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Revolutionizing protein degradation: Harnessing nanoparticles for PROTAC delivery
Yonghang Fan1, Jianfen Su1, Jun Yang2
1The Affiliated Panyu Central Hospital, Guangzhou Municipal and Guangdong Provincial Key Laboratory of Molecular Target & Clinical Pharmacology, the NMPA and State Key Laboratory of Respiratory Disease, Guangdong Basic Research Center of Excellence for Respiratory Medicine, School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou, 511436, PR China.
Materials Today. Bio
|March 5, 2026
Summary
Proteolysis-targeting chimeras (PROTACs) offer new drug discovery avenues but face delivery challenges. Nanomedicine enhances PROTAC bioavailability and specificity, accelerating clinical translation for various diseases.
Area of Science:
- Drug Discovery and Nanomedicine
- Biotechnology and Therapeutics
Background:
- Proteolysis-targeting chimeras (PROTACs) represent a novel therapeutic strategy for diseases like cancer.
- PROTACs degrade target proteins by hijacking the ubiquitin-proteasome system, expanding the druggable proteome.
- Clinical translation is hindered by PROTACs' poor solubility, membrane permeability, and off-target effects.
Purpose of the Study:
- To review recent advances in nanoparticle-based delivery systems for PROTACs.
- To explore how nanocarrier design can overcome PROTAC limitations and enhance therapeutic outcomes.
- To identify current challenges and future directions for PROTAC nanomedicine development.
Main Methods:
- Systematic review of nanoparticle-based PROTAC delivery systems.
- Analysis of various nanocarrier platforms including organic, inorganic, biomimetic, and prodrugs.
- Examination of PROTAC property optimization and therapeutic outcome enhancement through nanocarrier design.
Main Results:
- Nanomedicine delivery systems effectively address PROTAC physicochemical and pharmacokinetic challenges.
- Nanocarriers enhance PROTAC bioavailability, cellular delivery, and target specificity.
- Diverse nanocarrier designs demonstrate potential for optimizing PROTAC properties.
Conclusions:
- Nanoparticle-based delivery is crucial for unlocking the full therapeutic potential of PROTACs.
- Optimized nanocarrier design is key to improving PROTAC efficacy and safety.
- Further development of nanomedicine strategies will accelerate the clinical translation of PROTAC therapeutics.
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