ABSTRACT

The present study explores the therapeutic potential of gelatin nanoparticles as a carrier for the delivery of linezolid, a repurposed drug for the treatment ofMycobactrium tuberculosis. However, it has significant issues of large dose and toxicity. To overcome this problem, linezolid loaded mannosylated gelatin nanoparticles were prepared for specific targeting to alveolar macrophages. The system was characterised for  in-vitro, ex-vivo and in-vivo pharmacokinetics, biodistribution and toxicity studies to evaluate the safety and efficacy of the formulation. The method resulted in small-sized (197–298 nm) nanoparticles with a low polydispersity index (0.127–0.148) and higher drug entrapment (51–56%). The formulation was capable of sustained drug release with a significant increase in mean residence time and the half-life. The system is capable of reducing the dose, dosing frequency, and toxic adverse effects, which ultimately improves patient compliance and, therefore, a promising approach for the effective management of tuberculosis.

摘要

本研究探讨了明胶纳米颗粒作为利奈唑胺载体的治疗潜力，利奈唑胺是一种用于治疗结核分枝杆菌的再利用药物。然而，它具有大剂量和毒性的显着问题。为了克服这个问题，制备了载有利奈唑胺的甘露糖化明胶纳米颗粒，用于特异性靶向肺泡巨噬细胞。该系统的特征在于 体外、 离体 和 体内  药代动力学、生物分布和毒性研究，以评估制剂的安全性和有效性。该方法产生了具有低多分散指数（0.127-0.148）和更高药物截留率（51-56%）的小尺寸（197-298 nm）纳米粒子。该制剂能够持续药物释放，平均停留时间和半衰期显着增加。该系统能够减少剂量、给药频率和毒性副作用，最终提高患者的依从性，因此是有效管理结核病的有希望的方法。