Enhanced anti-malarial efficacy of mefloquine delivered via cationic liposome in a murine model of experimental cerebral malaria

Eur J Pharm Biopharm. 2024 Apr:197:114210. doi: 10.1016/j.ejpb.2024.114210. Epub 2024 Feb 9.

Abstract

Malaria is a longstanding global health challenge that continues to afflict over 90 countries located in tropical and subtropical regions of the globe. The rise of drug-resistant malarial parasites has curtailed the therapeutic efficacy of a number of once-effective anti-malarials, including mefloquine. In the present study, we have taken advantage of drug encapsulation approach to elevate the anti-malarial potential of mefloquine. Encouragingly, our findings unveil that liposomal formulations of mefloquine outperform equivalent doses of free mefloquine, both in laboratory cultures and in a murine model of malaria. Intriguingly, a cationic liposomal mefloquine formulation, administered at four successive doses of 3 mg/kg body weight, achieves complete resolution of cerebral malaria in the murine model while avoiding noticeable toxic repercussions. Altogether, our study furnishes pre-clinical validation for a therapeutic strategy that can remarkably enhance the drug efficacy, offering a revitalizing solution for failing anti-malarials.

Keywords: Drug delivery; Liposome; Malaria; Mefloquine; Nanocarriers.

MeSH terms

  • Animals
  • Antimalarials* / pharmacology
  • Disease Models, Animal
  • Liposomes
  • Malaria, Cerebral* / drug therapy
  • Mefloquine / therapeutic use
  • Mice

Substances

  • Antimalarials
  • Mefloquine
  • Liposomes