2008
DOI: 10.1021/mp8000292
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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 eliminat… Show more

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Cited by 76 publications
(59 citation statements)
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“…Also, there are preclinical promising in vitro and in vivo results with active targeting dendrimers [73,365], for example antibody-dendrimer conjugates showed better efficacy than free antibodies [380][381][382][383], peptide (RGD) dendrimer conjugates showed enhanced tumor targeting [384][385][386], and folic acid functionalized dendrimers generated better tumor accumulations than untargeted controls or free drug, producing a stronger reduction of the tumor size [73,[387][388][389][390]. The slow translation of these preclinical studies to clinical trials may be due to the current toxicity of dendrimers [391,392], with the aim of the current research in the development of new biocompatible and less toxic alternatives [367,[393][394][395][396][397][398][399].…”
Section: Polymeric Nanocarriersmentioning
confidence: 99%
“…Also, there are preclinical promising in vitro and in vivo results with active targeting dendrimers [73,365], for example antibody-dendrimer conjugates showed better efficacy than free antibodies [380][381][382][383], peptide (RGD) dendrimer conjugates showed enhanced tumor targeting [384][385][386], and folic acid functionalized dendrimers generated better tumor accumulations than untargeted controls or free drug, producing a stronger reduction of the tumor size [73,[387][388][389][390]. The slow translation of these preclinical studies to clinical trials may be due to the current toxicity of dendrimers [391,392], with the aim of the current research in the development of new biocompatible and less toxic alternatives [367,[393][394][395][396][397][398][399].…”
Section: Polymeric Nanocarriersmentioning
confidence: 99%
“…More interestingly, PEGylated bow-tie G3 dendrimers with a total MW~160 kDa (t 1/2 =50 h) had a significantly lower half-life compared with PEGylated lysine dendrimers with a total MW of 68 kDa (t 1/2 =75 h), suggesting that the potentially higher clearance was due to the greater flexibility of the bow-tie polyester dendrimers (38,116). Recently, Lim et al directly compared the PEG effect in symmetrical PEG-modified polytriazine dendrimers to asymmetrical PEG-modified bow-tie polyester dendrimers (120). Based on the total MW and flexibility assumption, asymmetrically PEG-modified bow-tie dendrimers seem to require a longer PEG of 10-20 kDa (MW 85-160 kDa) to obtain a similar half-life of 40-50 h as symmetrically PEG-modified dendrimers with a shorter PEG of 2 kDa (MW 30-70 kDa).…”
Section: Pegylationmentioning
confidence: 99%
“…The numbers inserted in symbols indicate the molecular mass of the PEG chains. (Adapted from (106,114,116,118,120)). …”
Section: Targeting Ligandmentioning
confidence: 99%
“…Others could decrease the number of toxic amyloid oligomers [55,56]. The slow translation of preclinical studies to clinical trials may be due to the toxicity of dendrimers [46,47], with the aim of the current research in the development of new biocompatible and less toxic alternatives [57,58].…”
Section: Dendrimers As Drug Delivery Systemsmentioning
confidence: 99%