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中国临床药理学与治疗学 ›› 2020, Vol. 25 ›› Issue (10): 1151-1159.doi: 10.12092/j.issn.1009-2501.2020.10.011

• 综述与讲座 • 上一篇    下一篇

抗肿瘤药物的瘤内转运评价研究进展

刘 妍1,刘嘉莉1,贾元威2,周 芳1,王广基1,张经纬1   

  1. 1中国药科大学药物代谢动力学重点实验室,南京 210009,江苏;2皖南医学院弋矶山医院药物临床评价中心,芜湖 241001,安徽

  • 收稿日期:2020-04-14 修回日期:2020-07-14 出版日期:2020-10-26 发布日期:2020-11-03
  • 通讯作者: 张经纬,男,副研究员,研究方向:药物代谢动力学。 Tel: 025-83271176 E-mail: zhangjw_cnnj@sina.com
  • 作者简介:刘妍,女,硕士研究生,研究方向:药物代谢动力学。 Tel: 15150669565 E-mail: ly199606@163.com
  • 基金资助:
    国家科技重大新药创制专项子课题(2017ZX09201004-19);江苏省科技计划项目(BK20180558);皖南医学院弋矶山医院引进人才专项基金(YR201913,YR202015);皖南医学院弋矶山医院科研能力“高峰”培育计划精英项目(201909,201910)

Advances in the evaluation of intra-tumoral delivery of antitumor drugs

LIU Yan 1, LIU Jiali 1, JIA Yuanwei 2, ZHOU Fang 1, WANG Guangji 1, ZHANG Jingwei 1   

  1. 1 Key Lab of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, Jiangsu, China; 2 Drug Clinical Evaluation Center, Yijishan Hospital, Wannan Medical College, Wuhu 241001, Anhui, China
  • Received:2020-04-14 Revised:2020-07-14 Online:2020-10-26 Published:2020-11-03

摘要: 肿瘤组织异质性高、结构复杂,存在众多屏障使得抗肿瘤药物很难到达肿瘤组织中心部位,进而影响疗效。现阶段,各种提高药物瘤内转运的策略层出不穷,但是临床转化效率低,因此完善肿瘤内药物转运早期评价体系至关重要。合理的药物瘤内转运评价可以基于三维细胞模型、体内成像技术及合适的数学模型来全面揭示药物在肿瘤组织中的转运过程,进而预测和筛选各种影响因素,并反馈指导优化药物的瘤内递送。本文综述了抗肿瘤药物瘤内转运评价的方法,旨在更为准确、合理地评价抗肿瘤药物在肿瘤组织内的转运,为抗肿瘤药物的合成、剂型设计、药物联用以及临床用药方案的优化提供借鉴和思路。

关键词: 肿瘤, 药物转运, 三维细胞模型, 体内成像, 数学模型

Abstract: Tumor tissue is highly heterogeneous and complex in structure. Numerous barriers make it difficult for anti-tumor drugs to reach the center of the tumor tissue, which affects the efficacy. Currently, various strategies to improve intra-tumoral drug delivery are emerging in an endless stream, but the clinical conversion efficiency is low. Hence, it is essential to improve the early evaluation system of intra-tumoral drug delivery. Reasonable evaluation of intra-tumoral drug delivery can rely on three-dimensional cell models, in-vivo imaging technology and appropriate mathematical model to comprehensively reveal the drug delivery process in tumor tissues, predict and screen various influencing factors, and feedback to guide the optimization of intra-tumoral delivery of drugs. This article reviews the evaluation methods of intra-tumoral delivery of anti-tumor drugs, aiming to evaluate the transport of anti-tumor drugs in tumor tissues more accurately and reasonably, and to provide reference and ideas for the synthesis, preparation design, drug combination and optimization of clinical drug regimen of anti-tumor drugs.

Key words: tumor, drug delivery, three-dimensional cell model, in vivo imaging, mathematical model

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