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Evaluating the efficacy of nintedanib-invasomes as a therapy for non-small cell lung cancer
Tamer M Mahmoud1, Mohamed Mahmoud AbdElrahman2, Mary Eskander Attia3
1Pharmaceutics and Industrial Pharmacy Department, Al-Manara College for Medical Sciences, Maysan 62010, Iraq.
Abstract:
Nintedanib (NDB) is a crucial tyrosine kinase inhibitor used in the treatment of non-small cell lung cancer (NSCLC). However, its oral administration results in limited uptake of NDB by the lungs, necessitating high and frequent dosages, which leads to severe systemic adverse effects and poor bioavailability. To address these issues, a nasal formulation of NDB-invasomes (NLI) was developed as a potential therapy for NSCLC, aiming to improve the sustainability, targeting, bioavailability, and efficacy of NDB. Utilizing design expert software, various formulations were created and optimized. Additionally, analyses were performed on the cytotoxicity, bioavailability, targeting, and toxicity of the optimized NLI formulation. The chosen formulation contained 1.723 % phospholipids, 1.5 % cineole, and 1 % ethanol. The optimized NLI formulation enhanced the sustainability and bioavailability of free NDB by 55 % and 7.93-fold, respectively. Targeting studies indicated that the NLI formulation could achieve a more localized accumulation of NDB in the lungs. Furthermore, the optimized NLI formulation demonstrated greater anticancer efficacy against A549 lung cancer cells than free NDB. Histopathological analysis of the lungs in the optimized NLI group revealed no signs of toxicity. These findings suggest that the nasal NLI formulation is a promising option for treatment of NSCLC.
Insights
A novel nasal formulation of Nintedanib-invasomes (NLI) significantly improves lung delivery and anticancer efficacy for non-small cell lung cancer (NSCLC). This nasal NLI approach enhances bioavailability and targets lung tissue, reducing systemic side effects.
Area of Science:
- Pharmaceutical Sciences
- Oncology
- Drug Delivery Systems
Background:
- Nintedanib (NDB), a tyrosine kinase inhibitor, is vital for non-small cell lung cancer (NSCLC) treatment.
- Oral NDB exhibits poor lung bioavailability and significant systemic toxicity due to limited lung uptake.
- Developing alternative delivery methods is crucial to enhance NDB efficacy and patient outcomes.
Purpose of the Study:
- To develop and optimize a nasal Nintedanib-invasome (NLI) formulation for improved NSCLC therapy.
- To evaluate the enhanced sustainability, lung targeting, bioavailability, and efficacy of the NLI formulation.
- To assess the safety profile of the nasal NLI formulation.
Main Methods:
- Formulation optimization using design expert software with varying concentrations of phospholipids, cineole, and ethanol.
- In vitro and in vivo assessments of NLI formulation including cytotoxicity, bioavailability, lung targeting, and anticancer efficacy.
- Histopathological analysis to evaluate lung toxicity.
Main Results:
- The optimized NLI formulation (1.723% phospholipids, 1.5% cineole, 1% ethanol) significantly improved NDB sustainability by 55% and bioavailability by 7.93-fold.
- Targeting studies confirmed localized NDB accumulation in the lungs.
- NLI demonstrated superior anticancer efficacy against A549 lung cancer cells compared to free NDB.
- Histopathological examination showed no lung toxicity in the NLI group.
Conclusions:
- Nasal Nintedanib-invasomes (NLI) represent a promising strategy for enhancing NSCLC treatment.
- The NLI formulation improves NDB bioavailability, lung targeting, and therapeutic efficacy while maintaining a favorable safety profile.
- This nasal delivery system offers a potential alternative to oral administration for improved NSCLC management.
