Sulfonates-PMMA nanoparticles conjugates: a versatile system for multimodal application.

Abstract

We report herein the viability of a novel nanoparticles (NPs) conjugated system, namely the attachment, based on ionic and hydrophobic interactions, of different sulfonated organic salts to positively charged poly(methylmethacrylate) (PMMA)-based core-shell nanoparticles (EA0) having an high density of ammonium groups on their shells. In this context three different applications of the sulfonates@EA0 systems have been described. In detail, their ability as cytotoxic drugs and pro-drugs carriers was evaluated in vitro on NCI-H460 cell line and in vivo against human ovarian carcinoma IGROV-1 cells. Besides, 8-hydroxypyrene-1,3,6-trisulfonic acid, trisodium salt (HPTS) was chosen for NPs loading, and its internalization as bioimaging probe was evaluated on Hep G2 cells. Overall, the available data support the interest for these PMMA NPs@sulfonates systems as a promising formulation for theranostic applications. In vivo biological data strongly support the potential value of these core-shell NPs as delivery system for negatively charged drugs or biologically active molecules. Additionally, we have demonstrated the ability of these PMMA core-shell nanoparticles to act as efficient carriers of fluorophores. In principle, thanks to the high PMMA NPs external charge density, sequential and very easy post-loading of different sulfonates is achievable, thus allowing the preparation of nanocarriers either with bi-modal drug delivery behaviour or as theranostic systems.

• Authors: Claudio Monasterolo, Marco Ballestri, Giovanna Sotgiu, Andrea Guerrini, Paolo Dambruoso, Katia Sparnacci, Michele Laus, Michelandrea De Cesare, Assunta Pistone, Giovanni Luca Beretta, Franco Zunino, Valentina Benfenati, Greta Varchi
• Journal: Bioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 20 Issue 22 Pg. 6640-7 (Nov 15 2012) ISSN: 1464-3391 [Electronic] England
• PMID: 23043726 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2012 Elsevier Ltd. All rights reserved.

Chemical References

• Antineoplastic Agents
• Drug Carriers
• Prodrugs
• Sulfonic Acids
• Polymethyl Methacrylate
• Paclitaxel

Topics

• Animals
• Antineoplastic Agents (chemistry, therapeutic use, toxicity)
• Cell Line, Tumor
• Cell Survival (drug effects)
• Drug Carriers (chemistry)
• Female
• Hep G2 Cells
• Humans
• Mice
• Mice, Nude
• Nanoparticles (chemistry)
• Ovarian Neoplasms (drug therapy)
• Paclitaxel (administration & dosage, chemistry)
• Polymethyl Methacrylate (chemistry)
• Prodrugs (chemistry)
• Sulfonic Acids (chemistry)
• Transplantation, Heterologous