Drug targeting to specific organs and tissues has become one of the critical endeavors of the century since the use of free drugs in conventional dosage forms generally involves difficulties in achieving the target site at the appropriate dose after or during a proper time period. Modern advanced drug delivery systems aim to achieve controlled dosage at specific time, slow and extended delivery, targeted delivery and stimuli responsive based on the requirement of the therapy. Nanoparticles, liposomes and polymers were the first generation of therapeutic drug delivery systems that entered the market over the past two decades. Despite the lack of controlled release and molecular targeting properties in these products, they were able to enhance drug tolerability and/or efficacy. The introduction of controlled-release properties and targeting ligands in developing next-generation carriers is a promising approach in further facilitating their application in theranostic nanomedicine. The field is a multidisciplinary area that applies nanotechnology, chemistry, biotechnology, and biomechanics toward development of new modes of safer yet more effective therapeutic drugs for clinical practice. The focus of my research in drug delivery intends to take advantage of bio-inspired self-assembled nanostructures for efficient, safe, targeted and controlled drug delivery.