Jul 2026· NEWPORT INTERNATIONAL JOURNAL OF SCIENTIFIC AND EXPERIMENTAL SCIENCES· Vol 7, pp. 78-83· 0 citations
TL;DR
The biological basis of epigenetic alterations in malignancy is examined, major nanocarrier platforms for epigenetic therapy are discussed, and advances in targeting DNA methylation, histone modifications, and chromatin architecture are highlighted.
Abstract
Epigenetic dysregulation is a defining feature of cancer, driving malignant transformation, tumor progression, and therapeutic resistance through reversible yet heritable alterations in gene expression. Aberrant DNA methylation, histone modifications, and chromatin remodeling disrupt normal cellular identity and enable oncogenic transcriptional programs without altering the underlying DNA sequence. Although epigenetic enzymes are druggable and several epigenetic inhibitors have reached clinical use, their therapeutic impact has been constrained by limited specificity, systemic toxicity, poor pharmacokinetics, and the inability to precisely modulate complex epigenetic networks within tumors. Nanotechnology-based strategies have emerged as powerful tools to address these limitations by enabling targeted delivery, controlled release, and combinatorial modulation of epigenetic regulators. By leveraging nanoscale materials such as liposomes, polymeric nanoparticles, inorganic nanocarriers, and self-assembled systems, epigenetic drugs can be selectively delivered to tumor cells and subcellular compartments, enhancing efficacy while minimizing off-target effects. This review provides a comprehensive overview of nanotechnology-based approaches for modulating epigenetic dysregulation in cancer. We examine the biological basis of epigenetic alterations in malignancy, discuss major nanocarrier platforms for epigenetic therapy, and highlight advances in targeting DNA methylation, histone modifications, and chromatin architecture. Current challenges, translational considerations, and future directions for precision epigenetic nanomedicine are also critically discussed.
Keywords: epigenetic therapy; nanotechnology; cancer; chromatin regulation; precision oncology.
Epigenetic mechanisms play a crucial role in OC drug resistance, and emerging evidence suggests that dysregulated epigenetic modifications are among the key contributors to OC. Epigenetic agents, including DNA methyltransferase inhibitors, histone deacetylase inhibitors, and non-coding RNA-based therapeutics, have important limitations, including poor water solubility, limited tissue distribution, low stability, and systemic toxicity. To overcome this, a novel drug delivery system is needed to manage variability in drug administration and maximize the efficacy of these drugs. In this regard, nanotechnology offers an attractive option for formulating epigenetic drugs with various encapsulation strategies to increase bioavailability and drug efficacy, reduce drug dose, administration frequency, and toxicity, and enhance cellular internalization and tumor-targeted delivery. In this review, we summarize various epigenetic regulators and their roles in OC therapy resistance as well as the development of nanosystems for epigenetic drug delivery, which could lay the foundation for designing nanoformulations encapsulating epigenetic therapeutics, ultimately advancing personalized, targeted therapy for patients with OC. This review also discusses the current clinical status of nanocarrier platforms and translational barriers that limit the clinical development of epigenetic nanomedicine, highlighting the future directions required for successful clinical translation.
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