A facile method for encapsulation of insoluble drugs has been developed based on the metal ion/polyphenol complexation and aerosol spraying process. The encapsulated paclitaxel nanodrug (PTX-C) is well-controlled in morphology and pH-responsive. In vivo and in vitro experiments demonstrated the enhanced anti-tumour activity of PTX-C. This study may pave the way for the fabrication of low cost, high efficiency drug delivery systems for cancer therapies.