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Floating drug delivery system of itraconazole: Formulation, in vitro and in vivo studies
Abstract
Abstract A multiple unit oral floating drug delivery system of itraconazole was developed to prolong gastric residence time, target stomach mucosa and increase drug bioavailability. To prepare non-effervescent floating microspheres/beads, ionotropic gelation method was used. Since the solubility of itraconazole is low at pH 1.2, it was attempted to increase the solubility by preparing inclusion complexes using randomly methylated beta-cyclodextrin and with polyvinylpyrrolidone cross linked and starch. In this study, the effects of formulation parameters like, concentration and types of polymer, crosslinking agent and the excipients, the floating ability, surface characteristics and drug release profiles were investigated. Optimum formulation (NG17) was used for Caco-2 cell culture studies. In permeability studies, at pH 5, 6 and 7.4, the formulation NG17 at pH 5, which is the pH of the proximal region of small intestine (absorption window of itraconazole), showed the highest permeability value which is 5.88 × 10−6 cm/s. NG17 was also used for in vivo imaging studies. It was conducted in rabbits by using gamma scintigraphy and obtained that NG17 floated for 6.5 h in the stomach. As a result, it was found that, with non-effervescent floating bead formulations, the bioavailability of itraconazole can be improved.
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“However, there are various drug delivery approaches such as cyclodextrin complexes (increasing stability and solubility), pH-sensitive formulations (for oral delivery), targeted delivery systems, intravenous formulations and lipid-based formulations to increase ITZ efficacy.106–108”
From Itraconazole as a repurposed anti-cancer agent: focusing on synthesis, mechanisms of action and therapeutic insights (2026) · cites this paper as [106]
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References 42 · Cited by 34
Research works printed but not linked: 2
- Türkmen, 2017, A new approach to enhance bioavailability: dosage forms with extended residence time in the stomach, FABAD J. Pharm. Sci., 42, 29
- Gökbulut, 2017, Enhancement of solubility of itraconazole by complexation with ß cyclodextrin derivatives, FABAD J. Pharm. Sci., 42, 1
Metadata
- Authors
- Gökbulut, E., Vural, İ., Aşıkoğlu, M., & Özdemir, N.
- Affiliations
- Hacettepe University (TR)
- Ege University (TR)
- Ankara University (TR)
- Corresponding author
- Özdemir, Nurten
- Venue
- Journal of Drug Delivery Science and Technology
- Publisher
- Elsevier BV
- Published
- 2019-02
- Volume
- 49
- Pages
- 491-501
- ISSN
- 1773-2247 (ISSN-L)
- OpenAlex
- W2905838151
- Cited by
- 34
- References
- 42
- Citations by year
- 2026: 2 · 2025: 3 · 2024: 3 · 2023: 5 · 2022: 9 · 2021: 4 · 2020: 4 · 2019: 4
- FWCI
- 1.41
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- www.elsevier.com/tdm/userlicense/1.0/ (tdm)
- www.elsevier.com/legal/tdmrep-license (tdm)
- Locations
- Journal of Drug Delivery Science and Technology (publishedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Inhalation and Respiratory Drug Delivery
- Keywords
- itraconazole, floating drug delivery systems, ionic gelation, β-cyclodextrin inclusion complex, polyvinylpyrrolidone, starch, gastric residence time, drug solubility enhancement, Caco-2 permeability, bioavailability, scintigraphy, antifungal formulation
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- CoChat. (2026). Citation check: Floating drug delivery system of itraconazole: Formulation, in vitro and in vivo studies. https://app.cochat.ai/papers/10.1016/j.jddst.2018.12.019
- The paper
- Gökbulut, E., Vural, İ., Aşıkoğlu, M., & Özdemir, N. (2019). Floating drug delivery system of itraconazole: Formulation, in vitro and in vivo studies. Journal of Drug Delivery Science and Technology. https://doi.org/10.1016/j.jddst.2018.12.019
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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.
