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将苯硝唑包裹于碳酸钙纳米颗粒中可提高其对克氏锥虫的选择性。

Nanoencapsulation of benznidazole in calcium carbonate increases its selectivity to Trypanosoma cruzi.

作者信息

Tessarolo Louise Donadello, de Menezes Ramon Róseo Paula Pessoa Bezerra, Mello Clarissa Perdigão, Lima Dânya Bandeira, Magalhães Emanuel Paula, Bezerra Eveline Matias, Sales Francisco Adilson Matos, Barroso Neto Ito Liberato, Oliveira Maria de Fátima, Dos Santos Ricardo Pires, Albuquerque Eudenilson L, Freire Valder Nogueira, Martins Alice Maria

机构信息

Departamento de Análises Clínicas e Toxicológicas,Faculdade de Farmácia,Universidade Federal do Ceará,Fortaleza, CE,Brasil.

Departamento de Ciências Naturais, Matemática e Estatística,Universidade Federal Rural do Semi-Árido,Mossoró, Rio Grande do Norte,Brasil.

出版信息

Parasitology. 2018 Aug;145(9):1191-1198. doi: 10.1017/S0031182018000197. Epub 2018 Apr 12.

Abstract

Chagas disease is a public health problem, affecting about 7 million people worldwide. Benznidazole (BZN) is the main treatment option, but it has limited effectiveness and can cause severe adverse effects. Drug delivery through nanoparticles has attracted the interest of the scientific community aiming to improve therapeutic options. The aim of this study was to evaluate the cytotoxicity of benznidazole-loaded calcium carbonate nanoparticles (BZN@CaCO3) on Trypanosoma cruzi strain Y. It was observed that BZN@CaCO3 was able to reduce the viability of epimastigote, trypomastigote and amastigote forms of T. cruzi with greater potency when compared with BZN. The amount of BZN necessary to obtain the same effect was up to 25 times smaller when loaded with CaCO3 nanoparticles. Also, it was observed that BZN@CaCO3 enhanced the selectivity index. Furthermore, the cell-death mechanism induced by both BZN and BZN@CaCO3 was evaluated, indicating that both substances caused necrosis and changed mitochondrial membrane potential.

摘要

恰加斯病是一个公共卫生问题,影响着全球约700万人。苯硝唑(BZN)是主要的治疗选择,但它疗效有限且会导致严重的不良反应。通过纳米颗粒进行药物递送已引起科学界的兴趣,旨在改善治疗选择。本研究的目的是评估载有苯硝唑的碳酸钙纳米颗粒(BZN@CaCO3)对克氏锥虫Y株的细胞毒性。观察到,与BZN相比,BZN@CaCO3能够更有效地降低克氏锥虫的前鞭毛体、无鞭毛体和锥鞭毛体形式的活力。当负载碳酸钙纳米颗粒时,获得相同效果所需的BZN量减少了多达25倍。此外,观察到BZN@CaCO3提高了选择性指数。此外,还评估了BZN和BZN@CaCO3诱导的细胞死亡机制,表明这两种物质均导致坏死并改变了线粒体膜电位。

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