alexa Poly(amidoamine) conjugates containing doxorubicin bound via an acid-sensitive linker.
Biomedical Sciences

Biomedical Sciences

Journal of Biomedical Engineering and Medical Devices

Author(s): Lavignac N, Nicholls JL, Ferruti P, Duncan R

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Abstract Poly(amidoamine)s with amino pendant groups were prepared by hydrogen-transfer polyaddition 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 containing 3 microg of DC per mg of polymer and 28 to 35 microg of Dox per mg of polymer. Release of DC and Dox at physiological and acidic pH varied from 0 to 35\% over 48 h and was pH dependent. Although the ISA1Dox conjugate (IC(50) = 6 microg Dox x mL(-1)) presented similar toxicity as the parent polymer without Dox, ISA23Dox showed increased toxicity (IC(50) = 10 microg Dox x mL(-1)). These results suggest that ISA23Dox is able to release biologically active Dox in vitro and that this conjugate might be suitable for further development. This article was published in Macromol Biosci and referenced in Journal of Biomedical Engineering and Medical Devices

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