title: Synthesis, characterization and in vitro anti-tumoral evaluation of Erlotinib-PCEC nanoparticles.
abstract: BACKGROUND
  Development of a nanosized polymeric delivery system for erlotinib was the main objective of this research.
  
  
  METHODS
  Poly caprolactone-polyethylene glycol-polycaprolactone (PCEC) copolymers with different compositions were synthesized via ring opening polymerization. Formation of triblock copolymers was confirmed by HNMR as well as FT-IR. Erlotinib loaded nanoparticles were prepared by means of synthesized copolymers with solvent displacement method.
  
  
  RESULTS
  Physicochemical properties of obtained polymeric nanoparticles were dependent on composition of used copolymers. Size of particles was decreased with decreasing the PCL/PEG molar ratio in used copolymers. Encapsulation efficiency of prepared formulations was declined by decreasing their particle size. Drug release behavior from the prepared nanoparticles exhibited a sustained pattern without a burst release. From the release profiles, it can be found that erlotinib release rate from polymeric nanoparticles is decreased by increase of CL/PEG molar ratio of prepared block copolymers. Based on MTT assay results, cell growth inhibition of erlotinib has a dose and time dependent pattern. After 72 hours of exposure, the 50% inhibitory concentration (IC50) of erlotinib hydrochloride was appeared to be 14.8 μM.
  
  
  CONCLUSIONS
  From the obtained results, it can be concluded that the prepared PCEC nanoparticles in this study might have the potential to be considered as delivery system for erlotinib.
authors.affiliation: Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran E-mail : valizadeh@tbzmed.ac.ir, valizadehh@gmail.com.
authors.forename: Leila
authors.initials: L
authors.lastname: Barghi
authors.forename: Davoud
authors.initials: D
authors.lastname: Asgari
authors.forename: Jaleh
authors.initials: J
authors.lastname: Barar
authors.forename: Aylar
authors.initials: A
authors.lastname: Nakhlband
authors.forename: Hadi
authors.initials: H
authors.lastname: Valizadeh
mesh_terms: D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D066246:ErbB Receptors / Q000037:antagonists & inhibitors; D000069347:Erlotinib Hydrochloride; D005027:Ethylene Oxide / Q000138:chemical synthesis*; D006801:Humans; D066298:In Vitro Techniques; D007783:Lactones / Q000138:chemical synthesis*; D053758:Nanoparticles; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D066244:Proton Magnetic Resonance Spectroscopy; D011799:Quinazolines / Q000494:pharmacology*; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D007783:Lactones; C400421:PLC(20)-b-PEO(44); D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D000069347:Erlotinib Hydrochloride; D066246:ErbB Receptors; D005027:Ethylene Oxide