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.

A nanostructured PLGA system for cell delivery of a tetrathiahelicene as a model for helical DNA intercalators / S. Cauteruccio, C. Bartoli, C. Carrara, D. Dova, C. Errico, G. Ciampi, D. Dinucci, E. Licandro, F. Chiellini. - In: CHEMPLUSCHEM. - ISSN 2192-6506. - 80:3(2015), pp. 490-493. [10.1002/cplu.201402347]

A nanostructured PLGA system for cell delivery of a tetrathiahelicene as a model for helical DNA intercalators

S. Cauteruccio
Primo
;
D. Dova;E. Licandro
Penultimo
;
2015

Abstract

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.
cell uptake; DNA intercalators; drug delivery; poly(lactic-co-glycolic acid); tetrathiahelicenes
Settore CHIM/06 - Chimica Organica
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/249277
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