API-2

Drug Delivery Systems Based on Pluronic Micelles with Antimicrobial Activit

Bacterial oral infections are typically chronic and require effective treatment strategies, including appropriate drug administration routes and dosing regimens. However, the growing challenge of multidrug-resistant microorganisms poses a significant threat to global healthcare. In this study, the commercial amphiphilic copolymer Pluronic F127 was employed to encapsulate a novel active pharmaceutical ingredient (API), 1-(5′-nitrobenzimidazole-2′-yl-sulphonyl-acetyl)-4-aryl-thiosemicarbazide, previously synthesized and characterized by our group. Encapsulation was performed at various copolymer/API weight ratios.
The resulting micellar formulations had particle sizes of approximately API-2 20 nm and remained stable for at least 30 days at 4 °C, showing no significant increase in Z-average size. Encapsulation and drug loading efficiencies varied with the copolymer/API ratio, with the highest values—84.8% and 11.1%, respectively—achieved at a 10:1 ratio. In vitro assays confirmed that the polymeric micelles (PMs) were both hemocompatible and cytocompatible. Notably, the formulation with a 2:1 copolymer/API ratio exhibited enhanced antibacterial activity, with inhibition zones of 36 mm against Staphylococcus aureus and 20 mm against Escherichia coli.
These promising findings suggest that the developed micellar systems represent a viable and effective alternative for treating bacterial oral infections, with potential for both injectable and topical applications.