Mucoadhesive polyelectrolyte complexes of fucoidan and chitin nanowhiskers to prolong the antiprotozoal activity of metronidazole

Abstract

The improvement of the specific pharmacological activity of agents with antimicrobial and antiprotozoal properties (e.g. metronidazole, MET) is of interest for clinical applications in the treatment of bacterial infections. In this work, we prepared the polyelectrolyte complexes (PEC) based on chitin nanowhiskers (CNW) and fucoidan (FUC) with hydrodynamic diameters of 244 and 816 nm, a ζ-potential of about −22 mV and good mucoadhesive properties. The incorporation of MET into PEC particles promoted the sustained release of MET for 10 h and maintained the antiprotozoal activity against clinical isolates of Trichomonas vaginalis for up to 10 h. At concentrations of 1–3 mg/mL, the CWN-FUC-MET particles showed no cytotoxicity (HeLa cell line). The sustained drug release rate, combined with pronounced mucoadhesive properties, improved pharmacological activity, and non-cytotoxicity makes the developed biopolymer delivery systems promising candidates for further clinical trials.