ArticlePharmaceutics2022
Simultaneous Improvement of Dissolution Behavior and Oral Bioavailability of Antifungal Miconazole via Cocrystal and Salt Formation.
Article in Pharmaceutics, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 33 citations in OpenAlex.
- From Chemistry to Clinic: Amorphous Solid-State Modification Strategies for Oral Azole Antifungals.ACS omega · 2026Review
- New Miconazole Salts with Heterocyclic Carboxylic Acids with Improved Water Solubility and Enhanced Antifungal Activity.Molecules (Basel, Switzerland) · 2026Article
- Enhancement of the Anti-Hepatoma Activity of Acacetin Through Salt Formation of Sodium Acacetin.Chemistry & biodiversity · 2026Article
- The Comparison of Mannitol Prepared with Different PVP: Crystal Form, Morphology, Functional Properties, andACS omega · 2026Article
- Electrospun PVP Nanofibrous Co-Loaded with Miconazole and Lidocaine for the Treatment of Oral Candidiasis.International journal of nanomedicine · 2026Article
- Ureasil-polyether hybrid polymer-based vaginal ovules for combination therapy in the treatment of vulvovaginal candidiasis.Drug delivery and translational research · 2025Article
- Novel Drug-Drug Cocrystalline Forms of Carbamazepine with Sulfacetamide: Preparation, Characterization, and In Vitro/In Vivo Performance Evaluation.Pharmaceutics · 2025Article
- Solubilization techniques used for poorly water-soluble drugs.Acta pharmaceutica Sinica. B · 2024Review
- Cocrystal Prediction of Nifedipine Based on the Graph Neural Network and Molecular Electrostatic Potential Surface.AAPS PharmSciTech · 2024Article
- The Fabrication, Drug Loading, and Release Behavior of Porous Mannitol.Molecules (Basel, Switzerland) · 2024Article
- Nanoparticles of Thiolated Xanthan Gum for the Oral Delivery of Miconazole Nitrate: In Vitro and In Vivo Evaluation.Pharmaceutics · 2024Article
- A triclinic polymorph of miconazole.Acta crystallographica. Section E, Crystallographic communications · 2024Article
- Modification of the Physicochemical Properties of Active Pharmaceutical Ingredients via Lyophilization.Pharmaceutics · 2023Review
- Article
- Cocrystal Prediction of Bexarotene by Graph Convolution Network and Bioavailability Improvement.Pharmaceutics · 2022Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Miconazole shows low oral bioavailability in humans due to poor aqueous solubility, although it has demonstrated various pharmacological activities such as antifungal, anti-tubercular and anti-tumor effects. Cocrystal/salt formation is one of the effective methods for solving this problem. In this study, different methods (liquid-assisted grinding, slurrying and lyophilization) were used to investigate their impact on the formation of the miconazole multicomponent crystals with succinic, maleic and dl-tartaric acids. The solid state of the prepared powder was characterized by differential scanning calorimetry, powder X-ray diffraction and scanning electron microscopy. It was found that lyophilization not only promotes partial amorphization of both salts but also allows obtaining a new polymorph of the miconazole salt with dl-tartaric acid. The lyophilized salts compared with the same samples prepared by two other methods showed better dissolution rates but low stability during the studies due to rapid recrystallization. Overall, it was determined that the preparation method of multicomponent crystals affects the solid-state characteristics and miconazole physicochemical properties significantly. The in vivo studies revealed that the miconazole multicomponent crystals indicated the higher peak blood concentration and area under the curve from 0 to 32 h values 2.4-, 2.9- and 4.6-fold higher than the pure drug. Therefore, this study demonstrated that multicomponent crystals are promising formulations for enhancing the oral bioavailability of poorly soluble compounds.
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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.