Revisiting Niclosamide Formulation Approaches - a Pathway Toward Drug Repositioning.

Area of Science:

• Pharmaceutical Science
• Drug Delivery
• Medicinal Chemistry

Background:

• Niclosamide (NIC), an anthelmintic, is being investigated for antiviral, antibacterial, and anticancer properties.
• Drug repurposing offers a cost-effective alternative to novel drug development.
• Poor aqueous solubility and low oral bioavailability of NIC hinder its therapeutic potential.

Purpose of the Study:

• To review and categorize formulation strategies aimed at improving NIC's solubility and bioavailability.
• To provide a comprehensive overview of NIC's physicochemical properties, metabolism, safety, and pharmacokinetics.
• To identify research gaps in NIC formulation and administration for future development.

Main Methods:

• Literature review of twelve distinct formulation categories for NIC.
• Analysis of various administration routes including oral, injectable, and inhalable.
• Consolidation of data on NIC's characteristics and pharmacokinetic profiles.

Main Results:

• Twelve formulation categories were identified: derivatives, amorphous solid dispersions, co-crystals, nanocrystals, micelles, nanohybrids, lipid nanoparticles/emulsions, cyclodextrins, polymeric nanoparticles, dry powders for inhalation, 3D printlets, and nanofibers.
• These formulations target diverse administration routes, including oral, injectable, inhalable, and potentially transdermal.
• A comprehensive summary of NIC's properties, safety, and pharmacokinetics was compiled.

Conclusions:

• Various advanced formulation strategies show potential to overcome NIC's poor solubility and bioavailability.
• Further research is needed to optimize specific formulations and administration pathways for enhanced therapeutic efficacy.
• Addressing formulation and delivery challenges is crucial for unlocking NIC's full repurposing potential.