The medical therapy of tissue regeneration achieved by biomaterial-based tissue engineering has been currently expected as the third option following reconstructive surgery and organ transplantation. The basic idea of this regenerative therapy is to assist the self-healing potentials of body to induce the natural regeneration and repairing of defective or injured tissue. To this end, it is practically important to create a local environment which enables cells to promote their proliferation and differentiation, resulting in the induction of cell-based tissue regeneration. Tissue engineering is a biomedical technology or methodology to build up this regeneration environment by making use of biomaterials. Drug delivery system (DDS) is a biomaterial technology to enhance the in vivo biological functions of bio-signaling molecules (growth factors and genes) for promoted tissue regeneration. This paper overviews the recent status of tissue regeneration therapy based on the DDS technology of bio-signaling molecules.