ArticleDrug delivery and translational research2021
A novel amorphous solid dispersion based on drug-polymer complexation.
Article in Drug delivery and translational research, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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Who cites it
3 citing papers in PubMed, 5 citations in OpenAlex.
- Innovative Wound Healing Strategy Through Amorphization of Active Pharmaceutical Ingredients as an Effective Approach for Hydrogel Formulation.Pharmaceuticals (Basel, Switzerland) · 2025Review
- New Development in Understanding Drug-Polymer Interactions in Pharmaceutical Amorphous Solid Dispersions from Solid-State Nuclear Magnetic Resonance.Molecular pharmaceutics · 2022Review
- Amorphous Form of Carvedilol Phosphate-The Case of Divergent Properties.Molecules (Basel, Switzerland) · 2021Article
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Rafoxanide (RAF) is a poorly water-soluble drug that forms a complex with povidone K25 (PVP) in a cosolvent system containing acetone and an alkaline aqueous medium. This study aims to investigate the impact of RAF-PVP complexation on in vitro and in vivo release of RAF. We prepared two RAF amorphous solid dispersions (ASDs) spray-dried from these two cosolvents. The first is a complexation-based spray-drying using a 70% 0.1 N NaOH solution with 30% acetone. The second is a traditional spray-dried formulation containing 80% acetone and 20% ethanol. Evidence from multiple solid-state characterization techniques indicated that ASDs spray-dried using both methods were amorphous. However, RAF ASDs based on drug-polymer complexation in the feed solution demonstrated not only faster drug release during dissolution testing but also higher in vivo absorption in an animal model. The improved RAF release in the complexation-based ASD is due to (1) high energy state of RAF owing to the amorphous form, (2) high pH in the microenvironment due to the ionized state of RAF and residual sodium hydroxide, (3) increased apparent solubility of RAF results from RAF-PVP complexation in dissolution media and biological media, and (4) improved wettability.
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