Targeting delivery of oxaliplatin with smart PEG-modified PAMAM G4 to colorectal cell line: In vitro studies

[Display omitted] •Surface modified and functionalized polymeric nano-complex was prepared for biocompatible targeted delivery of oxaliplatin.•Prepared nano-complex showed significant in vitro the controlled release of oxaliplatin in different pHs.•The folic acid tagging to the nanoparticle resulted in enhanced cellular uptake in the cancer cells.•The nano-complex was showed the excellent inhibitory effect on cancer cells. In this research, the anti-cancer efficacy of oxaliplatin (OX) was modulated using a nanocarrier system with enhanced targeting efficacy towards folic acid receptors (FAR) expressing colorectal cancer cells. Oxaliplatin was loaded into polyamidoamine dendrimers G4 (PAMAM) imprinted with polyethylene glycol (PEG) and folic acid (FA). The nano-complexes were characterized by FT-IR, 1H NMR, DSC, TGA, SEM, TEM, DLS and Zeta potential analyzer. Drug loading efficiency (34%) and in vitro drug release studies of PEG-PAMAM-FA-OX nano-complex showed higher drug release at acidic pH. Furthermore, in vitro investigation of nano-complex was carried out using cellular uptake (84.67 ± 1.98% for colorectal cancer cell line), MTT assay, flow cytometry assay and acridine orange staining, to ascertain the cell internalization efficiency, cell viability, apoptotic phase and morphology of dead cell, respectively. Less value of cell viability (18.39 ± 1.91%) and more value of late apoptotic phase (81.8%) were obtained for PEG-PAMAM-FA-OX nano-complex as a final synthetic system.