Enhanced anticancer activity of (–)-epigallocatechin-3-gallate (EGCG) encapsulated NPs toward colon cancer cell lines

(–)-Epigallocatechin-3-gallate (EGCG), a bioactive polyphenol of green tea has chemo- preventive effects against various cancer cells. Nanoparticles (NPs) carrying different ligands are able to specifically interact with their receptors on different cancer cells can provide effective release of cytotoxic drugs. In the present study we have prepared EGCG entrapped nanoparticles using PLGA (poly lactide-co-glycolide). PEG (poly ethylene glycol) and Folic acid (FA) via double emulsion solvent evaporation (DESE) method and the prepared PLGA-EGCG (P-E), PLGA-PEG-EGCG (PP-E) and PLGA-PEG-FA-EGCG (PPF-E) Nanoformulations had been characterized with 1H NMR and FT-IR techniques, AFM, DLS. PPF-E NPs showed an average size of 220nm. Analysis of Zeta potential confirmed the stability of NPs. HCT 116, HT-29, HCT-15, and HEK 293 cells were treated with both the prepared NPs and free EGCG (0-140μM). Result showed PPF-E NPs had improved delivery, uptake and cell cytotoxicity towards in Human folic acid receptor- positive (FR+) colorectal cancer cells (CRCs) as mainly on HCT116 compared to HT-29, but not on the folic acid - negative cells (FR -) as HCT-15. PPF-E NPs enhanced intracellular reactive oxygen species (ROS) level in absence of NAC (N-acetyl-l-cysteine), elevated DNA fragmentation level, and increased apoptotic cell death at higher doses compared to other two NPs and free EGCG. In conclusion PPF-E NPs exerted greater efficacy than PP-E, P-E and free EGCG in HCT 116 cells.