Nakmode Deepa D, Singh Baljinder, Abdella Sadikalmahdi, Song Yunmei, Garg Sanjay
Centre for Pharmaceutical Innovation, University of South Australia, North Terrace, Adelaide, SA, 5000, Australia.
Drug Deliv Transl Res. 2025 Apr;15(4):1156-1180. doi: 10.1007/s13346-024-01747-y. Epub 2024 Dec 11.
Despite being the most widely prescribed formulation, oral formulations possess several limitations such as low adherence, low bioavailability, high toxicity (in the case of anticancer drugs), and multiple-time administration requirements. All these limitations can be overcome by long-acting injectables. Improved adherence, patient compliance, and reduced relapse have been observed with long-acting formulation which has increased the demand for long-acting injectables. Drugs or peptide molecules with oral bioavailability issues can be easily delivered by long-acting systems. This review comprehensively addresses the various technologies used to develop long-acting injections with a particular focus on hydrophilic drugs and large molecules as well as the factors affecting the choice of formulation strategy. This is the first review that discusses the possible technologies that can be used for developing long-acting formulations for hydrophilic molecules along with factors which will affect the choice of the technology. Furthermore, the mechanism of drug release as well as summaries of marketed formulations will be presented. This review also discusses the challenges associated with the manufacturing and scale-up of the long-acting injectables.
尽管口服制剂是使用最广泛的剂型，但它存在一些局限性，如依从性低、生物利用度低、毒性高（抗癌药物的情况）以及需要多次给药。长效注射剂可以克服所有这些局限性。长效制剂已观察到依从性提高、患者顺应性提高和复发减少，这增加了对长效注射剂的需求。存在口服生物利用度问题的药物或肽分子可以通过长效系统轻松递送。本综述全面探讨了用于开发长效注射剂的各种技术，特别关注亲水性药物和大分子以及影响制剂策略选择的因素。这是第一篇讨论可用于开发亲水性分子长效制剂的可能技术以及影响技术选择的因素的综述。此外，还将介绍药物释放机制以及上市制剂的概述。本综述还讨论了长效注射剂制造和扩大生产规模方面的挑战。
