Yamamoto Eiichi
Analytical Research, Pharmaceutical Science & Technology Unit, Medicine Development Center, Eisai Co., Ltd.
Yakugaku Zasshi. 2019;139(2):249-254. doi: 10.1248/yakushi.18-00171-2.
Over the past few decades, liposome drug delivery systems (liposome DDS) have attracted much attention as the most advanced DDS. Efficacy and toxicity profiles of liposomes are based on their characteristic pharmacokinetics, drug release, and disposition after administration. Many attempts have been made to develop these systems especially as liposomal anti-cancer drugs. In the development of liposome DDS, identification of critical quality attributes and establishment of a control strategy to ensure consistent drug product quality are crucial. Among the quality attributes, particle size, drug encapsulation, and drug release from liposomes would affect their in vivo pharmacokinetic and pharmacodynamic properties. Thus these features need to be evaluated with appropriate analytical methods to confirm the quality and performance of the drug products. This article focuses on drug release from liposomes and reviews the effects of physicochemical properties of loaded drugs on release, simulation of drug release from liposomes, and design of a simulated body fluid for drug release assay of drug products.
在过去几十年中，脂质体药物递送系统（脂质体DDS）作为最先进的DDS备受关注。脂质体的疗效和毒性特征基于其给药后的特征性药代动力学、药物释放及处置情况。人们已进行了诸多尝试来开发这些系统，尤其是作为脂质体抗癌药物。在脂质体DDS的开发中，识别关键质量属性并建立控制策略以确保药品质量的一致性至关重要。在质量属性中，粒径、药物包封以及脂质体中的药物释放会影响其体内药代动力学和药效学性质。因此，需要用适当的分析方法评估这些特征，以确认药品的质量和性能。本文聚焦于脂质体中的药物释放，并综述了载药的物理化学性质对释放的影响、脂质体药物释放的模拟以及用于药品药物释放测定的模拟体液的设计。
