Label-free Raman microspectral analysis for comparison of cellular uptake and distribution between nontargeted and EGFR-targeted biodegradable polymeric nanoparticles

摘要

Active targeted delivery of nanoparticle-encapsulated agents to tumor cells in vivo is expected to enhance therapeutic effect with significantly less nonspecific toxicity. Active targeting is based on surface modification of nanoparticles with ligands that bind with extracellular targets and enhance payload delivery in the cells. In this study, we have used label-free Raman microspectral analysis and kinetic modeling to study cellular interactions and intracellular delivery of C6-ceramide using a nontargeted and an epidermal growth factor receptor (EGFR)-targeted biodegradable polymeric nano-delivery system, in EGFR-expressing human ovarian adenocarcinoma (SKOV3) cells. The results show that EGFR peptide-modified nanoparticles were rapidly internalized in SKOV3 cells leading to significant intracellular accumulation as compared to nonspecific uptake by the nontargeted nanoparticles. Raman microspectral analysis enables visualization and quantification of the carrier system, drug load, and responses of the biological systems interrogated, without exogenous staining and labeling procedures.