Biodistribution, pharmacokinetics and toxicity evaluation of mannosylated gelatin nanoparticles of linezolid for anti-tubercular therapy

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.

KEYWORDS:

• Linezolid
• gelatin nanoparticles
• mannosylation
• pharmacokinetic
• biodistribution
• toxicity

Acknowledgments

We would like to thank the faculty members of SVKM’s NMIMS, School of Pharmacy & Technology Management, Shirpur, India for their support and encouragement throughout the research process.

Disclosure statement

The authors have no conflicts of interest.