2006
DOI: 10.1211/jpp.58.11.0010
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Abstract: Dendrimers have generated tremendous interest in the field of drug delivery. Despite indications of their utility as drug carriers, the inherent cytotoxicity associated with polycationic dendrimers acts as a limiting factor to their clinical applications. Many functionalization strategies have been adopted to mask peripheral amines in order to overcome this limitation. The object of the present investigation was to evaluate the effect of functionalization on the toxicological profile of fifth-generation poly(p… Show more

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Cited by 171 publications
(102 citation statements)
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“…For poly(propylene imine) dendrimers, other candidates for nonviral gene transfer, the relation of primary amine groups and toxicity has been clearly shown. 4 Shielding of the amine groups by functionalization decreased the toxicity of these constructs. 5 This review aims to clarify if cationic NPs interact with other cellular targets, act by other cytotoxic mechanisms and use other uptake routes than anionic and neutral NPs.…”
Section: Introductionmentioning
confidence: 99%
“…For poly(propylene imine) dendrimers, other candidates for nonviral gene transfer, the relation of primary amine groups and toxicity has been clearly shown. 4 Shielding of the amine groups by functionalization decreased the toxicity of these constructs. 5 This review aims to clarify if cationic NPs interact with other cellular targets, act by other cytotoxic mechanisms and use other uptake routes than anionic and neutral NPs.…”
Section: Introductionmentioning
confidence: 99%
“…PPI dendrimers conjugated to galactose were less hematotoxic than parent dendrimers, 16 and a substantial reduction in cytotoxicity and hemolytic toxicity was observed for lactose and mannose conjugated PPI dendrimers. 17 Furthermore, a dense maltose shell on the surface of PPI dendrimers significantly reduced the level of hemolysis.…”
Section: Introductionmentioning
confidence: 99%
“…For example, compared with the nearly 40 per cent mortality rate of HepG2 cells upon treatment of 70 mM G5 PAMAM, glycodendrimers with glucose, mannose, GlcNAc, lactose and Gal derivation on the surface exhibited no significant difference in cell viability to the nontreated cell group [45]. In a study by Agashe et al [129] on saccharide-modified PPI in the range 0.001-1 mg ml 21 , uncoated G5 PPI led to 86 per cent haemolysis after 4 h incubation and around 98 per cent mortality in HepG2 and Cos-7 cells, but lactose-and mannose-derived PPI showed less than 3 per cent haemolysis and above 95 per cent cell viability. It is noted that in these experiments, saccharide-conjugated dendrimers could exhibit slight toxicity, presumably owing to unmodified cationic residues on the dendrimer surface.…”
Section: Toxicity Of Bioactive Dendrimer Conjugatesmentioning
confidence: 94%