Riboflavin-Targeted Drug Delivery

Area of Science:

• Oncology
• Biochemistry
• Nanomedicine

Background:

• Active targeting enhances drug delivery system retention in tumors.
• Vitamin receptors overexpressed in cancers are promising targets for drug delivery.
• Research focus is shifting from vitamin B9 (folate) to vitamin B2 (riboflavin) for cancer targeting.

Purpose of the Study:

• To review current knowledge on riboflavin transporter (RFVT) expression in healthy and pathological tissues.
• To discuss riboflavin internalization pathways.
• To provide an overview of riboflavin-targeted diagnostics and therapeutics.

Main Methods:

• Review of scientific literature on riboflavin transporters and their role in cancer.
• Analysis of riboflavin internalization mechanisms.
• Summary of preclinical and clinical studies on riboflavin-targeted drug delivery systems.

Main Results:

• Riboflavin carrier protein and riboflavin transporters (RFVT 1-3) are overexpressed in various tumor types, stem cells, and neovasculature.
• Tumor cells exhibit increased riboflavin metabolism compared to normal cells.
• Riboflavin conjugates with nanoparticles, polymers, dendrimers, and liposomes show high tumor affinity in preclinical studies.

Conclusions:

• Riboflavin transporters represent a promising target for active tumor targeting.
• Riboflavin-based drug delivery systems offer potential for enhanced cancer diagnostics and therapeutics.
• Further research into riboflavin internalization and targeted delivery is warranted.