Efficacy of Novel L-Carnitine/PEG6000-Modified Exemestane Loaded Protein Nanoparticles Against Pre-neoplastic Mammary Damage

The objective of the study was to formulate a novel protein nanocarrier system for efficient oral delivery of exemestane. The outcomes of this study are promising and offer hope for the future of pharmaceuticals, nanotechnology and oncology. Whey protein concentrate (WPC) was selected as a protein excipient and processed with a naturally occurring crosslinker. The effect of various independent variables (i.e. WPC concentrations, ethanol concentrations and genipin concentration) was observed on hydrodynamic size (HD), zeta potential (ZP) and entrapment efficiency (EE). The optimised nanoparticles were further surface-modified with PEG6000/L-carnitine and characterised for their efficacy against DMBA-induced mammary damage. The optimised nanoparticles (WExe) had HD 410.32 ± 37.01 nm, ZP − 21.53 ± 2.35 mV and EE 82.7 ± 7.23%. SEM image revealed a much smaller size of these nanoparticles and an increased size of surface-modified nanoparticles (Car-WExe) over WExe. The optimised nanoparticles followed the Higuchi model. The modified nanoparticles exhibited good cytotoxicity against MCF7 cell lines. The uptake of L-carnitine modified whey nanoparticles was higher than non-modified whey nanoparticles in MCF7 cells. In vivo studies confirmed better efficacy of nanoparticles (as determined via proliferation assessment through carmine staining, histopathological studies and oxidative stress parameters) against DMBA-induced pre-neoplastic mammary damage. In conclusion, whey nanoparticles were promising nanocarriers for the oral delivery of exemestane.