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pps proceeding
Symposium: S06 - Biopolymers and Polymer from Renewable Resources
Oral Presentation
 
 

Synthesis of new drug-phosphorus dendrimer conjugates and their evaluation as anticancer agents

El Kazzouli Saïd (1)*, El Brahmi Nabil (1), Mignani Serge (2), Cresteil Thierry (3), Bousmina Mosto (1), Majoral Jean-Pierre (4)

(1) Euro-Mediterranean University of Fes - Fes - Morocco, (2) Université Paris Descartes - Paris - France, (3) Institut de Chimie des Substances Naturelles - Paris - France, (4) Laboratoire de Chimie de Coordination du CNRS - Toulouse - France

Dendrimers which are nanosized polymeric molecules composed of a large number of perfectly branched monomers, have been studied for the delivery of both nontargeted and targeted drugs. In the targeted approach, the attachment of a targeting agent on the surface of the dendrimer allows preferential directing to, for example, cancer cell lines versus normal cell lines1. The small size of dendrimers enables their crossing through the gastrointestinal epithelium, tumor vasculature, and endothelium of cancer and inflammatory sites. While they are able to access the spleen and liver via fenestration, nanoparticles with 50−100 nm size are far too large to cross the endothelial barrier in all other healthy tissue but can reach some cancer cells and inflamed tissues2. In addition, nanoparticles have been shown to accumulate preferentially at tumor and inflammatory sites3. In this oral communication we will described our recent development concerning phosphorus dendrimers synthesis (generations Gc1 to Gc3) and functionalization using various drugs4. We will present also the anticancer activities of these drug-loaded dendrimers. References: 1) a) R. K. Tekade, P. V. Kumar, N. K. Jain, Chem. Rev. 109, 2009, 49. b) S. H. Medina, M. E. H. El-Sayed, Chem. Rev. 109, 2009, 3141. c) D. Astruc, E. Boisselier, C. Ornelas, Chem. Rev. 109, 2010, 1857. 2) V. P. Chauhan, T. Stylianopoulos, Y. Boucher, R. K. Jain, Annu. Rev. Chem. Biomol. Eng. 2, 2011, 281. 3) J. Fang, H. Nakamura, H. Maeda, Adv. Drug Delivery Rev. 18, 2011, 136 and references cited therein. 4) a) N. El Brahmi, S. El Kazzouli, S. Mignani, E. M. Essassi, G. Aubert, R. Laurent, A. M. Caminade, M. Bousmina, T. Cresteil, J-P. Majoral. Mol. Pharmaceutics. 10, 2013, 1459. b) N. El Brahmi, S. Mignani, J. Caron, S. El Kazzouli, M. Bousmina, A. M. Caminade, T. Cresteil, J. P. Majoral. Nanoscale. 7, 2015, 3915.