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基于包封卟啉衍生物的抗疟药开发策略。

Strategies for development of antimalarials based on encapsulated porphyrin derivatives.

作者信息

Deda Daiana K, Budu Alexandre, Cruz Laura N, Araki Koiti, Garcia Celia R S

机构信息

.

Departamento de Fisiologia, Instituto de Biociencias, Universidade de Sao Paulo..

出版信息

Mini Rev Med Chem. 2015;14(13):1055-71. doi: 10.2174/1389557515666150101094829.

Abstract

Despite the efforts in controlling the parasite and infection, and the significant progress achieved in recent years in its treatment, malaria is still prevalent in many regions and out of control in others. The repertoire of alternatives to fight malaria is being expanded, not only by designing new drugs but also by developing improved drug delivery systems able to enhance the antimalarial efficiency of conventional and new drugs. Among the new drugs that have been investigated, several publications report the use of porphyrin derivatives as antimalarials but their efficiency is contradictory. The low activity of porphyrins seems to be associated with low dispersibility and bioavailability. In this respect, Nanotechnology can provide efficient solutions to enhance bioavailability and delivery of conventional and new antimalarials, in order to assure high enough efficiency levels to inactivate the parasite. Thus, in this review we highlight the use of drug delivery systems for conventional and new antimalarials and we propose the encapsulation of porphyrins as a promising alternative for development of anti-malarial formulations.

摘要

尽管在控制疟原虫和感染方面做出了努力,且近年来在疟疾治疗上取得了重大进展,但疟疾在许多地区仍然流行,在其他一些地区则失控。对抗疟疾的替代方法库正在扩大,这不仅通过设计新药,还通过开发能够提高传统药物和新药抗疟效率的改进药物递送系统来实现。在已研究的新药中,有几篇出版物报道了使用卟啉衍生物作为抗疟药,但其效果相互矛盾。卟啉的低活性似乎与低分散性和生物利用度有关。在这方面,纳米技术可以提供有效的解决方案,以提高传统和新型抗疟药的生物利用度和递送,从而确保有足够高的效率水平来灭活疟原虫。因此,在本综述中,我们强调了传统和新型抗疟药药物递送系统的应用,并提出将卟啉封装作为开发抗疟制剂的一种有前景的替代方法。

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