ArticlePharmaceutics2018
Polymer⁻Surfactant System Based Amorphous Solid Dispersion: Precipitation Inhibition and Bioavailability Enhancement of Itraconazole.
Article in Pharmaceutics, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed, 73 citations in OpenAlex.
- Navigating Surfactant Selection in In Vitro Dissolution Testing: Mechanistic Insights and Practical Strategies.AAPS PharmSciTech · 2026Review
- The Impact of Polymers in Amorphous Solid Dispersion on the Bioavailability of Sulfonylureas and Meglitinides.Drug design, development and therapy · 2026Review
- Continuous Processing Strategies for Amorphous Solid Dispersions of Itraconazole: Impact of Polymer Selection and Manufacturing Techniques.Pharmaceutics · 2025Article
- Surfactant-Enabled Nanocarriers in Breast Cancer Therapy: Targeted Delivery and Multidrug Resistance Reversal.Pharmaceutics · 2025Review
- Mechanistic Insights into Amorphous Solid Dispersions: Bridging Theory and Practice in Drug Delivery.Pharmaceutical research · 2025Review
- Supersaturated Gel Formulation (SGF) of Atorvastatin at a Maximum Dose of 80 mg with Enhanced Solubility, Dissolution, and Physical Stability.Gels (Basel, Switzerland) · 2024Article
- Optimizing extrusion processes and understanding conformational changes in itraconazole amorphous solid dispersions using in-line UV-Vis spectroscopy and QbD principles.International journal of pharmaceutics: X · 2024Article
- Comparative analysis of drug-salt-polymer interactions by experiment and molecular simulation improves biopharmaceutical performance.Communications chemistry · 2023Article
- Ternary Solid Dispersions: A Review of the Preparation, Characterization, Mechanism of Drug Release, and Physical Stability.Pharmaceutics · 2023Review
- Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches.Molecules (Basel, Switzerland) · 2023Review
- Enteric Polymer-Based Amorphous Solid Dispersions Enhance Oral Absorption of the Weakly Basic Drug Nintedanib via Stabilization of Supersaturation.Pharmaceutics · 2022Article
- Characterizing the Physicochemical Properties of Two Weakly Basic Drugs and the Precipitates Obtained from Biorelevant Media.Pharmaceutics · 2022Article
- Improved Bioavailability of Poorly Water-Soluble Drug by Targeting Increased Absorption through Solubility Enhancement and Precipitation Inhibition.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Enhancing theDrug delivery · 2021Article
- Drug crystal growth in ternary amorphous solid dispersions: Effect of surfactants and polymeric matrix-carriers.International journal of pharmaceutics: X · 2021Article
- Exploring the Role of Surfactants in Enhancing Drug Release from Amorphous Solid Dispersions at Higher Drug Loadings.Pharmaceutics · 2021Article
- Improved Bioavailability and High Photostability of Methotrexate by Spray-Dried Surface-Attached Solid Dispersion with an Aqueous Medium.Pharmaceutics · 2021Article
- Supersaturable organic-inorganic hybrid matrix based on well-ordered mesoporous silica to improve the bioavailability of water insoluble drugs.Drug delivery · 2020Article
- Mechanisms of increased bioavailability through amorphous solid dispersions: a review.Drug delivery · 2020Review
- Multivariate Design of 3D Printed Immediate-Release Tablets with Liquid Crystal-Forming Drug-Itraconazole.Materials (Basel, Switzerland) · 2020Article
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The rapid release of poorly water-soluble drugs from amorphous solid dispersion (ASD) is often associated with the generation of supersaturated solution, which provides a strong driving force for precipitation and results in reduced absorption. Precipitation inhibitors, such as polymers and surfactants, are usually used to stabilize the supersaturated solution by blocking the way of kinetic or thermodynamic crystal growth. To evaluate the combined effect of polymers and surfactants on maintaining the supersaturated state of itraconazole (ITZ), various surfactants were integrated with enteric polymer hydroxypropyl methylcellulose acetate succinate (HPMC AS) to develop polymer⁻surfactant based solid dispersion. The supersaturation stability was investigated by in vitro supersaturation dissolution test and nucleation induction time measurement. Compared to the ASD prepared with HPMC AS alone, the addition of d-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) exhibited a synergistic effect on precipitation inhibition. The results indicated that the TPGS not only significantly reduced the degree of supersaturation which is the driving force for precipitation, but also provided steric hindrance to delay crystal growth by absorbing onto the surface of small particles. Subsequently, the formulations were evaluated in vivo in beagle dogs. Compared with commercial product Sporanox
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.