Souza Tainá Santos, Moreira Diogo Rodrigo Magalhães, Marcelino Henrique Rodrigues
Graduation Program in Pharmacy, College of Pharmacy, Federal University of Bahia, Salvador 40170-115, BA, Brazil.
Fundação Oswaldo Cruz (Fiocruz), Instituto Gonçalo Moniz, Salvador 40296-710, BA, Brazil.
Pharmaceutics. 2022 Jun 30;14(7):1383. doi: 10.3390/pharmaceutics14071383.
Decoquinate (DQ) is an antimicrobial agent commonly used as a feed additive for birds for human consumption. Its use as an additive is well established, but DQ has the potential for therapy as an antimicrobial drug for veterinary treatment and its optimized derivatives and/or formulations, mainly nanoformulations, have antimicrobial activity against pathogens that infect humans. However, DQ has a high partition coefficient and low solubility in aqueous fluids, and these biopharmaceutical properties have limited its use in humans. In this review, we highlight the antimicrobial activity and pharmacokinetic properties of DQ and highlight the solutions currently under investigation to overcome these drawbacks. A literature search was conducted focusing on the use of decoquinate against various infectious diseases in humans and animals. The search was conducted in several databases, including scientific and patent databases. Pharmaceutical nanotechnology and medicinal chemistry are the tools of choice to achieve human applications, and most of these applications have been able to improve the biopharmaceutical properties and pharmacokinetic profile of DQ. Based on the results presented here, DQ prototypes could be tested in clinical trials for human application in the coming years.
癸氧喹酯(DQ)是一种抗菌剂,常用作供人类食用禽类的饲料添加剂。其作为添加剂的用途已得到充分确立,但DQ有作为兽用抗菌药物进行治疗的潜力,其优化的衍生物和/或制剂(主要是纳米制剂)对感染人类的病原体具有抗菌活性。然而,DQ具有高分配系数且在水性流体中的溶解度低,这些生物药剂学性质限制了其在人类中的应用。在本综述中,我们重点介绍了DQ的抗菌活性和药代动力学性质,并着重介绍了目前正在研究的克服这些缺点的解决方案。我们针对癸氧喹酯用于人类和动物各种传染病的情况进行了文献检索。检索在包括科学和专利数据库在内的几个数据库中进行。药物纳米技术和药物化学是实现人类应用的首选工具,并且这些应用大多能够改善DQ的生物药剂学性质和药代动力学特征。基于此处给出的结果,未来几年可在临床试验中对DQ原型进行人体应用测试。