The role of the size and number of polyethylene glycol chains in the biodistribution and tumor localization of triazine dendrimers

Jongdoo Lim, Yi Guo, Cynthia L. Rostollan, Jennifer Stanfield, Jer Tsong Hsieh, Xiankai Sun, Eric E. Simanek

Research output: Contribution to journalArticlepeer-review

67 Scopus citations

Abstract

The synthesis and biodistribution of three triazine dendrimers differing in PEGylation are described. Dendrimers 1, 2, and 3 are derived from a common intermediate, dendrimer 4, and vary in molecular mass from 11 to 73 kDa as a result of PEGylation with multiple (theoretically, 16) PEG groups of 0.6, 2, and 5 kDa, respectively. As expected, elimination half-lives increased with an increase in molecular mass. In light of other results, however, molecular mass proves not to be the primary determinant of elimination half-lives. Instead, these times can be more readily predicted from the number of PEG groups on the dendrimer: the size of the PEG chain contributes to a lesser extent. Tumor uptake is observed for all the three dendrimers in mice bearing prostate cancer xenografts.

Original languageEnglish (US)
Pages (from-to)540-547
Number of pages8
JournalMolecular Pharmaceutics
Volume5
Issue number4
DOIs
StatePublished - Jul 2008

Keywords

  • Biodistribution
  • Dendrimer
  • Tumor

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery

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