高分子药物学的研究进展与期盼

THE PROGRESS AND EXPECTATION OF POLYMER PHARMACY

自从20世纪70年代提出高分子前药的概念以来,伴随着纳米技术的发展,"高分子药物学"作为高分子科学和材料学、纳米科学、药物学、临床医学、分析科学的交叉学科,正在悄然形成.本文综述了近年高分子药物在药物化学、制剂学、药效学等方面所取得的进展,概述了高分子药物的药理学和药代动力学与小分子药物的区别与联系,指出了高分子药物药效学、药理学和药代动力学研究中的难题和瓶颈,特别是高分子药物可能存在的"三种状态"及从"纳米颗粒药"到"单个高分子药"再到"小分子药"的转变,分析了高分子药输送过程中存在的多重屏障如毛细血管壁、细胞外基质和细胞壁等,阐述了高分子药物的"生理靶向"和"EPR"效应的竞争,指出了高分子药在靶向输送和逆转耐药方面的优势,强调了发展相关分析方法的必要性,期盼高分子科学家与药物学家进行真诚有效的合作,大力促进我国高分子药物学和高分子药物产业的创新和发展.

Since the ＂ polymer prodrug＂ concept was first proposed in 1970s,＂polymer pharmacy＂, as the interdiscipline of polymer science, material science, nano-science, pharmacy, clinical medicine and analysis science, has been quietly born along with the development of nanotechnology. In this paper, an overview of the progress of polymer drugs in pharmacochemistry, pharmaceutics, and pharmacodynamics is provided; the connection and distinction between polymer drugs and small molecule drugs in pharmacology and pharmacokinetics are outlined; the bottleneck tissues in pharmacodynamics and pharmacokinetics of polymer drugs are pointed out, especially the ＂three states＂ of polymer drugs and the transformation of the ＂ nano- particle drug＂ through ＂ macromolecular drug＂ to ＂ small molecular drug＂; the multiple obstacles on the pathway of polymer drugs such as capillary vessel wall, extracellular substance, cellular wall, etc. , are analyzed; the competition between the ＂physiological targeting＂ of human organs and the ＂ EPR effect＂ of cancerous tissues is elucidated ; the possible contribution and merits of polymer drugs in drug targeting delivery and in reversion of drug resistance are pointed out; the necessity of developing the related analytical methods is emphasized; and an urgent expectation is expressed that scientists and experts working in polymer science and in pharmacology cooperate with each other sincerely and effectively to promote the innovation and development in polymer pharmacy and polymer drug industry in our country.