Efficient Delivery of therapeutics is critical for successful treatments of diseases. Synthetic materials have been extensively studied for the delivery of small molecular or macromolecular therapeutics. However, there are still unsolved problems especially in the area of targeted intracellular delivery of therapeutics. The research of our laboratory is aimed to design and synthesize functional nanostructures self-assembled from biodegradable polymers for delivery of therapeutics based on the principles of bioengineering, materials chemistry, biology and medicine. In this talk, I will introduce several types of nanostructures that have been recently designed in our laboratory, and their applications for delivery of small molecular anticancer drugs and macromolecular therapeutics (e.g. Herceptin, siRNA and DNA).