Abstract
Background Leishmaniasis is a neglected tropical disease caused by the Leishmania 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 (Leishmania spp.). Reports suggest that quinine sulphate, not indicated for leishmaniasis, is effective in killing the Leishmania 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 in vitro and in vivo efficacy against Leishmania donovani. 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 in vitro release properties. Afterwards, the pharmacokinetic characteristics of quinine sulphate microparticles were estimated and in vivo efficacy studies were also conducted. Results The size range of the quinine sulphate microparticles was between 2.0 and 5.0 µm. Microparticles had an average zeta potential of −35.2 mV and an encapsulation efficiency of 94.5%. Also, Cmax, t1/2, 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 Leishmania donovani parasites in vivo. Thus, quinine sulphate microparticles have the potential, especially, in treating visceral leishmaniasis.
Highlights
Leishmaniasis, a neglected tropical disease, is known to cause morbidity in more than 1 billion people worldwide [1]
Leishmaniasis presents in 3 major forms: visceral leishmaniasis, called kala-azar, which can destroy internal organs such as the liver, spleen, and lungs; mucocutaneous leishmaniasis, which affects mainly mucous membranes; and cutaneous leishmaniasis, which mostly affects the skin and could lead to skin sores [6]
Particles Size Distribution, Zeta Potential, and Encapsulation Efficiency. e average size of quinine sulphateBSA microparticles obtained ranged between 2.0 and 5.0 μm, with a polydispersity index (PDI) of 0.31. e value of the PDI indicates that the size distribution may be broad. e scanning electron micrograph (Figure 1) showed that the particles were irregularly shaped and porous. e scanning electron microscope (SEM) image, showed a couple of large particles, explaining the value of PDI obtained. e encapsulation efficiency was calculated to be about 95%
Summary
Leishmaniasis, a neglected tropical disease, is known to cause morbidity in more than 1 billion people worldwide [1]. Leishmaniasis is a neglected tropical disease caused by the Leishmania parasite and transmitted by the female phlebotomine sandfly. Current treatment options for leishmaniasis have a number of adverse effects, and there appears to be resistance by the protozoan parasite (Leishmania spp.). Reports suggest that quinine sulphate, not indicated for leishmaniasis, is effective in killing the Leishmania parasite. E current study assessed the pharmacokinetic profile of the microparticulate formulation of quinine sulphate and its in vitro and in vivo efficacy against Leishmania donovani. Quinine sulphate microparticles were evaluated for size, zeta potential, drug content, encapsulation efficiency, and in vitro release properties. Quinine sulphate microparticles significantly reduced parasite load in rat organs than amphotericin B. Quinine sulphate microparticles had better pharmacokinetic profile and showed higher efficacy against Leishmania donovani parasites in vivo. Quinine sulphate microparticles had better pharmacokinetic profile and showed higher efficacy against Leishmania donovani parasites in vivo. us, quinine sulphate microparticles have the potential, especially, in treating visceral leishmaniasis
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