Department of Chemistry "Giacomo Ciamician", University of Bologna, 40126 Bologna, Italy.
Department of Chemistry "Giacomo Ciamician", University of Bologna, 40126 Bologna, Italy; byFlow srl, 40129 Bologna, Italy.
J Pharm Biomed Anal. 2023 Nov 30;236:115751. doi: 10.1016/j.jpba.2023.115751. Epub 2023 Sep 27.
Liposomes are nano-sized lipid-based vesicles widely studied for their drug delivery capabilities. Compared to standard carries they exhibit better properties such as improved site-targeting and drug release, protection of drugs from degradation and clearance, and lower toxic side effects. At present, scientific literature is rich of studies regarding liposomes-based systems, while 14 types of liposomal products have been authorized to the market by EMA and FDA and many others have been approved by national agencies. Although the interest in nanodevices and nanomedicine has steadily increased in the last two decades the development of documentation regulating and standardizing all the phases of their development and quality control still suffers from major inadequacy due to the intrinsic complexity of nano-systems characterization. Many generic documents (Type 1) discussing guidelines for the study of nano-systems (lipidic and not) have been proposed while there is a lack of robust and standardized methods (Type 2 documents). As a result, a widespread of different techniques, approaches and methodologies are being used, generating results of variable quality and hard to compare with each other. Additionally, such documents are often subject to updates and rewriting further complicating the topic. Within this context the aim of this work is focused on bridging the gap in liposome characterization: the most recent standardized methodologies suitable for liposomes characterization are here reported (with the corresponding Type 2 documents) and revised in a short and pragmatical way focused on providing the reader with a practical background of the state of the art. In particular, this paper will put the accent on the methodologies developed to evaluate the main critical quality attributes (CQAs) necessary for liposomes market approval.
脂质体是一种纳米级的基于脂质的囊泡，因其药物传递能力而被广泛研究。与标准载体相比，它们具有更好的特性，如改善的靶向部位和药物释放、保护药物免受降解和清除、降低毒性副作用。目前，科学文献中充满了关于基于脂质体的系统的研究，而 EMA 和 FDA 已经批准了 14 种脂质体产品上市，许多其他产品也已经获得了国家机构的批准。尽管在过去的二十年中，人们对纳米器件和纳米医学的兴趣稳步增加，但由于纳米系统特性的固有复杂性，规范和标准化其开发和质量控制各个阶段的文件的发展仍然存在重大不足。已经提出了许多讨论纳米系统（包括脂质和非脂质）研究指南的通用文件（类型 1），而缺乏稳健和标准化的方法（类型 2 文件）。因此，广泛使用了不同的技术、方法和方法，产生了质量参差不齐且难以相互比较的结果。此外，这些文件通常需要更新和重写，进一步使这个话题复杂化。在这种情况下，这项工作的目的是专注于弥合脂质体表征方面的差距：这里报告了最近适合脂质体表征的标准化方法（带有相应的类型 2 文件），并以简短而实用的方式进行了修订，重点是为读者提供最新技术状态的实际背景。特别是，本文将重点介绍为评估脂质体市场批准所需的主要关键质量属性（CQAs）而开发的方法。
