聚合物纳米药物制剂生物分析方法及药动学研究进展  

Advances in bioanalysis methods and pharmacokinetics of polymer nanopharmaceuticals

作　　者：崔雨琪 雷芳彬 张霖茜 尤建嵩 尹磊 史美云[1,2] CUI Yu-qi;LEI Fang-bin;ZHANG Lin-qian;YOU Jian-song;YIN Lei;SHI Mei-yun(School of Life and Pharmaceutical Sciences,Dalian University of Technology,Panjin 124221,China;Aim Honesty Biopharmaceutical Co.Ltd.,Dalian 116600,China)

机构地区：[1]大连理工大学生命科学与药学学院,辽宁盘锦124221 [2]艾美诚信生物制药有限公司,辽宁大连116600

出　　处：《药学学报》2023年第4期844-851,共8页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(81603182,81703607);大连市科技创新基金(2022JJ13SN075);中央高校基本科研业务费资助引进人才科研专题[DUT21RC(3)057]。

摘　　要：聚合物纳米药物制剂因其具有长循环、可降低免疫原性、不良反应小等优点,得到了越来越多的关注,已经成为纳米药物制剂研究的热点。然而,真正成功应用于临床的聚合物纳米药物制剂的数量非常少,药代动力学行为不理想是导致这一现象的主要原因之一。聚合物纳米制剂作为载药粒子进入体内之后,会释放出游离药物和聚合物辅料,游离药物是发挥药效的物质基础,而聚合物辅料则有可能会引起辅料-药物相互作用,因此,聚合物纳米药物制剂药代动力学研究的关注点不应该仅仅局限于游离药物本身,应该同时关注载药粒子、游离药物、聚合物辅料及其代谢物在体内的动态变化,这就为聚合物纳米药物制剂的生物分析方法提出了新的要求和挑战。基于此,本文简要介绍了聚合物纳米药物制剂的常用生物分析方法色谱分析法的特点及适用范围,概述了聚合物纳米药物制剂在体内的吸收、分布、代谢和排泄,希望能够为聚合物纳米药物制剂的药代动力学研究、安全性和有效性评价提供借鉴和参考。Polymer nanomaterials have been attracted more and more attention because of their advantages such as long circulation,reduced immunogenicity and less side effects,and have become a hot research topic in nanomaterials.However,the number of polymer nanomedicines successfully applied in clinical application is very limited,and the unsatisfactory pharmacokinetic behavior is one of the main reasons for thisresult.After polymer nanoparticles enter the body,they will release free drugs and polymer excipients.Polymer nanoparticles are the loaded drugs and free drugs are the active chemicals for efficacy,while polymer excipients may cause excipient drug interactions.Therefore,the focus of the pharmacokinetics study of polymer nanoparticles should not be only limited to the free drugs themselves,but should also focus on the loaded drugs,free drugs and polymer excipients.The dynamic changes of polymer excipients and their metabolites pose new requirements and challenges for the bioanalysis of polymer nanomedicines.The characteristics and application scope of common analytical methods for detection polymer nanomedicines including chromatographic assay will be discussed in this paper.Moreover,this review will also summarize the absorption,distribution,metabolism and excretion of polymer nanomedicines.We hope this review will provide reference for the pharmacokinetics study,safety and effectiveness evaluation of polymer nanomedicines.

关 键 词：聚合物 纳米制剂 生物分析方法 药动学 纳米载体 

分 类 号：R917[医药卫生—药物分析学]