Gold nanorods (GNRs) have a recognized role in treatment of cancers as efficient nanocarriers for chemotherapeutic drug delivery. In this study, GNRs modified with cholesterol-PEG were employed as a nanocarrier for a hydrophobic compound having a promising phosphatidylinositol 3-kinase (PI3Kα) inhibitory activity. The acquired nanocomplex was characterized by optical and infra-red (IR) absorption spectroscopies, in addition to hydrodynamic size and zeta potential. Glide docking and superposing of docked poses of the hydrophobic ligand and cholesterol moiety demonstrated that hydrophobic interactions drive the conjugation and attachment of the ligand to the cholesterol moiety of the nanocarrier. In vitro release study under a cellular environment indicates that the presence of cells has enhanced the release and the cellular uptake of the conjugated ligand. Furthermore, the anti-proliferative assay of the nanocomplex revealed potent cytotoxicity over a low concentration range of the nanocomplex against MCF-7 breast cancer cells compared to the free compound or the nanocarrier alone. Analysis of cellular death modality by flow cytometry showed that the nanocomplex has a rapid effect on cell death, as cells went toward the late apoptotic/necrotic stage rapidly and proportionally to the increase of the nanocomplex concentration. The overall results propose that cholesterol-decorated GNRs could be considered as a promising nanocarrier for hydrophobic drugs to achieve efficient delivery and potential therapy against breast cancer cells.
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