This study gives an original methodology to synthetize novel metallo‐drugs nanoparticles relevant for medicinal chemistry. Gold (HAuCl4) are complexes with antitumor compounds (paclitaxel (PTX); docetaxel (DTX)) and dicarboxylic acid‐terminated polyethylene‐glycol (PEG) that plays a role of surfactants. The proposed synthesis is fast and leads to hybrid‐metal nanoparticles (AuNPs) in which drug solubility is improved. The interactions between drugs (DTX, PTX), PEG diacid (PEG), and Au (III) ions to form hybrid nanocarriers called DTX IN PEG‐AuNPs and PTX IN PEG‐AuNPs, are characterized by various analytical techniques (Raman and UV–vis spectroscopies) and transmission electron microscopy. The efficient drugs release under pH conditions is also achieved and characterized showing an amazing reversible equilibrium between Au (III)‐complex‐drug and Au0NPs. For therapeutic purposes, such AuNPs are then decorated with the anti‐EGFR polyclonal antibodies, which specifically recognizes the hERG1 channel aberrantly expressed on the membrane of human lung cancer cells. This paper, through an original chemical approach, will occupy an important position in the field of nanomedicine, and hope that novel perspectives will be proposed for the development of high drug‐loading nanomedicines.

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