The delivery of poorly water-soluble drugs represents a considerable challenge in pharmaceutical sciences.Several approaches,such as solubilizing adjuvants (i.e.,co-solvents,surfactants,complexing agents) or molecular dispersion,have been developed to overcome the solubility issue.Most of the strategies are based on the physical interactions between drugs and excipients,which are not so stable neither controllable,especially when in vivo.Stimuli-responsive prodrug approach,linking the drug and solubilizing groups via covalent bonds,is regarded as a favorable choice in managing the in vivo drug delivery in a controllable way.Among drug-delivery routes,oral administration is the preferred modality because of convenience and better patient compliance.Surprisingly,only few prodrug approaches have been proposed for the oral delivery of poorly soluble drugs [1].