Fluorescent Self-Assembled Complexes Based on Glyco-Functionalized G-Quadruplexes as a Targeted Delivery Platform.

Area of Science:

• Biomaterials Science
• Nanotechnology
• Drug Delivery Systems

Background:

• Precision medicine requires advanced drug delivery systems for enhanced efficacy and reduced toxicity.
• Stimuli-responsive release and targeted delivery are key features for ideal therapeutic platforms.
• Developing versatile platforms with simple preparation and combinational payload capabilities is crucial.

Purpose of the Study:

• To develop pH-sensitive fluorescent self-assembled complexes (SACs) for targeted drug delivery.
• To create a versatile platform capable of co-delivering therapeutic agents.
• To evaluate the targeted delivery, safety, and efficacy of the developed SACs.

Main Methods:

• Nanoprecipitation method was used to synthesize galactose-functionalized G-quadruplex (G4) and coumarin carboxamidine derivative SACs.
• Fluorescence imaging was employed to assess the selective targeting of hepatocellular carcinoma (HepG2) cells.
• Co-delivery studies were performed with prodrug floxuridine oligomers and SACs to evaluate cytotoxicity on normal (NIH/3T3) and cancer cells.

Main Results:

• The developed SACs demonstrated selective targeting of HepG2 cells.
• Co-delivery of floxuridine oligomers with SACs significantly reduced cytotoxicity to normal cells while maintaining anticancer efficacy.
• The platform showed potential for targeted combinational therapy with minimal hemolytic effects.

Conclusions:

• pH-sensitive fluorescent SACs serve as an effective targeted delivery platform for precision medicine.
• The strategy enables selective cancer cell targeting and reduced systemic toxicity.
• This self-assembly approach is extendable to ratiometric multidrug delivery for enhanced combinational therapy.