There has been a surge of interest in the development of biomaterials for medical applications, including drug or gene delivery, medical implants, tissue engineering, and diagnostics. Some of them are already in the market or under development in great anticipation. In this seminar I will present some recent progress made in my lab aiming to develop nanoparticle-based nanomedicine for cancer imaging and therapy. A major focus will be given to the development of functional molecules and materials for biomedical applications including diagnostics, drug delivery, and in vivo imaging. The topics of this seminar will include: (1) Biomedical applications of a novel class of high-affinity peptides (aptides) (2) Multistimuli-responsive nanovesicles for anticancer and anti-inflammatory therapy (3) Nontoxic, small lipid nanoparticles as a systemic delivery platform for RNAi therapeutics.