Lecturer, University of Medical Sciences, Ondo, Nigeria
Malaria drug discovery
Mainstay chemotherapy for malaria is often faced with the problem of instability and poor bio-distribution thus resulting in impaired pharmacokinetics. Nanomedicine has been acclaimed for its success in drug delivery and improved efficacy. The aim of the study was to assess the antiplasmodial efficacy and safety of curcumin-artesunate entrapped nanoparticle in mice model. Curcumin (C) and artesunate (A) were loaded in poly (D,L-lactic-co-glycolic acid) (PLGA) using solvent evaporation from oil-in-water single emulsion method. The nanoparticle formed was characterized for size, polydispersity index, zeta potential and entrapment efficiency. The in vitro release of drugs was also determined. The in vivo antiplasmodial activity of CA-PLGA nanoparticle was tested on Plasmodium berghei at 5, 10 and 70 mg/kg doses. The drug efficacy was determined at day 5, 8 and 12. Hematological and hepatic toxicity assays were performed. The mean particle sizes of drug entrapped PLGA-nanoformulation was 251.1±12.6 nm. The drugs entrapment efficiency was 22.3±0.4. There was a sustained drug release from PLGA for 7 days. The percentage suppression of P. berghei was consistently significantly higher in CA-PLGA 5 mg/kg at day 5 (79.0%), day 8 (72.5%), day 12 (75.2%) than the corresponding values 65.3, 64.2, 59.0 % in the positive control group (P<0.05). No significant difference in the mean values of the different blood parameters in all treatment groups with the exception of platelets which was significantly higher in the positive control group. Aspartate aminotransferase (AST) with mean value 44.0±1.0 U/L in CA-PLGA 70 mg/kg was significantly higher than the values recorded in the other treatment groups (P<0.05). Alanine aminotransferase (ALT) however was significantly lower (27.0±2.0 U/L) in the positive control group than in the other treatment groups (P<0.05). A simple method of dual entrapment of curcumin and artesunate with moderate entrapment efficiency, better antiplasmodial efficacy and low toxicity has been synthesized.
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