Erlotinib-Loaded Poly(ε-Caprolactone) Nanocapsules Improve In Vitro Cytotoxicity and Anticlonogenic Effects on Human A549 Lung Cancer Cells

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 (NC ELB ) and evaluated their in vitro cytotoxicity in A549 cells. The formulation was characterized in re...

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Veröffentlicht in:AAPS PharmSciTech 2020-08, Vol.21 (6), p.229-229, Article 229
Hauptverfasser: Bruinsmann, Franciele Aline, Buss, Julieti Huch, Souto, Gabriele Dadalt, Schultze, Eduarda, de Cristo Soares Alves, Aline, Seixas, Fabiana Kömmling, Collares, Tiago Veiras, Pohlmann, Adriana Raffin, Guterres, Silvia Stanisçuaski
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container_end_page 229
container_issue 6
container_start_page 229
container_title AAPS PharmSciTech
container_volume 21
creator Bruinsmann, Franciele Aline
Buss, Julieti Huch
Souto, Gabriele Dadalt
Schultze, Eduarda
de Cristo Soares Alves, Aline
Seixas, Fabiana Kömmling
Collares, Tiago Veiras
Pohlmann, Adriana Raffin
Guterres, Silvia Stanisçuaski
description 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 (NC ELB ) 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). NC ELB 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 NC ELB was the induction of apoptosis in A549 cells. Further, a significant decrease in A549 colony formation was verified after NC ELB 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.
doi_str_mv 10.1208/s12249-020-01723-y
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subjects Biochemistry
Biomedical and Life Sciences
Biomedicine
Biotechnology
Pharmacology/Toxicology
Pharmacy
Research Article
title Erlotinib-Loaded Poly(ε-Caprolactone) Nanocapsules Improve In Vitro Cytotoxicity and Anticlonogenic Effects on Human A549 Lung Cancer Cells
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