Currently there is great interest in developing engineered nanoformulations with highly integrated multifunctional capabilities due to their profound impact on molecular imaging, diagnostics, and targeted therapy. This talk will focus on novel multifunctional nanoformulations-based strategies, which offer unique platforms to study biomolecular events within a single living cell in real-time using the techniques based on plasmonically enhanced elastic and inelastic scattering of light. The design principle and methodologies behind the biologically targeted plasmonic nanoparticles, which enable new understandings of chemical mechanisms in living cells will also be presented. In addition, I will also present our progress in establishing a novel minimally invasive implant-assisted tumor targeting strategy capable of precisely guiding the systemically administered multifunctional magneto-plasmonic nanoformulations to deep tumor tissues with limited off-target accumulation. The unique therapeutic, sensing, and imaging capabilities of these magneto-plasmonic nanoformulations will also be discussed.