Transporter-targeted nanoparticulate drug delivery systems (nano-DDS) have emerged as promising nanoplatforms for efficient drug delivery.Recently,great progress in transporter-targeted strategies has been made,especially with the rapid developments in nanotherapeutics.In this review,we outline the recent advances in transporter-targeted nano-DDS.First,the emerging transporter-targeted nano-DDS developed to facilitate oral drug delivery are reviewed.These include improvements in the oral absorption of protein and peptide drugs,facilitating the intravenous-to-oral switch in cancer chemotherapy.Secondly,the recent advances in transporter-assisted brain-targeting nano-DDS are discussed,focusing on the specific transporter-based targeting strategies.Recent developments in transportermediated tumor-targeting drug delivery are also discussed.Finally,the possible transport mechanisms involved in transporter-mediated endocytosis are highlighted,with special attention to the latest findings of the interactions between membrane transporters and nano-DDS.