Near infrared fluorescent peptide nanoparticles for enhancing esophageal cancer therapeutic efficacy

Abstract

Various types of nanoparticles have been proposed for targeted drug delivering, imaging, and tracking of therapeutic agents. However, highly biocompatible nanoparticles with structure-induced fluorescence and capability to conjugate with biomarkers and drugs remain lacking. This research proposes and synthesizes fluorescent nanoparticles (f-PNPs) assembled by cyclic peptides to combine imaging and drug delivering for esophageal cancer (EC). To achieve tumor targeting, f-PNPs are first conjugated with RGD moieties to selectively target EC cells via αvβ3 integrin; the nanoparticles are then embedded with epirubicin (EPI). Cell viability assays and analysis of tissue histology reveal that EPI-loaded RGD-f-PNPs (RGD-f-PNPs/EPI) led to significantly reduced cardiotoxicity and improved anti-tumor activity compared to EPI alone. Moreover, the drug delivery to tumor sites and therapeutic responses could be monitored with near-infrared fluorescence using RGD-f-PNPs/EPI. This unique nanoparticle system may lead to potential approaches for bioorganic fluorescence-based delivering, imaging, and drug release tracking.

Size‐Dependent Cellular Uptake of RGD Peptides

“…Additionally, RGD conjugates tend to accumulate on the cell surface as described for c (diketopiperazine‐RGD)‐sCy5 conjugates . However, in vivo experiments confirmed that numerous multivalent RGD conjugates are associated with improved uptake at tumor sites . These findings indicate that integrin‐mediated endocytosis is favored for peptides with multifold RGD sites.…”

Detection of enzyme‐triggered peptide self‐assembly via laser confocal Raman microscopy and circular dichroism spectroscopy in cellular environment

“…Raman peaks appeared during self‐assembly process for beta‐sheet formation are the best indications of these supramacromolecule‐based structures in both complex solutions and cellular environment . Hydrophobic interaction, hydrogen bonding interaction, and π–π stacking interactions are the forces present between the building blocks of these supramolecules. Self‐assemblies have been identified with a noninvasive label‐free technique based on Raman spectroscopy, which provides all the information for individual peak corresponding to trace elements.…”

A facile adenosine triphosphate‑responsive nanoplatform for efficacious therapy of esophageal cancer

“…Chemotherapy is a routine method for EC treatment. Commonly used chemotherapeutic agents include platinum drugs, taxanes and epirubicin (EPI) (5). However, low solubility in water and poor selective capability have greatly limited the clinical application of chemotherapeutic agents (6).…”