Owing to the diversity and ease of preparation of nanomaterials, the rational nanocarriers with a rational design have become increasingly popular in medical researches. Although nanoparticle-based drug delivery exhibits great potential, there are some challenges facing like rapid plasma clearance, triggering or aggravation of immune response, etc. Herein, cell-based targeted drug delivery systems have drawn more and more attention owing to low immunogenicity and intrinsic mutation rate, and innate ability to allow targeted delivery. Mesenchymal stem cells (MSCs) have been used in gene and drug delivery. The use of MSCs is a promising approach for the development of gene transfer systems and drug loading strategies because of their intrinsic properties, including homing ability and tumor tropism. By combining the inherent cell properties and merits of synthetic nanoparticles (NPs), cell membrane coated NPs emerge as the time requires. Overall, we provide a comprehensive overview of the utility of MSCs in drug and gene delivery as well as MSC membrane coated nanoparticles for therapy and drug delivery, aiming to figure out the significant room for development and highlight the potential future directions. Display omitted