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首页> 外文期刊>Journal of Tropical Medicine >Quinine Sulphate Microparticles as Treatment for Leishmaniasis
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Quinine Sulphate Microparticles as Treatment for Leishmaniasis

机译：奎宁硫酸盐微粒作为LeishManiaisis的治疗方法

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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.
机译：背景。 Leishmaniaisis是由Leishmania寄生虫引起的忽略热带病，并由雌性血红素砂蝇传播。该疾病会影响皮肤（最不致命的）或内脏（最致命的）。 LeishManiaisis的当前治疗方案具有许多不利影响，似乎由原生动物寄生虫（Leishmania SPP）似乎是抵抗力。报告表明，喹啉硫酸盐未指示Leishmaniaisis，是有效地杀死Leishmania寄生虫。实际上，任何药物的疗效取决于靶位点的浓度，这也几乎依赖于药物制剂。目前的研究评估了奎宁硫酸盐的微粒制剂的药代动力学分布及其体外和体内疗效对Leishmania Donovani的体内疗效。方法。通过喷雾干燥方法将奎宁硫酸盐包封在牛血清白蛋白中。评估喹啉硫酸盐微粒的尺寸，Zeta电位，药物含量，包封效率和体外释放性能。然后，还估计奎宁硫酸盐微粒的药代动力学特征，并进行了体内疗效研究。结果。奎宁硫酸盐微粒的尺寸范围在2.0和5.0？μm之间。微粒的平均Zeta电位为α35.2≤MV和封装效率为94.5％。此外，与药物粉末相比，CMAX，T1 / 2和AUC全部对奎宁硫酸盐微粒非常理想。奎宁硫酸盐微粒显着降低了大鼠器官的寄生虫载荷，而不是两性霉素B.结论。总体而言，奎宁硫酸盐微粒具有更好的药代动力学型材，并在体内对Leishmania Donovani寄生虫表现出更高的疗效。因此，奎宁硫酸盐微粒具有潜力，特别是在治疗内脏LeishManiaisis中。

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