10.6084/m9.figshare.4828969.v1 Nivishna Venkatraj Nivishna Venkatraj M. J. Nanjan M. J. Nanjan Pascal Loyer Pascal Loyer M. J. N. Chandrasekar M. J. N. Chandrasekar Sandrine Cammas Marion Sandrine Cammas Marion Poly(malic acid) bearing Doxorubicin and N-Acetyl Galactosamine as a site-specific prodrug for targeting hepatocellular carcinoma Taylor & Francis Group 2017 Poly(malic acid) prodrug Doxorubicin N-Acetyl Galactosamine hepatocellular carcinoma 2017-04-07 07:24:11 Journal contribution https://tandf.figshare.com/articles/journal_contribution/Poly_malic_acid_bearing_Doxorubicin_and_N-Acetyl_Galactosamine_as_a_site-specific_prodrug_for_targeting_hepatocellular_carcinoma/4828969 <p>In the past, several systems of drug delivery carriers have been designed with a high capacity to target specific cells and/or tissues and a reduced non-specific toxicity. In this context, we synthesized and characterized novel poly(malic acid) derivatives bearing Doxorubicin (Dox), Poly(ethylene glycol) (PEG) and/or N-Acetyl Galactosamine (NAcGal) for drug delivery. These poly(malic acid) derivatives were obtained by chemical modification of the carboxylic acid lateral groups of poly(malic acid) (PMLA). The resulting nanoplatforms were evaluated for their <i>in vitro</i> cytotoxicity using the human HepaRG hepatoma cell line. Results reveal that the PMLA nanoplatform modified with PEG and Dox has an IC<sub>50</sub> of 936 nM corresponding to a Dox concentration of 47 nM, while the grafting of NAcGal onto the nanoplatform reduced the IC<sub>50</sub> to 527 nM corresponding to a Dox concentration of 26 nM. The presence of the targeting moiety, NAcGal, thus improves the cellular toxicity of the Dox.</p>