Meng Xiangjun, Zhang Zhi, Tong Jin, Sun Hui, Fawcett John Paul, Gu Jingkai
Research Center for Drug Metabolism, School of Life Sciences, Jilin University, Changchun 130012, China.
School of Pharmaceutical Sciences, Tsinghua University, Beijing 100084, China.
Acta Pharm Sin B. 2021 Apr;11(4):1003-1009. doi: 10.1016/j.apsb.2021.02.018. Epub 2021 Mar 4.
Monomethoxy poly(ethylene glycol)--poly(d,l-lactic acid) (PEG-PLA) is a typical amphiphilic di-block copolymer widely used as a nanoparticle carrier (nanocarrier) in drug delivery. Understanding the fate of PEG-PLA is required to evaluate its overall safety and promote the development of PEG-PLA-based nanocarrier drug delivery systems. However, acquiring such understanding is limited by the lack of a suitable analytical method for the bioassay of PEG-PLA. In this study, the pharmacokinetics, biodistribution, metabolism and excretion of PEG-PLA were investigated in rat after intravenous administration. The results show that unchanged PEG-PLA is mainly distributed to spleen, liver, and kidney before being eliminated in urine over 48 h mainly (>80%) in the form of its PEG metabolite. Our study provides a clear and comprehensive picture of the fate of PEG-PLA which we anticipate will facilitate the scientific design and safety evaluation of PEG-PLA-based nanocarrier drug delivery systems and thereby enhance their clinical development.
单甲氧基聚（乙二醇）-聚（d，l-乳酸）（PEG-PLA）是一种典型的两亲性二嵌段共聚物，在药物递送中广泛用作纳米颗粒载体（纳米载体）。了解PEG-PLA的去向对于评估其整体安全性以及促进基于PEG-PLA的纳米载体药物递送系统的发展至关重要。然而，由于缺乏用于PEG-PLA生物测定的合适分析方法，获取此类信息受到限制。在本研究中，对大鼠静脉注射PEG-PLA后的药代动力学、生物分布、代谢和排泄进行了研究。结果表明，未变化的PEG-PLA主要分布于脾脏、肝脏和肾脏，然后在48小时内主要以其PEG代谢物的形式（>80%）经尿液排出。我们的研究提供了PEG-PLA去向的清晰而全面的情况，我们预计这将有助于基于PEG-PLA的纳米载体药物递送系统的科学设计和安全性评估，从而促进其临床开发。
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