We are witnessing a rapid development of innovative polymer-based biomaterials for controlled delivery of therapeutics and biotherapeutics (e.g., drugs, proteins, siRNA and DNA), targeted delivery of diagnostic agents (e.g., quantum dots and iron oxides), as well as functional delivery of cells and/or bioactives (e.g., stem cells and growth factors) in tissue engineering and regenerative medicine. It is interesting to note that innovation in delivery systems has already made significant technological impacts on medical research and practice. The Second Symposium on Innovative Polymers for Controlled Delivery (SIPCD 2012) was held in September 11–14, 2012 in Suzhou, China, to provide a high-level platform for worldwide top scientists, entrepreneurs, prominent young researchers and graduate students to meet and discuss state-of-the-art progress, challenging issues and future perspectives of controlled release systems. To our great pleasure, SIPCD 2012 has received overwhelming attention from different disciplines including polymers, biomedical engineering, pharmacy, nanotechnology, and regenerative medicine. The following block gives an overview of the highlights of the SIPCD 2012 symposium.