有前途的药物递送载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7c01/5455401/92e120fd88a2/materials-08-05332-g001.jpg

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