A HCOF-Based Drug Delivery System for Cancer Therapy via Intracellular Click Chemistry

Area of Science:

• Biomedical Engineering
• Organic Chemistry
• Drug Delivery Systems

Background:

• Click reactions offer high selectivity for synthesizing anticancer drugs.
• Tumor microenvironment enzymes can activate prodrugs, reducing conventional chemotherapy toxicity.
• Small-molecule drug metabolism necessitates advanced drug delivery systems.

Purpose of the Study:

• To develop a novel drug delivery platform using hollow covalent organic frameworks (HCOFs).
• To utilize click chemistry and nitroreductase (NTR) for targeted anticancer drug activation.
• To evaluate the antitumor efficacy and safety of the developed therapeutic system.

Main Methods:

• Synthesis and loading of prodrug molecules into HCOFs.
• In vitro and in vivo evaluation of the drug delivery system.
• Utilizing nitroreductase (NTR) to trigger click reactions for drug activation.

Main Results:

• The HCOF platform successfully loaded prodrugs and facilitated click reaction-based drug formation.
• Demonstrated significant antitumor efficacy in both in vitro and in vivo models.
• Indicated a promising approach to mitigate the toxicity associated with conventional chemotherapeutic agents.

Conclusions:

• Hollow covalent organic frameworks (HCOFs) are effective platforms for prodrug delivery via click chemistry.
• The NTR-triggered click reaction system shows excellent potential for targeted cancer therapy.
• This work expands the biomedical applications of HCOFs and click chemistry in drug development.