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半胱胺稳定化、定量分析及生物效应改善方面的挑战。

Challenges for cysteamine stabilization, quantification, and biological effects improvement.

作者信息

Atallah Carla, Charcosset Catherine, Greige-Gerges Hélène

机构信息

Bioactive Molecules Research Laboratory, Doctoral School of Sciences and Technologies, Faculty of Sciences, Lebanese University, Lebanon.

Laboratory of Automatic Control, Chemical and Pharmaceutical Engineering, Claude Bernard Lyon 1 University, France.

出版信息

J Pharm Anal. 2020 Dec;10(6):499-516. doi: 10.1016/j.jpha.2020.03.007. Epub 2020 Mar 21.

Abstract

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.

摘要

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、令人作呕的气味、化学不稳定性、吸湿性以及较差的药代动力学特性限制了其功效。使用包封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,通常建议将半胱胺与纳米颗粒表面结合,以改善环糊精 - 药物包合物的口腔内递送,并通过金纳米颗粒聚集法增强化合物的比色检测。另一方面,由于半胱胺结构中缺乏发色团且在分析前或分析过程中易被氧化,其检测和定量是一项具有挑战性的任务。因此,衍生化试剂被用于该分子的定量分析。据我们所知,此前尚未对半胱胺递送所使用的衍生化技术和包封系统进行综述。因此,本综述旨在汇总这些方法的所有数据,并概述半胱胺的各种生物学应用,重点关注其在皮肤方面的应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5871/7775854/901b26493348/fx1.jpg

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