Raloxifene (RXF) is a hormone-like medication used for treating postmenopausal\nosteoporosis and estrogen-dependent breast cancer, yet associated with bad low bioavailability\ndue to poor solubility. This study was intended to develop cyclodextrin/chitosan nanoparticles\n(ccNPs) for oral delivery of RXF in order to enhance the oral bioavailability. RXF-loaded ccNPs\n(RXF-ccNPs) were prepared by cyclodextrin inclusion followed by complexation with chitosan.\nRXF-ccNPs were fully characterized by particle size, morphology and in vitro drug release. The oral\ndelivery efficacy and transepithelial transport potential were evaluated by pharmacokinetics, in\nsitu single-pass intestinal perfusion, cellular uptake and ex vivo imaging. The resulting RXF-ccNPs\nwere around 165 nm in particle size with a narrow distribution. The oral bioavailability of RXF\nwas enhanced by 2.6 folds through ccNPs compared to RXF suspensions in rats. It was shown that\nRXF-ccNPs could improve the intestinal permeability of RXF, increase the cellular uptake of RXF and\nfacilitate its transport across the absorptive epithelia. The results indicate that our developed ccNPs\nbased on sulfobutylether ... cyclodextrin and oligochitosan are a promising vehicle to orally deliver\npoorly water-soluble drugs over and above RXF.
Loading....