Quality by design empowered preparation of itraconazole albumin nanoparticles for prostate cancer
Abstract
The current advent explores the potential of itraconazole (ITR) in prostate cancer (PCa), by its incorporation into albumin nanoparticles (NP). ITR as a repurposed moiety has displayed tremendous potential in various cancers. However, poor aqueous solubility poses hurdles towards its clinical translation. Amorphisation of ITR was observed post-incorporation within NP matrix which could prevent its precipitation in aqueous media. ITR NP was developed using quality by design and multivariate analysis and evaluated for cellular uptake, cell proliferation inhibition and the mechanism of PCa cell inhibition. Time and concentration-dependent serum stability and hemolytic potential revealed safety of ITR NP. Morphological changes and nuclear staining studies revealed the efficacy of ITR and ITR NP in promoting growth inhibition of PC-3 cells. Superior qualitative and quantitative uptake, reactive oxygen species (ROS) and mitochondrial impairment for ITR NP in comparison with ITR and control group was observed. Cell cycle study revealed remarkable G2/M phase inhibition in PC-3 cells. ITR NP demonstrated superior anticancer potential in 3D tumoroids mimicking the micro-metastatic lesions compared to control and ITR. Hence, ITR NP can be a favorable alternative therapeutic alternative in PCa.
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ITR NP showed superior qualitative and quantitative absorption, ROS, and mitochondrial damage compared to ITR and control groups.
“Compared to the ITR and control groups, ITR NP showed superior qualitative and quantitative absorption, ROS, and mitochondrial damage.”
From Itraconazole as a repurposed anti-cancer agent: focusing on synthesis, mechanisms of action and therapeutic insights (2026) · cites this paper as [87]
ITR NP may be a good substitute treatment option for prostate cancer.
“ITR NP may therefore be a good substitute treatment option for PCa.87”
From Itraconazole as a repurposed anti-cancer agent: focusing on synthesis, mechanisms of action and therapeutic insights (2026) · cites this paper as [87]
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“Abraxane ® , comprising of 130-nm nano-sized paclitaxel loaded nanoparticles showed superior therapeutic efficacy with substantially reduced incidences of toxicity in randomized clinical trials for breast cancer and non-small cell lung cancer [10, 11].”
Itraconazole Inhibits the Growth of Cutaneous Squamous Cell Carcinoma by Targeting HMGCS1/ACSL4 Axis
Xu, C., Zhuo, Y., Liu, Y., & Chen, H. (2022) · Frontiers in Pharmacology · doi:10.3389/fphar.2022.828983 · Cited by 23 · see citing works
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Marzi, M., Ghasemian, A., Ghanbariasad, A., Nournia, E., & Zarenezhad, E. (2026) · RSC Advances · doi:10.1039/d5ra09799a
- Authors
- Shah, S., Famta, P., Sharma, A., Kumar, R., Pandey, G., Vambhurkar, G., Srinivasarao, D. A., Shinde, A., Prasad, S. B., Asthana, A., & Srivastava, S.
- Affiliations
- National Institute of Pharmaceutical Education and Research (IN)
- Corresponding author
- Srivastava, Saurabh
- Venue
- Drug Delivery and Translational Research
- Published
- 2024-05-02
- Volume
- 15
- Issue
- 1
- Pages
- 253-268
- ISSN
- 2190-393X (ISSN-L)
- 2190-3948
- OpenAlex
- W4396578391
- Cited by
- 12
- References
- 3
- Citations by year
- 2026: 6 · 2025: 5 · 2024: 1
- FWCI
- 1.13
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- Locations
- Drug Delivery and Translational Research (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- 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
- Keywords
- itraconazole, albumin nanoparticles, prostate cancer, drug repurposing, quality by design, amorphous drug, water solubility, PC-3 cells, reactive oxygen species, mitochondrial dysfunction, G2/M cell cycle arrest, serum stability, hemolysis, drug delivery
- MeSH terms
- PC-3 Cells, Albumins, Antineoplastic Agents, Humans, Male, Prostatic Neoplasms, Reactive Oxygen Species, Itraconazole, Cell Line, Tumor, Cell Proliferation, Nanoparticles
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