Division of Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, The University of Texas at Austin, Austin, TX, USA.
Division of Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, The University of Texas at Austin, Austin, TX, USA.
Int J Pharm. 2020 Sep 25;587:119491. doi: 10.1016/j.ijpharm.2020.119491. Epub 2020 Jul 3.
How prevalent are peptide therapeutic products? How innovative are the formulations used to deliver peptides? This review provides a critical analysis of therapeutic peptide products and the formulations approved by the United States Food and Drug administration (FDA), the European Medicines Agency (EMA), and the Japanese Pharmaceuticals and Medical Devices Agency (PMDA). This review also provides an in-depth analysis of dosage forms and administration routes for delivering peptide therapeutics, including injectables, oral dosage forms, and other routes of administration. We discuss the function of excipients in parenteral formulations in detail, since most peptide therapeutics are parenterally administered. We provide case studies of alternate delivery routes and dosage forms. Based on our analysis, therapeutic peptides administered as injectables remain the most commonly used dosage forms, particularly in the form of subcutaneous, intravenous, or intramuscular injections. In addition, therapeutic peptides are formulated to achieve prolonged release, often through the use of polymer carriers. The limited number of oral therapeutic peptide products and their poor absorption and subsequent low bioavailability indicate a need for new technologies to broaden the formulation design space. Therapeutic peptide products may also be delivered through other administration routes, including intranasal, implant, and sublingual routes. Therefore, an in-depth understanding of how therapeutic peptides are now formulated and administered is essential to improve peptide delivery, improve patient compliance, and reduce the healthcare burden for these crucial therapeutic agents.
肽类治疗产品的流行程度如何？用于递送肽的制剂有何创新性？本综述对已获美国食品和药物管理局（FDA）、欧洲药品管理局（EMA）和日本药品和医疗器械管理局（PMDA）批准的治疗性肽产品和制剂进行了批判性分析。本综述还深入分析了递呈肽类治疗药物的剂型和给药途径，包括注射剂、口服剂型和其他给药途径。我们详细讨论了赋形剂在注射用制剂中的作用，因为大多数肽类治疗药物均采用注射给药。我们提供了替代给药途径和剂型的案例研究。基于我们的分析，作为注射剂的治疗性肽仍然是最常用的剂型，特别是以皮下、静脉或肌肉注射的形式。此外，治疗性肽被设计成实现延长释放，通常通过使用聚合物载体。为数不多的口服治疗性肽产品及其较差的吸收和随后的低生物利用度表明，需要新的技术来拓宽制剂设计空间。治疗性肽产品也可以通过其他给药途径递呈，包括鼻内、植入和舌下途径。因此，深入了解治疗性肽的现行配方和给药方式对于改善肽类递呈、提高患者顺应性以及降低这些重要治疗药物的医疗保健负担至关重要。
