肝X受体（LXR）是多种生物过程的主要调节因子，包括新陈代谢、炎症、发育和繁殖。作为核受体（NR）家族的已知核氧化固醇受体，LXR有两个同源亚型，LXRα（NR1H3）和LXRβ（NR1H2）。自上世纪90年代中期以来，已设计出许多针对LXR的药物，用于治疗动脉粥样硬化、系统性红斑狼疮和癌症等疾病。这些调节剂包括激动剂和拮抗剂，它们的选择性从不同的角度进行开发，包括亚型特异性、细胞特异性和组织特异性等。与此同时，也在研究先进的输送系统，以促进LXR药物在临床应用中的使用。其中最有希望的输送系统之一涉及纳米颗粒的使用，预计能提高LXR调节剂的临床潜力。本综述讨论了我们对LXR生物学和药理学的当前理解，重点关注LXRα和/或LXRβ调节剂的开发以及有潜力用作药物的纳米颗粒输送系统。版权所有©2023。由Elsevier B.V.出版。

Liver X receptors (LXRs) are master regulators of various biological processes, including metabolism, inflammation, development, and reproduction. As well-known nuclear oxysterol receptors of the nuclear receptor (NR) family, LXRs have two homologous subtypes, LXRα (NR1H3) and LXRβ (NR1H2). Since the mid-1990s, numerous LXR-targeted drugs have been designed to treat diseases such as atherosclerosis, systemic lupus erythematosus, and cancer. These modulators include agonists and antagonists, and the selectivity of them have been development from diverse aspects, including subtype-specific, cell-specific, tissue-specific types. Meanwhile, advanced delivery systems are also exploreed to facilitate the application of LXR drugs in clinical setting. One of the most promising delivery systems involves the use of nanoparticles and is expected to increase the clinical potential of LXR modulators. This review discusses our current understanding of LXR biology and pharmacology, focusing on the development of modulators for LXRα and/or LXRβ, and the nanoparticle-based delivery systems for promising LXR modulators with potential for use as drugs.Copyright © 2023. Published by Elsevier B.V.