Epigenetics mechanisms play a significant role in human diseases by altering DNA methylation status, chromatin structure, and/or modifying histone proteins. By modulating the epigenetic status, the expression of genes can be regulated without any change in the DNA sequence itself. Epigenetic drugs exhibit promising therapeutic efficacy against several epigenetically originated diseases including several cancers, neurodegenerative diseases, metabolic disorders, cardiovascular disorders, and so forth. Currently, a considerable amount of research is focused on discovering new drug molecules to combat the existing research gap in epigenetic drug therapy. A novel and efficient delivery system can be established as a promising approach to overcome the drawbacks associated with the current epigenetic modulators. Therefore, formulating the existing epigenetic drugs with distinct encapsulation strategies in nanocarriers, including solid lipid nanoparticles, nanogels, bio‐engineered nanocarriers, liposomes, surface modified nanoparticles, and polymer–drug conjugates have been examined for therapeutic efficacy. Nonetheless, several epigenetic modulators are untouched for their therapeutic potential through different delivery strategies. This review provides a comprehensive up to date discussion on the research findings of various epigenetics mechanism, epigenetic modulators, and delivery strategies utilized to improve their therapeutic outcome. Furthermore, this review also highlights the recently emerged CRISPR tool for epigenome editing.

中文翻译：

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通过表观遗传调节剂的先进递送策略靶向表观基因组


表观遗传学机制通过改变 DNA 甲基化状态、染色质结构和/或修饰组蛋白在人类疾病中发挥重要作用。通过调节表观遗传状态，可以在不改变DNA序列本身的情况下调节基因的表达。表观遗传药物对多种表观遗传疾病（包括多种癌症、神经退行性疾病、代谢紊乱、心血管疾病等）表现出有希望的治疗功效。目前，大量的研究集中在发现新的药物分子，以弥补表观遗传药物治疗中现有的研究空白。可以建立一种新颖且有效的递送系统作为克服当前表观遗传调节剂相关缺点的有前途的方法。因此，在纳米载体中配制具有不同封装策略的现有表观遗传药物，包括固体脂质纳米颗粒、纳米凝胶、生物工程纳米载体、脂质体、表面修饰纳米颗粒和聚合物-药物缀合物，已对其治疗效果进行了检查。尽管如此，一些表观遗传调节剂通过不同的递送策略其治疗潜力并未受到影响。这篇综述对各种表观遗传学机制、表观遗传调节剂以及用于改善治疗结果的递送策略的研究结果进行了全面的最新讨论。此外，这篇综述还重点介绍了最近出现的用于表观基因组编辑的 CRISPR 工具。