Utilization of Near-Infrared Fluorescent Imaging for Pharmaceutically Relevant Applications.

Optical imaging can be utilized for several pharmaceutical applications involving near-infrared fluorescent (NIRF) dyes or NIRF moiety-containing products. Especially during the early phases of product development, NIRF dyes can be used as surrogates for drugs and optical imaging methods can be utilized to optimize the pharmaceutical product properties based on dye entrapment efficiency, in vitro dye release, cellular uptake, and in vivo biodistribution. Based on in vivo accumulation, product efficacy and toxicity can be evaluated in the early development stage. Compared to visible fluorescent dyes, NIRF offers advantages such as low background from formulation excipients as well as biological components.In this chapter, the utility of NIRF imaging methods for in vitro characterization (in vitro release and cellular uptake) and in vivo/ex vivo applicability of pharmaceutically relevant products is presented in detail. Specifically, the application of fluorescence imaging to characterize perfluorocarbon-based formulations for dye loading, in vitro release, cellular uptake, and in vivo imaging to assess target accumulation and biodistribution is discussed. These methods are widely applicable to other nanoparticle-based products involved in inflammation/cancer imaging and therapy. Overall, NIRF-based techniques are indispensible because they are relatively easy, fast, and cost effective to characterize and optimize pharmaceutical products at different stages of product development.