Yen Jui-Hung, Chang Chun-Chun, Wu Tien-Yuan, Yang Chin-Hao, Hsu Hao-Jen, Liou Je-Wen
Department of Molecular Biology and Human Genetics, Tzu Chi University, Hualien, Taiwan.
Department of Laboratory Medicine, Hualien Tzu Chi Hospital, Buddhist Tzu Chi Medical Foundation, Hualien, Taiwan.
Tzu Chi Med J. 2025 May 2;37(3):223-234. doi: 10.4103/tcmj.tcmj_321_24. eCollection 2025 Jul-Sep.
Therapeutic peptides have become an intensively anticipated research field for novel drug discovery and design owing to their high specificity, efficacy, and biocompatibility. The advances in computer technology and structural biology, together with the invention of chemical peptide synthesis methods, have led to tremendous progress in this research field. Over the years, more than 100 peptide-based therapeutics have been approved for clinical use, and many others are currently under clinical trials. However, the application of therapeutic peptides is hindered by intrinsic disadvantages of peptides, such as poor stability against enzymatic degradations, short half-life, and low oral bioavailability. Therefore, strategies for efficiently protecting the peptides inside the body and facilitating the delivery of peptides to their targets are required. Lipid-based nanoparticles are considered a versatile class of carriers for drug delivery. Their biocompatibility, biodegradability, and ability to interact with biological membranes make them ideal platforms for delivery of peptides. Here, by leveraging examples, we aim to provide a comprehensive review of the current status of therapeutic peptide developments and lipid-based nanoparticles as drug carriers. Recent attempts to utilize lipid-based nanoparticles as platforms for the oral delivery of therapeutic peptides are also discussed.
由于其高特异性、有效性和生物相容性，治疗性肽已成为新药发现和设计中备受期待的研究领域。计算机技术和结构生物学的进步，以及化学肽合成方法的发明，推动了该研究领域的巨大进展。多年来，已有100多种基于肽的疗法被批准用于临床，还有许多正在进行临床试验。然而，治疗性肽的应用受到肽的固有缺点的阻碍，如对酶降解的稳定性差、半衰期短和口服生物利用度低。因此，需要能够在体内有效保护肽并促进肽向其靶点递送的策略。基于脂质的纳米颗粒被认为是一类通用的药物递送载体。它们的生物相容性、可生物降解性以及与生物膜相互作用的能力使其成为递送肽的理想平台。在此，我们通过举例，旨在全面综述治疗性肽的发展现状以及基于脂质的纳米颗粒作为药物载体的情况。还讨论了最近将基于脂质的纳米颗粒用作治疗性肽口服递送平台的尝试。
