Article history: Targeted delivery aims to concentrate therapeutic agents at their site of action and thereby enhance Received 23 November 2011 treatment and limit side-effects. E-selectin on endothelial cells is markedly up-regulated by cytokine Received in revised form 11 January 2012 stimulation of inﬂamed and some tumoral tissues, promoting the adhesion of leukocytes and metastatic Accepted 13 January 2012 tumor cells, thus making it an interesting molecular target for drug delivery systems. Available online 23 January 2012 We report here the preparation of targeted nanoparticles from original amphiphilic block copolymers functionalized with an analog of sialyl Lewis X (SLEx), the physiological ligand of E-selectin. Nanoparticles, Keywords: prepared by nanoprecipitation, caused no signiﬁcant cytotoxicity. Ligand-functionalized nanoparticles Carbohydrate ligand conjugated polymers were speciﬁcally recognized and internalized better by tumor necrosis factor (TNF-)-activated human E-selectin umbilical vein endothelial cells (HUVECs) than control nanoparticles or HUVECs with low E-selectin HUVECs expression. These nanoparticles are designed to carry the ligand at the end of a PEG spacer to improve Nanoparticles accessibility. This system has potential for the treatment of inﬂammation, inhibition of tumor metastasis, and for molecular imaging. © 2012 Elsevier B.V. All rights reserved. 1. Introduction peptides (Myrset et al., 2011; Shamay
International Journal of Pharmaceutics – Elsevier
Published: Apr 15, 2012
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