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Formulation and Evaluation of Lipid/Soluplus-Stabilized Nanocrystals of Paclitaxel and Bosutinib for a Synergistic
Manish Kumar1,2, Pooja Goswami3, Abhishek Jha1,4
1Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (BHU), Varanasi 221005, Uttar Pradesh, India.
Abstract:
Tyrosine kinase inhibitors have been employed for the treatment of lung cancer, owing to their role in regulating irregulated pathways or mutated genes. Bosutinib, a nonreceptor tyrosine kinase, has been recently investigated for lung cancer treatment. Bosutinib can also be used with paclitaxel as a combinatorial approach to receive a synergistic effect for the effective management of lung cancer. Furthermore, the nanocrystals of each can also be prepared and in combination can produce a more pronounced impact than the drug combination. Herein, the prepared Soluplus/lipid-stabilized nanocrystals of paclitaxel and bosutinib were rod to cubic in shape of about 150-250 nm. The nanocrystals were stable, provided controlled drug release, and exhibited a higher aerosolization performance. The nanocrystal combination demonstrated higher anticancer activity than the drug combination synergy against A549 cancer cells. The nanocrystals increased the level of cellular internalization in cancer cells, thereby inducing higher ROS generation and apoptosis of cancer cells. Furthermore, the lipid/Soluplus-stabilized nanocrystals exhibited higher translocation potential compared with only Soluplus-stabilized nanocrystals. The nanocrystals administered intratracheally showed a lower drug distribution to other organs, with prolonged drug retention in the lungs, suggesting the higher efficacy of developed nanocrystals in targeting the lungs. In conclusion, lipid-modified nanocrystals can be a novel approach for the effective management of lung cancer.
Insights
Lipid-modified nanocrystals of paclitaxel and bosutinib show enhanced lung cancer treatment efficacy. This approach improves drug delivery, increases cancer cell death, and targets the lungs effectively.
Area of Science:
- Nanomedicine
- Cancer Therapeutics
- Drug Delivery Systems
Background:
- Tyrosine kinase inhibitors (TKIs) like bosutinib are crucial for treating lung cancer by targeting mutated genes.
- Combinatorial therapy with paclitaxel and bosutinib offers synergistic effects for lung cancer management.
- Nanocrystal formulations can enhance drug efficacy and delivery compared to traditional drug combinations.
Purpose of the Study:
- To develop and evaluate Soluplus/lipid-stabilized nanocrystals of paclitaxel and bosutinib for lung cancer treatment.
- To assess the synergistic effects, drug release, aerosolization, and anticancer activity of the nanocrystal combination.
- To investigate the cellular internalization, ROS generation, apoptosis induction, and lung-targeting potential of the developed nanocrystals.
Main Methods:
- Preparation of Soluplus/lipid-stabilized nanocrystals of paclitaxel and bosutinib (150-250 nm).
- Evaluation of nanocrystal stability, controlled drug release, and aerosolization performance.
- In vitro assessment of anticancer activity against A549 lung cancer cells, including cellular internalization, ROS generation, and apoptosis.
- In vivo evaluation of lung targeting and biodistribution after intratracheal administration.
Main Results:
- The nanocrystals exhibited stability, controlled release, and superior aerosolization performance.
- The nanocrystal combination demonstrated significantly higher anticancer activity against A549 cells than the drug combination.
- Nanocrystals enhanced cellular uptake, leading to increased ROS generation and apoptosis.
- Lipid-modified nanocrystals showed improved translocation and lung-specific delivery with prolonged retention, reducing off-target organ distribution.
Conclusions:
- Lipid-modified nanocrystals represent a promising strategy for enhanced lung cancer therapy.
- This approach offers improved drug efficacy, targeted lung delivery, and reduced systemic toxicity.
- The developed nanocrystal formulation provides a novel and effective method for managing lung cancer.
