Comparative Evaluation of Amodiaquine and Quinine Sulphate Microspheres in the Treatment of Leishmaniasis

Abstract

Leishmaniasis is an infectious protozoan disease caused by the Leishmania parasite and transmitted by the female phlebotomine sand fly. Pentavalent antimicrobials have been the backbones for treatment however certain antiprotozoal such as quinine sulphate and amodiaquine among others have been proven to be effective in this regard. The numerous side effects, cost and low availability of current medication has necessitated the need for alternate delivery of this drug hence the emergence of the formulation of drugs into microparticles. Microparticles are known to possess unique physicochemical properties that make them suitable for the management of this debilitating and disfiguring disease. The aim of this research was to specifically assess an alternate formulation for the treatment of leishmaniasis by making microparticulate forms of amodiaquine and quinine sulphate for use in the treatment of leishmaniasis. Using bovine serum albumin as the polymer matrix, amodiaquine and quinine sulfate microparticles were formulated using the spray drying method by crosslinking in solution. The microparticles formed were characterized then the particle size was determined using a Scanning Electron Microscope and the zeta potential determined. The drug content and encapsulation were then determined by preparing standard solutions of each drug. With the aid of the UV/Vis spectrophotometer and CytoFluor well plate reader, the absorbance and intensity were measured respectively and the parameters calculated. An in vitro release studies was then performed. The results showed that both amodiaquine and quinine sulphate microparticles had a percentage release of 100% and 2.6% respectively over 24 hours and encapsulation efficiency of 94.5% and 111% respectively. This study served as a significant breakthrough as amodiaquine, and quinine sulphate microparticles were successfully formed using the spray dryer method by solution crosslinking paving the way for use in leishmaniasis.

KEYWORDS: amodiaquine, quinine sulphate, encapsulation, pharmacokinetics, microparticle