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. 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 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.

Total Structural Elucidation of Erlotinib and Gefitinib by Mainly 2D-Rotating Frame Overhauser Effect Spectroscopy (2D ROESY NMR)

“…It seems to be there is a mess about the previously published NMR data of Erlotinib and its HCl salt [6][7][8][9][10][11][12][13][14][15][16][17][18][19] . There are several reasons for this confusion.…”

“…Silver stabilize deuterated CDCl 3 causes to yellow coloured precipitate, probably the reason of the reaction between the Ag and acetylene group, that is why, it cannot be used. Highly different melting points and colors are reported in lit [6][7][8][9][10][11][12][13][14][15][16][17][18][19] . Actually pure Erlotinib sample must be white.…”

“…Yellow coloured samples should have some impurities. As a matter of course, highly different 1 H and 13 C NMR spectra (in DMSO-d 6 ) of Erlotinib HCl have been reported in literature [6][7][8][9][10][11][12][13][14][15][16] . Our 1 H NMR results are totally in agreement with literature [6][7][8][9][10][11] .…”

Overexpression of EGFR Protein in Bruneian Lung Cancer Patients

“…Gefitinib and Erlotinib are two drugs used for the treatment of advanced NSCLC. The mode of action of these two drugs is based on their capability to inhibit the tyrosine kinase activity of EGFR by competing with ATP for the ATP-binding site (Barghi et al, 2014;Han et al, 2015;Hsieh et al 2015). Recently published study developed a nanosized polymeric delivery system for the drug "Erlotinib" (Barghi et al, 2014).…”

Design, Development and Evaluation of Erlotinib-Loaded Hybrid Nanoparticles for Targeted Drug Delivery to NonSmall Cell Lung Cancer

“…ETB loaded polymeric NPs in mice has shown improved efficacy and reduced toxicities associated with the drug (223). Another study revealed polymeric NPs improved antitumor efficacy of ETB in A549 human lung adenocarcinoma cells (224). Formulation of reverse micelles containing ETB showed improved in vitro efficacy of ETB in pancreatic cancer cells (225).…”