ArticlePharmaceutics2021
Amorphous Solid Dispersions and the Contribution of Nanoparticles to In Vitro Dissolution and In Vivo Testing: Niclosamide as a Case Study.
Article in Pharmaceutics, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed.
- Development of hesperidin loaded lipid-chitosan nanoparticles: physicochemical characterization, molecular docking and ex vivo study.Scientific reports · 2026Article
- Soluplus Stabilized Amorphous Dispersions for Enhanced Oral Absorption of Felodipine.Current drug delivery · 2026Article
- Comparative evaluation of ternary amorphous solid dispersions: Identifying optimal excipient systems for enhancing drug solubility.International journal of pharmaceutics: X · 2025Review
- Niclosamide - encapsulated lipid nanoparticles for the reversal of pulmonary fibrosis.Materials today. Bio · 2024Article
- Revisiting Niclosamide Formulation Approaches - a Pathway Toward Drug Repositioning.Drug design, development and therapy · 2024Review
- Enteric coating of tablets containing an amorphous solid dispersion of an enteric polymer and a weakly basic drug: A strategy to enhance in vitro release.International journal of pharmaceutics · 2023Article
- Dehydration of Niclosamide Monohydrate Polymorphs: Different Mechanistic Pathways to the Same Product.Crystal growth & design · 2023Article
- Salicylanilides and Their Anticancer Properties.International journal of molecular sciences · 2023Review
- Oral Delivery of Niclosamide as an Amorphous Solid Dispersion That Generates Amorphous Nanoparticles during Dissolution.Pharmaceutics · 2022Article
- Niclosamide-loaded nanoparticles disrupt Candida biofilms and protect mice from mucosal candidiasis.PLoS biology · 2022Article
- A Niclosamide-releasing hot-melt extruded catheter prevents Staphylococcus aureus experimental biomaterial-associated infection.Scientific reports · 2022Article
- Effects of curcumin and γ-oryzanol solid dispersion on the brain of middle-aged rats.Biomedical reports · 2022Article
- Cyclodextrin and its derivatives as effective excipients for amorphous ulipristal acetate systems.RSC advances · 2022Article
- The Value of Bead Coating in the Manufacturing of Amorphous Solid Dispersions: A Comparative Evaluation with Spray Drying.Pharmaceutics · 2022Article
- Hesperidin-Loaded Lipid Polymer Hybrid Nanoparticles for Topical Delivery of Bioactive Drugs.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Injectable niclosamide nanohybrid as an anti-SARS-CoV-2 strategy.Colloids and surfaces. B, Biointerfaces · 2021Article
- Niclosamide encapsulated in mesoporous silica and geopolymer: A potential oral formulation for COVID-19.Microporous and mesoporous materials : the official journal of the International Zeolite Association · 2021Article
- Impact of Laser Speed and Drug Particle Size on Selective Laser Sintering 3D Printing of Amorphous Solid Dispersions.Pharmaceutics · 2021Article
- Niclosamide inhalation powder made by thin-film freezing: Multi-dose tolerability and exposure in rats and pharmacokinetics in hamsters.International journal of pharmaceutics · 2021Article
- Hydrotalcite-Niclosamide Nanohybrid as Oral Formulation towards SARS-CoV-2 Viral Infections.Pharmaceuticals (Basel, Switzerland) · 2021Article
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Authors and funding
3 authors.
Funding
Abstract
We developed an amorphous solid dispersion (ASD) of the poorly water-soluble molecule niclosamide that achieved a more than two-fold increase in bioavailability. Notably, this niclosamide ASD formulation increased the apparent drug solubility about 60-fold relative to the crystalline material due to the generation of nanoparticles. Niclosamide is a weakly acidic drug, Biopharmaceutics Classification System (BCS) class II, and a poor glass former with low bioavailability in vivo. Hot-melt extrusion is a high-throughput manufacturing method commonly used in the development of ASDs for increasing the apparent solubility and bioavailability of poorly water-soluble compounds. We utilized the polymer poly(1-vinylpyrrolidone-co-vinyl acetate) (PVP-VA) to manufacture niclosamide ASDs by extrusion. Samples were analyzed based on their microscopic and macroscopic behavior and their intermolecular interactions, using differential scanning calorimetry (DSC), X-ray diffraction (XRD), nuclear magnetic resonance (NMR), Fourier-transform infrared (FTIR), and dynamic light scattering (DLS). The niclosamide ASD generated nanoparticles with a mean particle size of about 100 nm in FaSSIF media. In a side-by-side diffusion test, these nanoparticles produced a four-fold increase in niclosamide diffusion. We successfully manufactured amorphous extrudates of the poor glass former niclosamide that showed remarkable in vitro dissolution and diffusion performance. These in vitro tests were translated to a rat model that also showed an increase in oral bioavailability.
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