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Repurposing Itraconazole Loaded PLGA Nanoparticles for Improved Antitumor Efficacy in Non-Small Cell Lung Cancers
1Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Abstract:
Itraconazole (ITR) is a broad-spectrum antifungal drug, which has been shown to possess some promising anticancer, anti-proliferative, and anti-angiogenic properties in some cancers, such as cancers of the lung, breast, and skin. However, ITR has some drawbacks, such as poor water solubility, which hinder its use as a therapeutic agent. Therefore, in the present study, we developed and characterized chitosan-coated PLGA nanoparticles of itraconazole and studied their anticancer activities in H1299 lung cancer cells. The prepared ITR nanoparticles showed a small particle size, narrow poly dispersity index (PDI), positive zeta potential, and a controlled drug release profile. The cytotoxicity of ITR nanoparticles (NPs) on H1299 cancer cells after 24 h of exposure was greater than that of the ITR solution. Apoptosis of cancer cells exposed to ITR nanoparticles was also enhanced in comparison with the ITR solution. At the molecular level, ITR NPs were more effective than ITR solution in inducing pro-apoptotic Bax and p53 while reducing anti-apoptotic Bcl2 protein expression. ITR NPs were more effective than ITR solution in arresting cells both at the G0/G1 as well as G2/M phases of the cell cycle. Hence, repurposing itraconazole by encapsulation into PLGA NPs with chitosan coating is a potentially promising approach to treat lung cancers.
Insights
Chitosan-coated nanoparticles effectively delivered itraconazole (ITR), enhancing its anticancer effects against lung cancer cells. This formulation improved drug solubility and increased cancer cell death and apoptosis.
Area of Science:
- Pharmacology
- Nanotechnology
- Oncology
Background:
- Itraconazole (ITR) exhibits anticancer properties but suffers from poor water solubility, limiting its therapeutic application.
- Lung cancer remains a significant global health challenge, necessitating novel treatment strategies.
Purpose of the Study:
- To develop and characterize chitosan-coated poly(lactic-co-glycolic acid) (PLGA) nanoparticles encapsulating itraconazole (ITR NPs).
- To evaluate the in vitro anticancer efficacy of ITR NPs in H1299 lung cancer cells.
Main Methods:
- Formulation and characterization of chitosan-coated PLGA nanoparticles loaded with itraconazole.
- Assessment of nanoparticle properties including particle size, polydispersity index (PDI), and zeta potential.
- In vitro evaluation of cytotoxicity, apoptosis induction, and cell cycle arrest in H1299 lung cancer cells exposed to ITR NPs and ITR solution.
Main Results:
- ITR NPs exhibited optimal physicochemical properties: small particle size, narrow PDI, positive zeta potential, and controlled drug release.
- ITR NPs demonstrated significantly enhanced cytotoxicity and apoptosis induction in H1299 cells compared to free ITR solution.
- Molecular analysis revealed ITR NPs effectively modulated pro-apoptotic (Bax, p53) and anti-apoptotic (Bcl2) proteins and induced cell cycle arrest at G0/G1 and G2/M phases.
Conclusions:
- Chitosan coating of PLGA nanoparticles improves itraconazole's solubility and delivery for lung cancer treatment.
- Repurposing itraconazole via nanoparticle encapsulation presents a promising strategy to enhance its anticancer efficacy against lung cancer.
