Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China; Municipal Key Laboratory of Biopharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
J Control Release. 2017 Oct 28;264:145-159. doi: 10.1016/j.jconrel.2017.08.034. Epub 2017 Aug 26.
Unsaturated fatty acids (UFAs), with the distinct advantages of good biocompatibility and innate tumor-targeting effect, have been widely investigated for the rational design of chemotherapy agent-unsaturated fatty acid (CA-UFA) prodrugs in cancer therapy. Among them, several CA-UFA prodrugs have successfully entered clinical trials and are promising prospects for potential clinical applications. In addition, CA-UFA prodrug-based nanoparticulate drug delivery systems (nano-DDS), which integrate the advantages of CA-UFA prodrugs and nano-DDS, have been emerging as versatile nano-carriers for the efficient delivery of chemotherapeutics. In this paper, we review the advanced drug delivery strategies based on UFA conjugates and focus on the recent advances in CA-UFA prodrugs and the emerging CA-UFA prodrug-based nano-DDS. First, we discuss the rational design of CA-UFA prodrugs in response to the multiple obstacles in chemotherapy, with particular emphasis on the latest progress in both preclinical studies and clinical trials. Moreover, the emerging CA-UFA prodrug-based nano-DDS are also addressed. Finally, the prospects and potential challenges of CA-UFA prodrug-based drug delivery strategies in chemotherapy are highlighted.
不饱和脂肪酸（UFAs）具有良好的生物相容性和先天的肿瘤靶向作用等显著优势，已广泛应用于癌症治疗中化疗药物-不饱和脂肪酸（CA-UFA）前药的合理设计。其中，一些 CA-UFA 前药已成功进入临床试验，具有广阔的潜在临床应用前景。此外，基于 CA-UFA 前药的纳米药物递送系统（nano-DDS）将 CA-UFA 前药和 nano-DDS 的优势集于一体，已成为高效递送达化疗药物的多功能纳米载体。本文综述了基于 UFA 缀合物的先进药物递送策略，并重点介绍了 CA-UFA 前药和新兴 CA-UFA 前药纳米药物递送系统的最新进展。首先，我们讨论了针对化疗中多重障碍的 CA-UFA 前药的合理设计，特别强调了临床前研究和临床试验中的最新进展。此外，还介绍了新兴的 CA-UFA 前药纳米药物递送系统。最后，强调了 CA-UFA 前药药物递送策略在化疗中的前景和潜在挑战。
