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非离子型两亲性 bola 分子的合成及其在药物递送应用中的自组装和传输行为研究。

Synthesis of non-ionic bolaamphiphiles and study of their self-assembly and transport behaviour for drug delivery applications.

作者信息

Singh Abhishek K, Achazi Katharina, Schade Boris, Böttcher Christoph, Haag Rainer, Sharma Sunil K

机构信息

Department of Chemistry, University of Delhi Delhi 110 007 India

Institut für Chemie und Biochemie, Freie Universität Berlin Takustraße 3 14195 Berlin Germany

出版信息

RSC Adv. 2018 Sep 12;8(55):31777-31782. doi: 10.1039/c8ra05921g. eCollection 2018 Sep 5.

Abstract

A series of four bolaamphiphiles with different hydrophilic units has been synthesised. All the amphiphiles were well characterised from their physiochemical data. The aggregation tendency of newly synthesised amphiphiles was studied using fluorescence spectroscopy, dynamic light scattering (DLS), and cryogenic electron microscopy (cryo-TEM). Furthermore, their application as nanocarriers for hydrophobic guests was demonstrated by using two established standards, the dye Nile red and the drug nimodipine. A cytotoxicity and cellular uptake study has been carried out using A549 cells. Due to the presence of an ester linkage in PEG based bolaamphiphiles, a drug release study was performed in the presence of an immobilized enzyme Novozym-435 (a lipase).

摘要

已经合成了一系列具有不同亲水单元的双极两亲分子。所有两亲分子都通过其物理化学数据得到了很好的表征。使用荧光光谱、动态光散射(DLS)和低温电子显微镜(cryo-TEM)研究了新合成两亲分子的聚集趋势。此外,通过使用两种既定标准,即染料尼罗红和药物尼莫地平,证明了它们作为疏水性客体的纳米载体的应用。使用A549细胞进行了细胞毒性和细胞摄取研究。由于基于聚乙二醇的双极两亲分子中存在酯键,因此在固定化酶诺维信-435(一种脂肪酶)存在的情况下进行了药物释放研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/49b2/9085746/531d6672fa52/c8ra05921g-f1.jpg

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