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Challenges for cysteamine stabilization, quantification, and biological effects improvement
Journal of Pharmaceutical Analysis ( IF 8.8 ) Pub Date : 2020-03-21 , DOI: 10.1016/j.jpha.2020.03.007
Carla Atallah 1, 2 , Catherine Charcosset 2 , Hélène Greige-Gerges 1
Affiliation  

The aminothiol cysteamine, derived from coenzyme A degradation in mammalian cells, presents several biological applications. However, the bitter taste and sickening odor, chemical instability, hygroscopicity, and poor pharmacokinetic profile of cysteamine limit its efficacy. The use of encapsulation systems is a good methodology to overcome these undesirable properties and improve the pharmacokinetic behavior of cysteamine. Besides, the conjugation of cysteamine to the surface of nanoparticles is generally proposed to improve the intra-oral delivery of cyclodextrin-drug inclusion complexes, as well as to enhance the colorimetric detection of compounds by a gold nanoparticle aggregation method. On the other hand, the detection and quantification of cysteamine is a challenging mission due to the lack of a chromophore in its structure and its susceptibility to oxidation before or during the analysis. Derivatization agents are therefore applied for the quantification of this molecule. To our knowledge, the derivatization techniques and the encapsulation systems used for cysteamine delivery were not reviewed previously. Thus, this review aims to compile all the data on these methods as well as to provide an overview of the various biological applications of cysteamine focusing on its skin application.



中文翻译:

半胱胺稳定、定量和生物效应改善的挑战

氨基硫醇半胱胺源自哺乳动物细胞中辅酶 A 的降解,具有多种生物学应用。然而,半胱胺的苦味和令人作呕的气味、化学不稳定、吸湿性和较差的药代动力学特征限制了其功效。使用封装系统是克服这些不良特性并改善半胱胺药代动力学行为的良好方法。此外,通常提出将半胱胺缀合到纳米颗粒表面以改善环糊精-药物包合物的口腔内递送,以及增强金纳米颗粒聚集方法对化合物的比色检测。另一方面,半胱胺的检测和定量是一项具有挑战性的任务,因为其结构中缺乏发色团并且在分析之前或分析过程中易于氧化。因此,应用衍生剂来定量该分子。据我们所知,用于半胱胺递送的衍生化技术和封装系统以前没有经过审查。因此,本综述旨在汇编这些方法的所有数据,并概述半胱胺的各种生物应用,重点关注其皮肤应用。

更新日期:2020-03-21
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