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


Background: Development of a nanosized polymeric delivery system for erlotinib was the main objectiveof this research. Materials and
Methods: Poly caprolactone-polyethylene glycol-polycaprolactone (PCEC)copolymers with different compositions were synthesized via ring opening polymerization. Formation of triblockcopolymers was confirmed by HNMR as well as FT-IR. Erlotinib loaded nanoparticles were prepared by meansof synthesized copolymers with solvent displacement method.
Results: Physicochemical properties of obtainedpolymeric nanoparticles were dependent on composition of used copolymers. Size of particles was decreased withdecreasing the PCL/PEG molar ratio in used copolymers. Encapsulation efficiency of prepared formulationswas declined by decreasing their particle size. Drug release behavior from the prepared nanoparticles exhibiteda sustained pattern without a burst release. From the release profiles, it can be found that erlotinib release ratefrom 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 72hours of exposure, the 50% inhibitory concentration (IC50) of erlotinib hydrochloride was appeared to be 14.8μM.
Conclusions: From the obtained results, it can be concluded that the prepared PCEC nanoparticles in thisstudy might have the potential to be considered as delivery system for erlotinib.