Quinine Sulphate Microparticles as Treatment for Leishmaniasis.

BACKGROUND

Leishmaniasis is a neglected tropical disease caused by the parasite and transmitted by the female phlebotomine sandfly. The disease can affect the skin (least fatal) or internal organs (most fatal). Current treatment options for leishmaniasis have a number of adverse effects, and there appears to be resistance by the protozoan parasite ( spp.). Reports suggest that quinine sulphate, not indicated for leishmaniasis, is effective in killing the parasite. Indeed, the efficacy of any drug is dependent on the concentration at the target site, which is also almost dependent on drug formulation. The current study assessed the pharmacokinetic profile of the microparticulate formulation of quinine sulphate and its and efficacy against .

METHODS

Quinine sulphate was encapsulated in bovine serum albumin by the spray-drying method. Quinine sulphate microparticles were evaluated for size, zeta potential, drug content, encapsulation efficiency, and release properties. Afterwards, the pharmacokinetic characteristics of quinine sulphate microparticles were estimated and efficacy studies were also conducted.

RESULTS

The size range of the quinine sulphate microparticles was between 2.0 and 5.0 m. Microparticles had an average zeta potential of -35.2 mV and an encapsulation efficiency of 94.5%. Also, , , and AUC were all significantly desirable for quinine sulphate microparticles compared to the drug powder. Quinine sulphate microparticles significantly reduced parasite load in rat organs than amphotericin B.

CONCLUSION

Overall, quinine sulphate microparticles had better pharmacokinetic profile and showed higher efficacy against parasites . Thus, quinine sulphate microparticles have the potential, especially, in treating visceral leishmaniasis.