Cyclodextrin-based nanosponges for the targeted delivery of the anti-restenotic agent DB103: A novel opportunity for the local therapy of vessels wall subjected to percutaneous intervention

Abstract

Nano-sized colloidal carriers represent innovative drug delivery systems, as they allow a targeted and prolonged release of poorly water-soluble drugs, improving their bioavailability and modifying their pharmacokinetic parameters. In this work we describe cyclodextrin-based nanosponges, obtained through polimerization of β-cyclodextrin with diphenyl carbonate as the cross-linking agent, loaded with a novel multi-effective heterocyclic compound, DB103, able to regulate key cellular events involved in the remodelling of vessels wall. Fabrication and drug-loading procedures, as well as physical-chemical characterization and drug-release profile of the novel colloidal system are reported. Results achieved demonstrate the ability of nanosponges to enclose efficiently the target drug and release it slowly and continuously, thus suggesting the exploitability of the novel system for the local therapy of vessels wall subjected to percutaneous intervention.

Keywords: 2-(3,4-Dimethoxyphenyl)-3-phenyl-4H-pyrido [1,2-a]pyrimidin-4-one.; 2-(3,4-Dimethoxyphenyl)-3-phenyl-4H-pyrido[1,2-a]pyrimidin-4-one (Scheme 1); Cardiovascular diseases; Diphenylcarbonate (PubChem CID: 7597); Drug-eluting stent; β-Cyclodextrin; β-Cyclodextrin (PubChem CID: 70702285); β-Cyclodextrin-based nanosponge.