Book excerpt: This book comprehensively reviews the recent advances in nanomaterial-based molecular imaging, diagnostics, and personalized therapy. It discusses the novel biocompatible fluorescent nanomaterials, their synthesis, and modern state of art characterization, as well as the various strategies for immobilization of biomacromolecules on the nanomaterial surface and approaches for increasing their stability. In addition, the book describes the synthesis of lectin nanoconjugates using different types of biocompatible raw materials and their systematic characterization. Lastly, it presents our current understanding of the biomolecular carona, which affects nanoparticle-based targeted drug delivery, and examines the conceptual approaches to improve the in-vivo efficacy of targeted drug delivery.