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Synthesis, Characterization and in vitro Anti-Tumoral Evaluation of Erlotinib-PCEC Nanoparticles

  • Barghi, Leila (Faculty of Pharmacy, Tabriz University of Medical Sciences) ;
  • Asgari, Davoud (Faculty of Pharmacy, Tabriz University of Medical Sciences) ;
  • Barar, Jaleh (Faculty of Pharmacy, Tabriz University of Medical Sciences) ;
  • Nakhlband, Aylar (Research Center for Pharmaceutical Nanotechnology, Tabriz University of Medical Sciences) ;
  • Valizadeh, Hadi (Faculty of Pharmacy, Tabriz University of Medical Sciences)
  • Published : 2015.01.06

Abstract

Background: Development of a nanosized polymeric delivery system for erlotinib was the main objective of this research. Materials and 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 $14.8{\mu}M$. 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.

Keywords

Erlotinib;PCEC;solvent displacement method;nanoparticles

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