药代动力学和生物分布对聚合物结构的依赖性：环状聚合物与线性聚合物的影响
Dependence of pharmacokinetics and biodistribution on polymer architecture: effect of cyclic versus linear polymers.
作者信息
Nasongkla Norased, Chen Bo, Macaraeg Nichole, Fox Megan E, Fréchet Jean M J, Szoka Francis C
机构信息
Department of Biopharmaceutical Sciences, School of Pharmacy, University of California, 513 Parnassus Avenue, San Francisco, California 94143-0912, USA.
出版信息
J Am Chem Soc. 2009 Mar 25;131(11):3842-3. doi: 10.1021/ja900062u.
Abstract
The ability of a polymer to reptate through a nanopore has an influence on its circulatory half-life and biodistribution, since many physiological barriers contain nanopores. A cyclic polymer lacks chain ends, and therefore, cyclic polymers with molecular weights greater than the renal threshold for elimination should circulate longer than their linear-polymer counterparts when injected into animals. As predicted, radiolabeled cyclic polymers with molecular weights greater than the renal threshold have longer blood circulation times in mice than do linear polymers of comparable molecular weight.
摘要
聚合物通过纳米孔进行蛇形运动的能力会对其循环半衰期和生物分布产生影响，因为许多生理屏障都含有纳米孔。环状聚合物没有链端，因此，当注射到动物体内时，分子量大于肾脏清除阈值的环状聚合物的循环时间应比其线性聚合物对应物更长。正如预测的那样，分子量大于肾脏阈值的放射性标记环状聚合物在小鼠体内的血液循环时间比具有相同分子量的线性聚合物更长。
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