Mycobacteria Research Laboratory, Department of Biological Sciences, Institute of Structural and Molecular Biology (ISMB), Birkbeck, University of London, Malet Street, London WC1E 7HX, UK.
Material Synthesis and Characterization Laboratory, Institute of Advanced Technology (ITMA), Universiti Putra Malaysia (UPM), Serdang 43400, Selangor, Malaysia.
Molecules. 2017 Oct 12;22(10):1697. doi: 10.3390/molecules22101697.
Tuberculosis (TB) is a dreadful bacterial disease, infecting millions of human and cattle every year worldwide. More than 50 years after its discovery, ethambutol continues to be an effective part of the World Health Organization's recommended frontline chemotherapy against TB. However, the lengthy treatment regimens consisting of a cocktail of antibiotics affect patient compliance. There is an urgent need to improve the current therapy so as to reduce treatment duration and dosing frequency. In this study, we have designed a novel anti-TB multifunctional formulation by fabricating graphene oxide with iron oxide magnetite nanoparticles serving as a nano-carrier on to which ethambutol was successfully loaded. The designed nanoformulation was characterised using various analytical techniques. The release of ethambutol from anti-TB multifunctional nanoparticles formulation was found to be sustained over a significantly longer period of time in phosphate buffer saline solution at two physiological pH (7.4 and 4.8). Furthermore, the nano-formulation showed potent anti-tubercular activity while remaining non-toxic to the eukaryotic cells tested. The results of this in vitro evaluation of the newly designed nano-formulation endorse its further development in vivo.
结核病（TB）是一种可怕的细菌性疾病，每年在全球范围内感染数百万人和牛。在发现它 50 多年后，乙胺丁醇仍然是世界卫生组织推荐的抗结核一线化疗的有效组成部分。然而，由抗生素鸡尾酒组成的长期治疗方案会影响患者的依从性。迫切需要改进目前的治疗方法，以减少治疗持续时间和剂量频率。在这项研究中，我们设计了一种新型的抗结核多功能制剂，方法是将氧化石墨烯与作为纳米载体的氧化铁磁铁矿纳米颗粒结合在一起，成功地将乙胺丁醇负载在上面。使用各种分析技术对设计的纳米制剂进行了表征。在磷酸盐缓冲盐水溶液中，在两个生理 pH 值（7.4 和 4.8）下，从抗结核多功能纳米粒子制剂中释放的乙胺丁醇被发现可以持续更长的时间。此外，该纳米制剂在对测试的真核细胞保持非毒性的同时表现出很强的抗结核活性。对新设计的纳米制剂进行的体外评估结果支持其在体内进一步开发。
