Quinine Sulphate Microparticles as Treatment for Leishmaniasis

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,...

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Main Authors: Grace Lovia Allotey-Babington, Seth Kwabena Amponsah, Thomas Nettey, Clement Sasu, Henry Nettey
Format: Article
Language:English
Published: Hindawi Limited 2020-01-01
Series:Journal of Tropical Medicine
Online Access:http://dx.doi.org/10.1155/2020/5278518
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spelling doaj-4caf2198bc8b4cddb70782861362c8442020-11-25T02:25:24ZengHindawi LimitedJournal of Tropical Medicine1687-96861687-96942020-01-01202010.1155/2020/52785185278518Quinine Sulphate Microparticles as Treatment for LeishmaniasisGrace Lovia Allotey-Babington0Seth Kwabena Amponsah1Thomas Nettey2Clement Sasu3Henry Nettey4Department of Pharmaceutics and Microbiology, School of Pharmacy, University of Ghana, P.O. Box LG 43 Legon, Accra, GhanaDepartment of Pharmacology and Toxicology, School of Pharmacy, University of Ghana, P.O. Box LG 43 Legon, Accra, GhanaDepartment of Pharmaceutics and Microbiology, School of Pharmacy, University of Ghana, P.O. Box LG 43 Legon, Accra, GhanaDepartment of Pharmaceutics and Microbiology, School of Pharmacy, University of Ghana, P.O. Box LG 43 Legon, Accra, GhanaDepartment of Pharmaceutics and Microbiology, School of Pharmacy, University of Ghana, P.O. Box LG 43 Legon, Accra, GhanaBackground. 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.http://dx.doi.org/10.1155/2020/5278518
collection DOAJ
language English
format Article
sources DOAJ
author Grace Lovia Allotey-Babington
Seth Kwabena Amponsah
Thomas Nettey
Clement Sasu
Henry Nettey
spellingShingle Grace Lovia Allotey-Babington
Seth Kwabena Amponsah
Thomas Nettey
Clement Sasu
Henry Nettey
Quinine Sulphate Microparticles as Treatment for Leishmaniasis
Journal of Tropical Medicine
author_facet Grace Lovia Allotey-Babington
Seth Kwabena Amponsah
Thomas Nettey
Clement Sasu
Henry Nettey
author_sort Grace Lovia Allotey-Babington
title Quinine Sulphate Microparticles as Treatment for Leishmaniasis
title_short Quinine Sulphate Microparticles as Treatment for Leishmaniasis
title_full Quinine Sulphate Microparticles as Treatment for Leishmaniasis
title_fullStr Quinine Sulphate Microparticles as Treatment for Leishmaniasis
title_full_unstemmed Quinine Sulphate Microparticles as Treatment for Leishmaniasis
title_sort quinine sulphate microparticles as treatment for leishmaniasis
publisher Hindawi Limited
series Journal of Tropical Medicine
issn 1687-9686
1687-9694
publishDate 2020-01-01
description 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.
url http://dx.doi.org/10.1155/2020/5278518
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