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硫酸奎宁胺包封壳聚糖甘露醇纳米粒子在苏拉兔模型中的生物相容性和靶向效率。

Biocompatibility and Targeting Efficiency of Encapsulated Quinapyramine Sulfate-Loaded Chitosan-Mannitol Nanoparticles in a Rabbit Model of Surra.

机构信息

ICAR-National Research Centre on Equines, Hisar, Haryana, India

ICAR-National Research Centre on Equines, Hisar, Haryana, India.

出版信息

Antimicrob Agents Chemother. 2018 Oct 24;62(11). doi: 10.1128/AAC.00466-18. Print 2018 Nov.

Abstract

Quinapyramine sulfate (QS) produces trypanocidal effects against the parasite but is often poorly tolerated and causes serious reactions in animals. The encapsulation of QS in chitosan-mannitol to provide sustained release would improve both the therapeutic effect of QS and the quality of life of animals treated with this formulation. QS was encapsulated into a nanoformulation prepared from chitosan, tripolyphosphate, and mannitol nanomatrix (ChQS-NPs). ChQS-NPs were well ordered in shape, with nanoparticle size, as determined by transmission electron microscopy and atomic force microscopy. Our research revealed dose-dependent effects on biosafety and DNA damage in mammalian cells treated with ChQS-NPs. ChQS-NPs were absolutely risk-free at effective as well as many times higher doses against ChQS-NPs were effective in rabbits, as they killed the parasites, relieving the animals from the clinical symptoms of the disease. The extent of this protection was similar to that observed with the conventional drug at higher dosages (5 mg QS/kg of body weight). ChQS-NPs are safe, nontoxic, and more effective than QS and offer a promising alternative to drug delivery against surra in animal models. ChQS-NPs may be useful for the treatment of surra due to reduced dosages and frequency of administration.

摘要

硫酸喹吡胺(QS)对寄生虫具有杀锥虫作用,但通常耐受性差,会在动物中引起严重反应。将 QS 包封在壳聚糖-甘露醇中以提供缓释作用,将提高 QS 的治疗效果和用该制剂治疗的动物的生活质量。QS 被包裹在壳聚糖、三聚磷酸和甘露醇纳米基质(ChQS-NPs)制成的纳米制剂中。ChQS-NPs 形状整齐有序,通过透射电子显微镜和原子力显微镜确定纳米颗粒大小。我们的研究表明,用 ChQS-NPs 处理的哺乳动物细胞的生物安全性和 DNA 损伤存在剂量依赖性效应。ChQS-NPs 在有效剂量以及高得多的剂量下都是绝对安全的,对兔的 ChQS-NPs 有效,因为它们杀死了寄生虫,使动物摆脱了疾病的临床症状。这种保护程度与高剂量下的常规药物相似(5mg QS/kg 体重)。ChQS-NPs 安全、无毒,比 QS 更有效,为动物模型中的苏拉病药物输送提供了有希望的替代方案。由于剂量减少和给药频率降低,ChQS-NPs 可能对苏拉病的治疗有用。

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