Laís de Castro Carvalho Silva, Luís Felipe Cunha Dos Reis, Luiz Cosme Cotta Malaquias, Flávia Chiva Carvalho, Rômulo Dias Novaes, Marcos José Marques
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引用次数: 0
Abstract
Background: Schistosomiasis is a neglected tropical disease caused by Schistosoma sp., and praziquantel (PZQ) is the first-line treatment. However, traditional PZQ formulations have low solubility and fast metabolism, limiting its effectiveness. Thus, nanoparticles have been proposed to improve the bioavailability and efficacy of poorly soluble antischistosomal drugs.
Aims: This systematic review used in vivo preclinical studies to map the available evidence and compare the efficacy of free PZQ and PZQ-based nanostructured formulations (N-PZQ) for schistosomiasis treatment.
Methods: PubMed, Embase, Scopus, and Web of Science were searched, and 1186 experimental studies published between 1974 and 2024 were screened. Parasitological, histopathological, pharmacokinetic, and toxicological outcomes were evaluated.
Results: Twelve relevant studies were identified exploring N-PZQ formulations based on liposomes, nanoliposomes, and nanocrystals. N-PZQ demonstrated better therapeutic efficacy than free PZQ, reducing parasite load, modifying oogram profiles, and down-regulating liver granuloma development (number and size). N-PZQ also exhibited improved pharmacokinetic profile, with enhanced bioavailability and longer half-life, as well as reduced toxicity (cytotoxicity, genotoxicity, and hepatotoxicity) compared to free PZQ.
Conclusion: PZQ-based nanostructured formulations represent a promising strategy to enhance schistosomiasis treatment by improving chemotherapy efficacy, optimizing antiparasitic responses, pharmacokinetics, and reducing drug toxicity.
背景:血吸虫病是由血吸虫引起的一种被忽视的热带疾病,吡喹酮(PZQ)是一线治疗药物。然而,传统的PZQ制剂溶解度低,代谢快,限制了其有效性。因此,纳米颗粒被提出用于提高难溶性抗血吸虫药物的生物利用度和疗效。目的:本系统综述使用体内临床前研究来绘制现有证据,并比较游离PZQ和基于PZQ的纳米结构制剂(N-PZQ)治疗血吸虫病的疗效。方法:检索PubMed、Embase、Scopus、Web of Science,筛选1974 ~ 2024年间发表的1186篇实验研究。评估了寄生虫学、组织病理学、药代动力学和毒理学结果。结果:12项相关研究确定了基于脂质体、纳米脂质体和纳米晶体的N-PZQ配方。N-PZQ的治疗效果优于游离PZQ,可降低寄生虫载量,改变卵谱,下调肝脏肉芽肿的发展(数量和大小)。与游离PZQ相比,N-PZQ还表现出更好的药代动力学特征,具有更高的生物利用度和更长的半衰期,并且毒性(细胞毒性、遗传毒性和肝毒性)降低。结论:基于pzq的纳米结构制剂通过提高化疗疗效、优化抗寄生虫反应、药代动力学和降低药物毒性来增强血吸虫病的治疗效果。
期刊介绍:
JPP keeps pace with new research on how drug action may be optimized by new technologies, and attention is given to understanding and improving drug interactions in the body. At the same time, the journal maintains its established and well-respected core strengths in areas such as pharmaceutics and drug delivery, experimental and clinical pharmacology, biopharmaceutics and drug disposition, and drugs from natural sources. JPP publishes at least one special issue on a topical theme each year.