EGFR targeted delivery of paclitaxel and parthenolide co-loaded in PEG-Phospholipid micelles enhance cytotoxicity and cellular uptake in non-small cell lung cancer cells

The objective of this study was to formulate, characterize and evaluate the biological efficacy of EGF-conjugated mixed micelles of PEG(2000)-DSPE and vitamin E-TPGS loaded with paclitaxel and parthenolide against paclitaxel resistant and sensitive NSCLC cell lines. Micelles were prepared by the film casting method and characterized for particle size, encapsulation efficiency, zeta potential, and EGF binding efficiency onto the micellar surface. The encapsulation efficiency of paclitaxel and parthenolide was 97 +/- 3% and 95 +/- 3%, respectively with average particle size of 15 +/- 3 nm and zeta potential of -34 my. Binding efficiency of EGF to micelles was about 60%. The cell viability studies showed that EGF targeted micelles were more effective in cancer cell killing than non-targeted micelles. Cellular uptake study revealed that EGF-targeted micelles afford higher intracellular delivery of paclitaxel as compared to non targeted micelles in both resistant and sensitive cell lines. Confocal microscopy confirmed the efficacy of EGF-targeted micelles in delivering higher payloads of drugs to the cells:In conclusion, this study demonstrated that the EGF micelles have the potential to be further pursued as a versatile nanotechnology platform for targeted delivery of a wide range of chemotherapeutic agents as a combination therapy for the treatment of EGFR-over expressing cancers. (C) 2016 Elsevier B.V. All rights reserved.