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A Nanostructured PLGA System for Cell Delivery of a Tetrathiahelicene as a Model for Helical DNA Intercalators
Author(s) -
Cauteruccio Silvia,
Bartoli Cristina,
Carrara Claudio,
Dova Davide,
Errico Cesare,
Ciampi Giulia,
Dinucci Dinuccio,
Licandro Emanuela,
Chiellini Federica
Publication year - 2015
Publication title -
chempluschem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.801
H-Index - 61
ISSN - 2192-6506
DOI - 10.1002/cplu.201402347
Subject(s) - chemistry , plga , intercalation (chemistry) , dna , biophysics , cytotoxicity , drug delivery , intracellular , molecule , conjugated system , rhodamine , combinatorial chemistry , small molecule , cytotoxic t cell , fluorescence , biochemistry , in vitro , organic chemistry , polymer , biology , physics , quantum mechanics
A novel nanoconstruct based on poly(lactic‐co‐glycolic acid) nanoparticles loaded with a tetrathiahelicene molecule conjugated to a fluorescent rhodamine probe was prepared and characterized. Because helicenes are known to be very promising DNA intercalators, the tetrathiahelicene was selected for this study as a model therapeutic cytotoxic molecule. The ability of the nanoconstruct to internalize the tetrathiahelicene and deliver it intracellularly in a safe manner has been investigated by means of cytotoxicity and cell uptake tests on Balb/3T3 clone A31 fibroblasts. The outcomes of this study suggest the suitability of the developed nanoconstruct to act as a vector for the intracellular delivery of hydrophobic small molecules, such as helicenes, thus contributing to their possible future exploitation as novel therapeutics.