Han Hwa Seung, Koo Song Yi, Choi Ki Young
Natural Product Informatics Research Center, Korea Institute of Science and Technology (KIST), Gangneung, 25451, Republic of Korea.
Division of Bio-Medical Science and Technology, KIST School, University of Science and Technology (UST), Seoul, 02792, Republic of Korea.
Bioact Mater. 2021 Dec 20;14:182-205. doi: 10.1016/j.bioactmat.2021.11.027. eCollection 2022 Aug.
Over thousands of years, natural bioactive compounds derived from plants (bioactive phytocompounds, BPCs) have been used worldwide to address human health issues. Today, they are a significant resource for drug discovery in the development of modern medicines. Although many BPCs have promising biological activities, most of them cannot be effectively utilized in drugs for therapeutic applications because of their inherent limitations of low solubility, structural instability, short half-life, poor bioavailability, and non-specific distribution to organs. Researchers have utilized emerging nanoformulation (NF) technologies to overcome these limitations as they have demonstrated great potential to improve the solubility, stability, and pharmacokinetic and pharmacodynamic characteristics of BPCs. This review exemplifies NF strategies for resolving the issues associated with BPCs and summarizes recent advances in their preclinical and clinical applications for imaging and therapy. This review also highlights how innovative NF technologies play a leading role in next-generation BPC-based drug development for extended therapeutic applications. Finally, this review discusses the opportunities to take BPCs with meaningful clinical impact from bench to bedside and extend the patent life of BPC-based medicines with new formulations or application to new adjacent diseases beyond the primary drug indications.
数千年来，源自植物的天然生物活性化合物（生物活性植物化合物，BPCs）在全球范围内被用于解决人类健康问题。如今，它们是现代药物开发中药物发现的重要资源。尽管许多BPCs具有良好的生物活性，但由于其固有的低溶解度、结构不稳定、半衰期短、生物利用度差以及在器官中分布不特异等局限性，它们中的大多数无法有效地用于治疗性药物。研究人员利用新兴的纳米制剂（NF）技术来克服这些局限性，因为这些技术已显示出改善BPCs的溶解度、稳定性以及药代动力学和药效学特性的巨大潜力。本综述举例说明了用于解决与BPCs相关问题的NF策略，并总结了其在成像和治疗的临床前及临床应用中的最新进展。本综述还强调了创新的NF技术在基于BPCs的下一代药物开发以实现扩展治疗应用方面如何发挥主导作用。最后，本综述讨论了将具有有意义临床影响的BPCs从实验室应用到临床的机会，以及通过新制剂或应用于主要药物适应症以外的新相邻疾病来延长基于BPCs的药物的专利寿命。
