Construction of esterase-responsive hyperbranched polyprodrug micelles and their antitumor activity <i>in vitro</i>

Abstract This research constructs an esterase-responsive hyperbranched polyprodrug nano pharmaceutical and investigates their antitumor activity. Polyprodrug micelle was prepared by one-pot method based on glutathione (GSH), doxorubicin (DOX), polyethylene glycol (PEG) under the catalyst of N , -dicyclohexylcarbodiimide (DCC), 4-dimethylaminopyridine (DMAP), 1-hydroxybenzotriazole (HOBt). The characterized nuclear magnetic resonance (NMR), Fourier transform infrared spectrometer (FT-IR), ultraviolet-visible spectrophotometer (UV-Vis), dynamic light scattering (DLS), transmission electron microscope (TEM), respectively. activity evaluated Hela cell distributions micelles in cells were observed fluorescent microscope. NMR FT-IR confirmed that DOX-GSH-PEG successfully synthesized. drug loading rate is 10.21% particle size 106.4 ± 1 nm with a narrowed polydispersity (PDI = 0.145). DLS showed stable during 7 days at 25°C. release results could be disrupted, reach 43% 72 h. Cell uptake viability demonstrated distribute to nuclei 8 h induce apoptosis 48 Overall, these disrupted drugs high esterase environment for cancer therapy vitro . These confirm effective nanomedicine endogenous-based strategy synthesis construct would probably preferred choice future.