title: The role of the size and number of polyethylene glycol chains in the biodistribution and tumor localization of triazine dendrimers.
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.
authors.affiliation: Department of Chemistry, Texas A&M University, College Station, TX 77843-3255, USA.
authors.forename: Jongdoo
authors.initials: J
authors.lastname: Lim
authors.forename: Yi
authors.initials: Y
authors.lastname: Guo
authors.forename: Cynthia L
authors.initials: CL
authors.lastname: Rostollan
authors.forename: Jennifer
authors.initials: J
authors.lastname: Stanfield
authors.forename: Jer-Tsong
authors.initials: JT
authors.lastname: Hsieh
authors.forename: Xiankai
authors.initials: X
authors.lastname: Sun
authors.forename: Eric E
authors.initials: EE
authors.lastname: Simanek
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D050091:Dendrimers / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics*; D006801:Humans; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D015394:Molecular Structure; D008970:Molecular Weight; D009369:Neoplasms / Q000473:pathology*; D011092:Polyethylene Glycols / Q000737:chemistry*; D013154:Spleen / Q000187:drug effects / Q000378:metabolism; D014018:Tissue Distribution; D014227:Triazines / Q000737:chemistry*; D023041:Xenograft Model Antitumor Assays
chemical_list: D050091:Dendrimers; D014227:Triazines; D011092:Polyethylene Glycols