Shanghai Center for Drug Evaluation and Inspection, Haiqu Road 58, Shanghai 201210, China.
Molecules. 2022 Feb 17;27(4):1372. doi: 10.3390/molecules27041372.
Liposomes have been considered promising and versatile drug vesicles. Compared with traditional drug delivery systems, liposomes exhibit better properties, including site-targeting, sustained or controlled release, protection of drugs from degradation and clearance, superior therapeutic effects, and lower toxic side effects. Given these merits, several liposomal drug products have been successfully approved and used in clinics over the last couple of decades. In this review, the liposomal drug products approved by the U.S. Food and Drug Administration (FDA) and European Medicines Agency (EMA) are discussed. Based on the published approval package in the FDA and European public assessment report (EPAR) in EMA, the critical chemistry information and mature pharmaceutical technologies applied in the marketed liposomal products, including the lipid excipient, manufacturing methods, nanosizing technique, drug loading methods, as well as critical quality attributions (CQAs) of products, are introduced. Additionally, the current regulatory guidance and future perspectives related to liposomal products are summarized. This knowledge can be used for research and development of the liposomal drug candidates under various pipelines, including the laboratory bench, pilot plant, and commercial manufacturing.
脂质体被认为是一种很有前途和多功能的药物载体。与传统的药物传递系统相比，脂质体具有更好的性质，包括靶向部位、持续或控制释放、保护药物免受降解和清除、更好的治疗效果和更低的毒副作用。鉴于这些优点，在过去的几十年中，已经有几种脂质体药物产品成功获得批准并在临床上使用。在这篇综述中，讨论了美国食品和药物管理局 (FDA) 和欧洲药品管理局 (EMA) 批准的脂质体药物产品。基于 FDA 发布的批准文件包和 EMA 的欧洲公共评估报告 (EPAR)，介绍了已上市脂质体产品中应用的关键化学信息和成熟的制药技术，包括脂质赋形剂、制造方法、纳米化技术、载药方法以及产品的关键质量属性 (CQA)。此外，还总结了与脂质体产品相关的当前监管指导意见和未来展望。这些知识可用于各种研发阶段（包括实验室、中试和商业化生产）的脂质体候选药物的研发。
