Instability, poor cellular uptake and unfavorable pharmacokinetics and biodistribution of many therapeutic molecules require modification in their physicochemical properties. The conjugation of these APIs with fatty acids has demonstrated an enhancement in their lipophilicity and stability. The improvement in the formulations that resulted from the conjugation of a drug with a fatty acid includes increased half-life, enhanced cellular uptake and retention, targeted tumor delivery, reduced chemoresistance in cancer, and improved blood-brain-barrier (BBB) penetration. In this review, various therapeutic molecules, including small molecules, peptides and oligonucleotides, that have been conjugated with fatty acid have been thoroughly discussed along with various conjugation strategies. The application of nano-system based delivery is gaining a lot of attention due to its ability to provide controlled drug release, targeting and reducing the extent of side effects. This review also covers various nano-carriers that have been utilized for the delivery of fatty acid drug conjugates. The enhanced lipophilicity of the drug-fatty acid conjugate has shown to enhance the affinity of the drug towards these carriers, thereby increasing the entrapment efficiency and formulation performance.

许多治疗分子的不稳定、细胞摄取差和不利的药代动力学和生物分布需要改变它们的理化特性。这些 API 与脂肪酸的结合证明了它们的亲脂性和稳定性的增强。由于药物与脂肪酸结合而导致的配方改进包括增加半衰期、增强细胞摄取和保留、靶向肿瘤递送、降低癌症中的化学抗性以及改善血脑屏障 (BBB) 渗透。在这篇综述中，与脂肪酸结合的各种治疗分子，包括小分子、肽和寡核苷酸，已经与各种结合策略一起进行了彻底的讨论。基于纳米系统的递送应用因其提供控制药物释放、靶向和减少副作用程度的能力而受到广泛关注。本综述还涵盖了已用于递送脂肪酸药物偶联物的各种纳米载体。药物-脂肪酸偶联物增强的亲脂性已显示增强药物对这些载体的亲和力，从而提高包封效率和制剂性能。