Poly(amidoamine)s with amino pendant groups were prepd. by hydrogen-transfer poly-addn. of primary and secondary amines to bis-acrylamines. Dansyl cadaverine (DC) doxorubicin (Dox) were bound to the polymers via a cis-aconityl spacer to give conjugates contg. 3 μg of DC per mg of polymer and 28 to 35 μg of Dox per mg of polymer. Release of DC and Dox at physiol. and acidic pH varied from 0 to 35% over 48 h and was pH dependent. Although the ISA1Dox conjugate (IC50 = 6 μg Dox/mL) presented similar toxicity as the parent polymer without Dox, ISA23Dox showed increased toxicity (IC50 = 10 μg Do
Poly(amidoamine) conjugates containing doxorubicin bound via an acid-sensitive linker / N. Lavignac, J.L. Nicholls, P. Ferruti, R. Duncan. - In: MACROMOLECULAR BIOSCIENCE. - ISSN 1616-5187. - 9:5(2009), pp. 480-487. [10.1002/mabi.200800163]
Poly(amidoamine) conjugates containing doxorubicin bound via an acid-sensitive linker
P. FerrutiPenultimo
;
2009
Abstract
Poly(amidoamine)s with amino pendant groups were prepd. by hydrogen-transfer poly-addn. of primary and secondary amines to bis-acrylamines. Dansyl cadaverine (DC) doxorubicin (Dox) were bound to the polymers via a cis-aconityl spacer to give conjugates contg. 3 μg of DC per mg of polymer and 28 to 35 μg of Dox per mg of polymer. Release of DC and Dox at physiol. and acidic pH varied from 0 to 35% over 48 h and was pH dependent. Although the ISA1Dox conjugate (IC50 = 6 μg Dox/mL) presented similar toxicity as the parent polymer without Dox, ISA23Dox showed increased toxicity (IC50 = 10 μg Do
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