Nanotechnology has great potential in bio-medicine, leading to tremendous efforts in gene transfection, drug delivery, cell targeting and hyperthermia. As researchers gain familiarity with homogeneous nanomaterials, more attention is drawn to Janus nanostructure, an emerging new material with two or more distinct properties. With the uniqueness in asymmetry, Janus nanomaterials offer more possibilities for assembling multifunctional carriers. In this chapter, the synthesis of ternary Janus system of silica, Fe 3 O 4 and polystyrene is introduced. A relatively easy method of combining miniemulsion and sol-gel is employed. The reaction mechanism is discussed with controllable morphology obtained. Dual surface functionalities are explored by selectively conjugating targeting group and anti-cancer drug. In vitro drug release profi les indicate a pH-responsive fashion. Cell study proves that the Janus nanocomposites successfully combine targeting and controlled drug release, achieving higher drug effi cacy. Future endeavors will focus on structure novelty as well as fabrication simplifi cation and scaling up. With its potential for higher integration, Janus nanostructures can well-serve as a versatile platform for biomedical applications.Bio-Inspired Nanomaterials and Applications Downloaded from www.worldscientific.com by KAINAN UNIVERSITY on 02/03/15. For personal use only.