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Stimuli-responsive non-ionic Gemini amphiphiles for drug delivery applications
Polymer Chemistry ( IF 4.1 ) Pub Date : 2020-09-29 , DOI: 10.1039/d0py01040e
Rashmi 1, 2, 3, 4 , Abhishek K. Singh 5, 6, 7, 8 , Katharina Achazi 5, 6, 7, 8 , Svenja Ehrmann 5, 6, 7, 8, 9 , Christoph Böttcher 5, 6, 7, 8, 9 , Rainer Haag 5, 6, 7, 8 , Sunil K. Sharma 1, 2, 3, 4
Affiliation  

A series of six novel disulfide-bond-linked Gemini amphiphiles have been synthesized using polyethylene glycol (PEG) as hydrophilic units and alkoxy aryl moieties as hydrophobic units. The self-assembling behaviour of the resulting amphiphiles was studied using fluorescence spectroscopy and dynamic light scattering (DLS). The inner hydrophobic core with an alkyl and fluoroalkyl chain aggregates differently in aqueous medium as evidenced by a cryo-TEM study. Also they are found to be capable of encapsulating a lipophilic guest. The encapsulation behaviour was studied using Nile red as a model hydrophobic dye and extended further by including curcumin and an anti-cancerous drug doxorubicin. Furthermore, for biological evaluation, their cytotoxicity and cellular uptake were studied. The presence of stimuli responsive disulfide linkages and the ester functionality provides the possibility of redox responsive and enzymatic release of the encapsulated cargo, which was studied by using various concentrations of glutathione (GSH) and an immobilized lipase Novozym 435.

中文翻译:

刺激反应性非离子双子两亲药物在药物输送中的应用

使用聚乙二醇(PEG)作为亲水单元和烷氧基芳基部分作为疏水单元,合成了一系列六个新颖的二硫键连接的Gemini两亲物。使用荧光光谱和动态光散射(DLS)研究了所得两亲物的自组装行为。低温TEM研究表明,具有烷基和氟烷基链的内部疏水核在水性介质中的聚集方式不同。还发现它们能够包封亲脂性客体。使用尼罗红作为模型疏水染料研究了包封行为,并通过包含姜黄素和抗癌药阿霉素进一步扩展了包封行为。此外,为了进行生物学评估,研究了它们的细胞毒性和细胞摄取。
更新日期:2020-11-03
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