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Effective Non-Invasive Delivery of Epigenetic Drugs Using Functionalized Accessory Unit Conjugates.

Toshihiko Tashima1

  • 1Tashima Laboratories of Arts and Sciences, 1239-5 Toriyama-cho, Kohoku-ku, Yokohama 222-0035, Kanagawa, Japan.

Pharmaceutics
|January 28, 2026
PubMed
Summary

Epigenetic drugs target gene expression changes without altering DNA. Functionalized accessory units improve delivery of these therapies, overcoming challenges like poor permeability for better disease treatment.

Keywords:
antibody–drug conjugatecancer therapycarrier-mediated transportepigenetic drug deliveryepigeneticsnanoparticle-mediated deliveryreceptor-mediated endocytosis

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Area of Science:

  • Pharmaceutical Sciences
  • Molecular Biology
  • Genetics

Background:

  • Epigenetics involves heritable gene expression changes (DNA methylation, histone modifications, non-coding RNAs) without DNA sequence alteration.
  • Targeting epigenetic mechanisms offers a root cause intervention for diseases, driving advancements in pharmaceutical sciences.
  • Approved epigenetic drugs exist, but face delivery challenges like poor membrane permeability and biodistribution.

Purpose of the Study:

  • To review the potential and advantages of non-invasive delivery for epigenetic drugs.
  • To discuss overcoming delivery barriers using functionalized accessory units in epigenetic modulators.

Main Methods:

  • This narrative review synthesizes current research on epigenetic drug delivery.
  • Focuses on strategies incorporating functionalized accessory units into epigenetic modulators.

Main Results:

  • Functionalized accessory units, acting as vectors or carriers, can enhance epigenetic drug delivery.
  • Examples of accessory units include cell-penetrating peptides, tumor-homing peptides, and nanoparticles.
  • These conjugates show potential to overcome common drug delivery barriers.

Conclusions:

  • Functionalized accessory unit conjugates offer a promising strategy for effective non-invasive delivery of epigenetic drugs.
  • This approach may improve therapeutic outcomes by addressing current limitations in epigenetic drug development.