title: Entrapment of an EGFR inhibitor into nanostructured lipid carriers (NLC) improves its antitumor activity against human hepatocarcinoma cells.
abstract: 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.
authors.affiliation: Istituto per lo Studio dei Materiali Nanostrutturati, U,O,S, Palermo, Consiglio Nazionale delle Ricerche, Via Ugo la Malfa 153, Palermo 90146, Italy. marialuisa.bondi@ismn.cnr.it.
authors.forename: Maria Luisa
authors.initials: ML
authors.lastname: Bondì
authors.forename: Antonina
authors.initials: A
authors.lastname: Azzolina
authors.forename: Emanuela Fabiola
authors.initials: EF
authors.lastname: Craparo
authors.forename: Chiara
authors.initials: C
authors.lastname: Botto
authors.forename: Erika
authors.initials: E
authors.lastname: Amore
authors.forename: Gaetano
authors.initials: G
authors.lastname: Giammona
authors.forename: Melchiorre
authors.initials: M
authors.lastname: Cervello
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D006801:Humans; D008055:Lipids / Q000737:chemistry; D008099:Liver / Q000187:drug effects / Q000473:pathology; D008113:Liver Neoplasms / Q000188:drug therapy* / Q000473:pathology; D049329:Nanostructures / Q000737:chemistry*; D011799:Quinazolines / Q000008:administration & dosage* / Q000494:pharmacology; D020032:Tyrphostins / Q000008:administration & dosage* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008055:Lipids; D011799:Quinazolines; D020032:Tyrphostins; C101044:RTKI cpd; D066246:ErbB Receptors