▎ 摘　　要

With the increasing development in scientific technology, building a nanocarrier system for cancer drugs has become a bliss for cancer patients. To allow for the oral administration of hydrophilic drugs, a nanocarrier that was based on negatively charged graphene oxide (GO) and prepared through the Layer-by-Layer (LbL) self-assembly of poly(acrylic acid)-cysteine (PAA-cys) and poly(allylamine hydrochloride) (PAH) was established. In the present study, we demonstrated the excellent biological properties of GO, the biological adhesiveness of PAA-cys, and the protection and controlled release profiles of polyelectrolyte. Pingyangmycin (PYM) was loaded onto the nanocarrier through non-covalent interactions. In vitro drug release studies of the prepared PAAcys-PAH-GO-PYM were pH-sensitive and showed sustained release effects for over 8 h, before they were completely expelled by gastrointestinal peristalsis. Furthermore, cell viability experiments using A549 lung adenocarcinoma cells revealed that the IC50 of PAA-cys-PAH-GO-PYM, free drug, and GO-PYM were 159.241 mu M, 134.960 mu M, and 129.815 mu M respectively, indicating the higher retention and cytotoxicity of PYM in vitro. When comparing the oral bioavailability of PYM with free drug, in vivo pharmacokinetics studies showed a 1.03-fold and 1.74-fold increase after GO loading and double-layer polyelectrolyte coating, respectively. Thus, PAA-cys-PAH-GO was successfully developed for oral delivery of PYM as anti-cancer therapy, and may provide further insight for oral administration of GO-based nanomaterials.