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. Deliver the goods: A preliminary study of the cellular uptake of a nanoconstruct obtained by loading poly(lactic-co-glycolic acid) (PLGA) nanoparticles with a tetrathiahelicene conjugated to a fluorescent rhodamine probe has been carried out. The ability to internalize the tetrathiahelicene and deliver it intracellularly has been investigated by means of cytotoxicity and cell uptake tests on Balb/3T3 clone A31 fibroblasts (see figure). Copyright © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
A nanostructured PLGA system for cell delivery of a tetrathiahelicene as a model for helical DNA intercalators
BARTOLI, CRISTINA;ERRICO, CESARE;CIAMPI, GIULIA;DINUCCI, DINUCCIO;CHIELLINI, FEDERICA
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. Deliver the goods: A preliminary study of the cellular uptake of a nanoconstruct obtained by loading poly(lactic-co-glycolic acid) (PLGA) nanoparticles with a tetrathiahelicene conjugated to a fluorescent rhodamine probe has been carried out. The ability to internalize the tetrathiahelicene and deliver it intracellularly has been investigated by means of cytotoxicity and cell uptake tests on Balb/3T3 clone A31 fibroblasts (see figure). Copyright © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
