International Journal of Biological Macromolecules, Journal Year: 2025, Volume and Issue: unknown, P. 143225 - 143225
Published: April 1, 2025
Language: Английский
International Journal of Biological Macromolecules, Journal Year: 2025, Volume and Issue: unknown, P. 143225 - 143225
Published: April 1, 2025
Language: Английский
Health Sciences Review, Journal Year: 2025, Volume and Issue: unknown, P. 100218 - 100218
Published: Jan. 1, 2025
Language: Английский
Citations
1Pharmaceutics, Journal Year: 2025, Volume and Issue: 17(4), P. 501 - 501
Published: April 9, 2025
Proteolysis targeting chimeras (PROTACs), heterobifunctional molecules that hijack the ubiquitin–proteasome system (UPS) to degrade specific proteins, hold great promise in treating diseases driven by traditionally “undruggable” targets. However, their large molecular weight, high hydrophobicity, and other physicochemical hurdles contribute limited bioavailability, suboptimal pharmacokinetics, attenuated therapeutic efficacy. Consequently, diverse formulation innovations have been investigated optimize PROTAC delivery. This review examines current challenges advances specialized drug delivery approaches designed bolster pharmacological performance. We first outline fundamental limitations of PROTACs—their low aqueous solubility, poor cell permeability, rapid clearance, concentration-dependent “hook effect”. then discuss how various enabling formulations address these issues, including polymeric micelles, emulsions, amorphous solid dispersions, lipid-based nanoparticles, liposomes, exosomes. Collectively, technologies substantially improve outcomes PROTACs preclinical cancer models. Future applications may extend beyond oncology complex using newly emerging molecules. By integrating advanced science with innovative degrader design, field stands poised unlock clinical potential for protein degradation therapies.
Language: Английский
Citations
0International Journal of Biological Macromolecules, Journal Year: 2025, Volume and Issue: unknown, P. 143225 - 143225
Published: April 1, 2025
Language: Английский
Citations
0