Co-administration with cell penetrating peptide enhances the oral bioavailability of docetaxel-loaded nanoparticles

This study proposes a novel docetaxel (DTX) cyclodextrin inclusion-loaded poly (lactic-co-glycolic acid) (PLGA) nanoparticles (D-CNPs) system with cell penetrating peptide (CPP), and evaluates its potential for oral administration of DTX. Heptaarginine (R₇) was used as the CPP. D-CNPs were prepared by the double-emulsification method. The mean particle size and zeta potential of the resulting D-CNPs were 198.7?±?12.56?nm and??27.25?±?4.62?mV, respectively, and their mean encapsulation efficiency and drug loading were 80.35?±?6.37% and 1.02?±?0.15%, respectively. The morphology of the D-CNPs was observed by scanning electron microscope (SEM) and transmission electron microscope (TEM). The release behavior of the D-CNPs was studied by using the dialysis method. The relative bioavailability of D-CNPs and D-CNPs co-administered with R₇ was enhanced about 5.57- and 9.43-fold, respectively, compared with the free DTX suspension. Furthermore, D-CNPs with R₇ displayed maximum cytotoxicity against MCF-7 cells in MTT assay. D-CNPs co-administered with R₇ showed markedly higher fluorescence intensity than D-CNPs without CPP. The results suggest that the D-CNPs co-administered with R₇ could be a potential delivery system with excellent therapeutic efficacy for targeting the drugs to cancer cells.