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Parameters that determine dissolution and efficacy of itraconazole and its relevance to recalcitrant dermatophytoses
Abstract
INTRODUCTION: Recalcitrant dermatophytoses is on the rise. Though myriad factors contribute to recalcitrance including terbinafine resistance, itraconazole largely remains sensitive. However, there are increasing instances of patients not responding adequately to itraconazole despite low MICs, probably due to issues plaguing the pelletization process, resulting in suboptimal quality. Data on this topic was searched on pubmed using the search items: itraconazole, MIC, MFC, quality, assay, pharmacokinetics, pharmacodynamics, dermatophytoses, and recalcitrance. Areas covered: A detailed analysis of the manufacturing process of itraconazole with emphasis on pelletization and parameters affecting the dissolution and bioavailability is presented. Important formulation factors including drug-polymer ratio, polymer type, coating thickness, bead size, and number are discussed. Also covered is the rationale of dosimetry of itraconazole in dermatophytoses based on the skin pharmacokinetics and MIC of the organism. Expert opinion: The process of pelletization has multiple components aiming to achieve maximum dissolution of the drug. Variations in the process, pellet quality, number, and polymer determine absorption. Morphometric analysis of pellets is a simple method to quantify quality of the drug. Once the process has been standardized, dosimetry depends on the route of secretion and site of infection, accounting for the variation of doses from 100 mg to 400 mg/day.
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From Itraconazole as a repurposed anti-cancer agent: focusing on synthesis, mechanisms of action and therapeutic insights (2026) · cites this paper as [103]
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Cited by
Marzi, M., Ghasemian, A., Ghanbariasad, A., Nournia, E., & Zarenezhad, E. (2026) · RSC Advances · doi:10.1039/d5ra09799a
Metadata
- Authors
- Sardana, K., Khurana, A., & Gupta, A.
- Affiliations
- Atal Bihari Vajpayee Institute of Medical Sciences and Dr. Ram Manohar Lohia Hospital (IN)
- Corresponding author
- Sardana, Kabir
- Venue
- Expert Review of Clinical Pharmacology
- Publisher
- Informa UK Limited
- Published
- 2019-04-22
- Volume
- 12
- Issue
- 5
- Pages
- 443-452
- ISSN
- 1751-2433 (ISSN-L)
- 1751-2441
- OpenAlex
- W2933163054
- Cited by
- 28
- References
- 1
- Citations by year
- 2026: 2 · 2025: 2 · 2024: 5 · 2023: 9 · 2022: 1 · 2021: 4 · 2020: 2 · 2019: 3
- FWCI
- 0.37
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Expert Review of Clinical Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Dermatology › Nail Diseases and Treatments
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Keywords
- itraconazole, antifungal resistance, pelletization, drug dissolution, bioavailability, drug-polymer ratio, polymer coatings, coating thickness, bead size, morphometrics, skin pharmacokinetics, minimum inhibitory concentration, minimum fungicidal concentration, dosimetry, terbinafine resistance
- MeSH terms
- Antifungal Agents, Chemistry, Pharmaceutical, Drug Compounding, Humans, Microbial Sensitivity Tests, Polymers, Solubility, Tinea, Treatment Outcome, Itraconazole
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- The paper
- Sardana, K., Khurana, A., & Gupta, A. (2019). Parameters that determine dissolution and efficacy of itraconazole and its relevance to recalcitrant dermatophytoses. Expert Review of Clinical Pharmacology. https://doi.org/10.1080/17512433.2019.1604218
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.