Revisiting Niclosamide Formulation Approaches – a Pathway Toward Drug Repositioning

IF 4.7 2区医学 Q1 CHEMISTRY, MEDICINAL Drug Design, Development and Therapy Pub Date : 2024-09-17 DOI:10.2147/dddt.s473178

Mario Jug, Flavia Laffleur, Gioconda Millotti

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Abstract

Abstract: Niclosamide (NIC), an anthelmintic drug, has garnered recent attention for its potential as an antiviral, antibacterial, and chemotherapeutic agent, among other applications. Repurposing NIC presents a current trend, offering significant time and cost savings compared to developing entirely new therapeutic chemical entities. However, its drawback lies in poor solubility, resulting in notably low oral bioavailability. This review consolidates efforts to overcome this limitation by summarizing twelve categories of formulations, spanning derivatives, amorphous solid dispersions, co-crystals, nanocrystals, micelles, nanohybrids, lipid nanoparticles and emulsions, cyclodextrins, polymeric nanoparticles, dry powders for inhalation, 3D printlets, and nanofibers. These formulations cover oral, injectable, inhalable and potentially (trans)dermal routes of administration. Additionally, we present a comprehensive overview of NIC characteristics, including physico-chemical properties, metabolism, safety, and pharmacokinetics. Moreover, we identify gaps in formulation and administration pathways that warrant further investigation to address NIC poor bioavailability.

Keywords: niclosamide, drug repurposing, solubility, formulations, administration pathways, pharmaco-kinetics

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重新审视氯硝柳胺的配制方法--实现药物重新定位的途径

摘要：尼克洛沙胺（NIC）是一种抗蠕虫药物，最近因其作为抗病毒、抗菌和化疗药物等应用的潜力而备受关注。与开发全新的治疗化学实体相比，重新利用 NIC 可大大节省时间和成本，是当前的一种趋势。然而，其缺点在于溶解性差，导致口服生物利用度明显偏低。本综述总结了 12 类制剂，包括衍生物、无定形固体分散体、共晶体、纳米晶体、胶束、纳米混合物、脂质纳米颗粒和乳剂、环糊精、聚合物纳米颗粒、吸入用干粉、3D 打印小剂和纳米纤维，以此来克服这一局限性。这些制剂涵盖口服、注射、吸入以及潜在的（经）皮肤给药途径。此外，我们还全面概述了 NIC 的特性，包括物理化学特性、新陈代谢、安全性和药代动力学。此外，我们还指出了在制剂和给药途径方面存在的差距，这些差距值得进一步研究，以解决 NIC 生物利用率低的问题。关键词：尼氯沙坦；药物再利用；溶解度；制剂；给药途径；药代动力学

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来源期刊

Drug Design, Development and Therapy CHEMISTRY, MEDICINAL-PHARMACOLOGY & PHARMACY

CiteScore

9.00

自引率

0.00%

发文量

382

审稿时长

>12 weeks

期刊介绍： Drug Design, Development and Therapy is an international, peer-reviewed, open access journal that spans the spectrum of drug design, discovery and development through to clinical applications. The journal is characterized by the rapid reporting of high-quality original research, reviews, expert opinions, commentary and clinical studies in all therapeutic areas. Specific topics covered by the journal include: Drug target identification and validation Phenotypic screening and target deconvolution Biochemical analyses of drug targets and their pathways New methods or relevant applications in molecular/drug design and computer-aided drug discovery* Design, synthesis, and biological evaluation of novel biologically active compounds (including diagnostics or chemical probes) Structural or molecular biological studies elucidating molecular recognition processes Fragment-based drug discovery Pharmaceutical/red biotechnology Isolation, structural characterization, (bio)synthesis, bioengineering and pharmacological evaluation of natural products** Distribution, pharmacokinetics and metabolic transformations of drugs or biologically active compounds in drug development Drug delivery and formulation (design and characterization of dosage forms, release mechanisms and in vivo testing) Preclinical development studies Translational animal models Mechanisms of action and signalling pathways Toxicology Gene therapy, cell therapy and immunotherapy Personalized medicine and pharmacogenomics Clinical drug evaluation Patient safety and sustained use of medicines.