Entrapment of an EGFR inhibitor into nanostructured lipid carriers (NLC) improves its antitumor activity against human hepatocarcinoma cells

Autor: di gesu, R, Bondì, ML, Azzolina, A, Craparo, EF, Botto, C, Amore, E, Giammona, G, Cervello, M
Přispěvatelé: di gesu, R, Bondì, ML, Azzolina, A, Craparo, EF, Botto, C, Amore, E, Giammona, G, Cervello, M
Jazyk: angličtina
Rok vydání: 2014
Předmět:
Drug
Carcinoma
Hepatocellular
Hepatocellular carcinoma
media_common.quotation_subject
Biomedical Engineering
Medicine (miscellaneous)
Pharmaceutical Science
Antineoplastic Agents
Bioengineering
Pharmacology
Applied Microbiology and Biotechnology
Cell Line
Tumor
medicine
Humans
Epidermal growth factor receptor
Nanostructured lipid carriers
Tyrphostin AG-1478
Drug release
Hepatocellular carcinoma
EGFR inhibitor
media_common
EGFR inhibitors
Drug Carriers
Nanostructured lipid carriers
biology
Chemistry
Research
Liver Neoplasms
Correction
Drug release
Tyrphostins
medicine.disease
Lipids
Tyrphostin AG-1478
Molecular medicine
In vitro
Nanostructures
ErbB Receptors
EGFR inhibitor
Liver
Settore CHIM/09 - Farmaceutico Tecnologico Applicativo
Drug delivery
Quinazolines
biology.protein
Molecular Medicine
Drug carrier
Zdroj: Journal of nanobiotechnology 12 (2014): 21. doi:10.1186/1477-3155-12-21
info:cnr-pdr/source/autori:Bondi, Maria Luisa; Azzolina, Antonina; Craparo, Emanuela Fabiola; Botto, Chiara; Amore, Erika; Giammona, Gaetano; Cervello, Melchiorre/titolo:Entrapment of an EGFR inhibitor into nanostructured lipid carriers (NLC) improves its antitumor activity against human hepatocarcinoma cells/doi:10.1186%2F1477-3155-12-21/rivista:Journal of nanobiotechnology/anno:2014/pagina_da:21/pagina_a:/intervallo_pagine:21/volume:12
Journal of Nanobiotechnology
DOI: 10.1186/1477-3155-12-21
Popis: Background: In hepatocellular carcinoma (HCC), different signaling pathways are de-regulated, and among them, the expression of the epidermal growth factor receptor (EGFR). Tyrphostin AG-1478 is a lipophilic low molecular weight inhibitor of EGFR, preferentially acting on liver tumor cells. In order to overcome its poor drug solubility and thus improving its anticancer activity, it was entrapped into nanostructured lipid carriers (NLC) by using safe ingredients for parenteral delivery. Results: Nanostructured lipid carriers (NLC) carrying tyrphostin AG-1478 were prepared by using the nanoprecipitation method and different matrix compositions. The best system in terms of mean size, PDI, zeta potential, drug loading and release profile was chosen to evaluate the anti-proliferative effect of drug-loaded NLC versus free drug on human hepatocellular carcinoma HA22T/VGH cells. Conclusions: Thanks to the entrapment into NLC systems, tyrphostin AG-1478 shows an enhanced in vitro anti-tumor activity compared to free drug. These finding raises hope of future drug delivery strategy of tyrphostin AG-1478 -loaded NLC targeted to the liver for the HCC treatment.
Databáze: OpenAIRE
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