A Nanostructured PLGA System for Cell Delivery of a Tetrathiahelicene as a Model for Helical DNA Intercalators

Silvia Cauteruccio; Cristina Bartoli; Claudio Carrara; Davide Dova; Cesare Errico; Giulia Ciampi; Dinuccio Dinucci; Emanuela Licandro; Federica Chiellini

doi:10.1002/cplu.201402347

A Nanostructured PLGA System for Cell Delivery of a Tetrathiahelicene as a Model for Helical DNA Intercalators

Chempluschem. 2015 Mar;80(3):490-493. doi: 10.1002/cplu.201402347. Epub 2014 Dec 4.

Authors

Silvia Cauteruccio¹, Cristina Bartoli², Claudio Carrara¹, Davide Dova¹, Cesare Errico², Giulia Ciampi², Dinuccio Dinucci², Emanuela Licandro¹, Federica Chiellini²

Affiliations

¹ Dipartimento di Chimica, Università degli Studi di Milano, via Golgi 19, I-20133 Milano (Italy).
² Department of Chemistry and Industrial Chemistry, University of Pisa, Via Giuseppe Moruzzi 3, 56124 Pisa (Italy).

PMID: 31973409
DOI: 10.1002/cplu.201402347

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.

Keywords: DNA intercalators; cell uptake; drug delivery; poly(lactic-co-glycolic acid); tetrathiahelicenes.