TY - JOUR
T1 - Sulfonates-PMMA nanoparticles conjugates
T2 - A versatile system for multimodal application
AU - Monasterolo, Claudio
AU - Ballestri, Marco
AU - Sotgiu, Giovanna
AU - Guerrini, Andrea
AU - Dambruoso, Paolo
AU - Sparnacci, Katia
AU - Laus, Michele
AU - Cesare, Michelandrea De
AU - Pistone, Assunta
AU - Beretta, Giovanni Luca
AU - Zunino, Franco
AU - Benfenati, Valentina
AU - Varchi, Greta
N1 - Funding Information:
Mediteknology S.r.l, Area Ricerca CNR, Via Gobetti 101, I-40129 Bologna, Italy for kindly providing compounds 6 – 8 . This work was also supported by Italian MIUR project FIRB-RBPR05JH2 (ITALNANONET).
PY - 2012/11/15
Y1 - 2012/11/15
N2 - 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.
AB - 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.
KW - Drug delivery
KW - Nanoparticles
KW - Organic dyes
KW - PMMA
KW - Theranostic systems
UR - http://www.scopus.com/inward/record.url?scp=84867861231&partnerID=8YFLogxK
U2 - 10.1016/j.bmc.2012.09.023
DO - 10.1016/j.bmc.2012.09.023
M3 - Article
SN - 0968-0896
VL - 20
SP - 6640
EP - 6647
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 22
ER -