Organic solvent-free benznidazole nanosuspension as an approach to a novel pediatric formulation for Chagas disease.

IF 3 Q2 PHARMACOLOGY & PHARMACY Therapeutic delivery Pub Date : 2024-01-01 Epub Date: 2024-08-05 DOI:10.1080/20415990.2024.2380244

María Sol Magi, Lucía Lopez-Vidal, Mónica Cristina García, Cinthia Carolina Stempin, Constanza Marin, Belkys Maletto, Santiago Daniel Palma, Juan Pablo Real, Alvaro Federico Jimenez-Kairuz

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Abstract

Aim: Benznidazole (BNZ), a class-II drug, is the primary treatment for Chagas disease, but its low aqueous solubility presents challenges in formulation and efficacy. Nanosuspensions (NS) could potentially address these issues.Methods: BNZ-NS were prepared using a simple, organic solvents-free nano-milling approach. Physicochemical characterizations were conducted on both NS and lyophilized solid-state BNZ-nanocrystals (NC).Results: BNZ-NS exhibited particle size <500 nm, an acceptable polydispersity index (0.23), high Z-potential, and physical stability for at least 90 days. BNZ-NC showed tenfold higher solubility than pure BNZ. Dissolution assays revealed rapid BNZ-NS dissolution. BNZ-NC demonstrated biocompatibility on an eukaryotic cell and enhanced BNZ efficacy against trypomastigotes of Trypanosoma cruzi.Conclusion: BNZ-NS offers a promising alternative, overcoming limitations associated with BNZ for optimized pharmacotherapy.

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无有机溶剂苯并咪唑纳米悬浮剂作为治疗南美锥虫病的新型儿科制剂的一种方法。

目的：苯并咪唑（BNZ）是一种二类药物，是治疗南美锥虫病的主要药物，但其水溶性较低，给配制和疗效带来了挑战。纳米悬浮剂（NS）有可能解决这些问题。方法：采用简单、无有机溶剂的纳米研磨方法制备 BNZ-NS。对纳米悬浮剂和冻干固态 BNZ 纳米晶体（NC）进行了物理化学表征。结果显示BNZ-NS 的粒度与克鲁斯锥虫的粒度一致。结论：BNZ-NSBNZ-NS 是一种很有前景的替代品，它克服了 BNZ 在优化药物治疗方面的局限性。

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来源期刊

Therapeutic delivery PHARMACOLOGY & PHARMACY-

CiteScore

5.50

自引率

0.00%

发文量

期刊介绍： Delivering therapeutics in a way that is right for the patient - safe, painless, reliable, targeted, efficient and cost effective - is the fundamental aim of scientists working in this area. Correspondingly, this evolving field has already yielded a diversity of delivery methods, including injectors, controlled release formulations, drug eluting implants and transdermal patches. Rapid technological advances and the desire to improve the efficacy and safety profile of existing medications by specific targeting to the site of action, combined with the drive to improve patient compliance, continue to fuel rapid research progress. Furthermore, the emergence of cell-based therapeutics and biopharmaceuticals such as proteins, peptides and nucleotides presents scientists with new and exciting challenges for the application of therapeutic delivery science and technology. Successful delivery strategies increasingly rely upon collaboration across a diversity of fields, including biology, chemistry, pharmacology, nanotechnology, physiology, materials science and engineering. Therapeutic Delivery recognizes the importance of this diverse research platform and encourages the publication of articles that reflect the highly interdisciplinary nature of the field. In a highly competitive industry, Therapeutic Delivery provides the busy researcher with a forum for the rapid publication of original research and critical reviews of all the latest relevant and significant developments, and focuses on how the technological, pharmacological, clinical and physiological aspects come together to successfully deliver modern therapeutics to patients. The journal delivers this essential information in concise, at-a-glance article formats that are readily accessible to the full spectrum of therapeutic delivery researchers.