部分聚乙二醇化聚赖氨酸树枝状聚合物与完全聚乙二醇化树枝状聚合物相比，血浆稳定性和循环时间降低。

Partly-PEGylated Poly-L-lysine dendrimers have reduced plasma stability and circulation times compared with fully PEGylated dendrimers.

机构信息

Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.

出版信息

J Pharm Sci. 2009 Oct;98(10):3871-5. doi: 10.1002/jps.21692.

DOI:10.1002/jps.21692

PMID:19283758

Abstract

The current study was performed to examine the effect of 50% surface PEGylation on the plasma circulation, biodistribution and metabolism of intravenously administered Generation 4 poly-L-lysine dendrimers in rats. Partial surface PEGylation blocked the rapid and extensive vascular binding previously described for the non-PEGylated dendrimer and slowed metabolism of the core, however the effect was less than that observed for total surface coverage of PEG. Capping the residual surface amines with acetyl groups further improved plasma stability.

摘要

本研究旨在考察 50%表面聚乙二醇化对静脉给予的第四代聚-L-赖氨酸树枝状聚合物在大鼠体内的血浆循环、分布和代谢的影响。部分表面聚乙二醇化阻止了先前描述的非聚乙二醇化树枝状聚合物的快速和广泛的血管结合，并减缓了核心的代谢，但效果不如完全表面聚乙二醇化覆盖观察到的那么明显。用乙酰基封闭残留的表面胺进一步提高了血浆稳定性。