Nitric oxide-releasing cyclodextrins as biodegradable antibacterial scaffolds: a patent evaluation of US2019343869(A1)

Introduction: Antimicrobial resistance is one of the major scourges for healthcare worldwide, therefore novel investigational approaches are needed to potentiate and preserve the current antibacterial arsenal. Cyclodextrins are known to improve the formulability of several different therapeutic agents. When functionalized with nitric oxide (NO) releasing groups, and suitably loaded with an antibacterial or antitumoral agents, they can exert additive activity especially toward certain bacterial strains and cell cancer lines.

Areas covered: US2019343869 describes a NO-releasing cyclodextrins, a method for their synthesis, a composition that is based on them and their application as anticancer or antibacterial agents, especially toward planktonic P. aeruginosa and the biofilm resulting from infection. Anticancer activity is measured against A549 cells. The amount of NO released is in the range of 0.5 μmol to 2.5 μmol per milligram of functionalized cyclodextrin with a half-life for NO release in a range of between about 0.7-4.2 hours.

Expert opinion: The results support the use of NO-releasing cyclodextrins as matrix for the delivery of antibacterial and anticancer drugs in a suitable formulation. However, antibacterial activity seems to be weak and more focused studies are needed.

Pieroni M: Affiliations expandNitric oxide-releasing cyclodextrins as biodegradable antibacterial scaffolds: a patent evaluation of US2019343869(A1). Expert Opin Ther Pat . 2020 Sep 9. https://doi.org/10.1080/13543776.2020.1822328..