Erlotinib-Loaded Poly(ε-Caprolactone) Nanocapsules Improve In Vitro Cytotoxicity and Anticlonogenic Effects on Human A549 Lung Cancer Cells.
Franciele Aline BruinsmannJulieti Huch BussGabriele Dadalt SoutoEduarda SchultzeAline de Cristo Soares AlvesFabiana Kömmling SeixasTiago Veiras CollaresAdriana Raffin PohlmannSilvia Stanisçuaski GuterresPublished in: AAPS PharmSciTech (2020)
Lung cancer is the most frequent type of cancer and the leading cause of cancer-related mortality worldwide. This study aimed to develop erlotinib (ELB)-loaded poly(ε-caprolactone) nanocapsules (NCELB) and evaluated their in vitro cytotoxicity in A549 cells. The formulation was characterized in relation to hydrodynamic diameter (171 nm), polydispersity index (0.076), zeta potential (- 8 mV), drug content (0.5 mg.mL-1), encapsulation efficiency (99%), and pH (6.0). NCELB presented higher cytotoxicity than ELB in solution against A549 cells in the MTT and LIVE/DEAD cell viability assays after 24 h of treatment. The main mechanism of cytotoxicity of NCELB was the induction of apoptosis in A549 cells. Further, a significant decrease in A549 colony formation was verified after NCELB treatment in comparison with the unencapsulated drug treatment. The reduction in clonogenic capacity is very relevant as it can reduce the risk of tumor recurrence and metastasis. In conclusion, erlotinib-loaded PCL nanocapsules are promising nanoparticles carriers to increase the efficacy of ELB in lung cancer treatment.
Keyphrases
- cell cycle arrest
- induced apoptosis
- drug delivery
- endoplasmic reticulum stress
- oxidative stress
- type diabetes
- endothelial cells
- advanced non small cell lung cancer
- epidermal growth factor receptor
- cardiovascular disease
- signaling pathway
- risk assessment
- papillary thyroid
- cardiovascular events
- cell proliferation
- single cell
- optic nerve
- electronic health record