Nanotechnology-based advanced materials are rapidly expanding development of better medicines. Long-standing efforts with lipid and polymer colloidal delivery systems, i.e. nanoparticles, have yielded better imaging and therapy. These benefits of nanotechnology, though limited, have driven efforts to develop advanced nanoparticles. This is particularly the case for targeted nucleic acid (gene) therapeutics based on short interfering ribonucleic acid (siRNA), which is a new gene inhibitor that is highly potent and selective. Here, we evaluate the use of modular conjugates to construct targeted nanoparticle therapeutics for nucleic acids. These nanoparticles are beginning to emulate the sophistication of virus particles – nature's own nanoscale assemblies for nucleic acids. For medicine, they promise the creation of a new generation of ‘targeted’ therapeutics that can offer multiple levels of selectivity.

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DOI: 10.1016/S1369-7021(05)71035-X