Preparation and characterization of Luteolin-loaded MPEG-PCL-g-PEI micelles for oral Candida albicans infection

Abstract Candida albicans (C. albicans) is one of the most common opportunistic pathogens in the infection disease, which always invades the oral cavities of people with low immune function and brings huge suffering to the patients. In this research, Luteolin (Lu)/monomethoxy poly (ethylene glycol)-poly (epsilon-caprolactone)-graft-polyethyleneimine (MPEG-PCL-g-PEI, MPP) micelles was prepared with improved aqueous solubility of Lu. The micelles were spherical shape, nano-sized and stably dispersed with high DL% (15.8% ± 0.3%) and EE% (97.3% ± 1.1%). In vitro, Lu/MPP micelles were slowly released in pH 5.8 solution and followed the Higuchi equation. The buccal tablets containing Lu/MPP micelles were prepared with acceptable relative parameters (weight variation, hardness, friability values). In vitro release of the buccal tablets was measured in the designed dissolution rate test apparatus and the release rate of buccal tablets could be sustained for 8 h. In vivo histopathological data demonstrated that Lu/MPP micelles had no discernible effects on the buccal mucosa of the rats. In addition, Lu/MPP micelles could significantly enhance the antifungal activity of Lu against both planktonic and biofilm state of C. albicans. This research may provide more theoretical and experimental basis for the development and application of Lu for the treatment of oral C. albicans infection.