A multi-microcarrier of metronidazole-biopolymers complexes as a potential vaginal delivery system

ABSTRACT

The advantages of multiparticulate carriers over monolithic one are well known. In this study, mucoadhesive micropellets (MPs) composed of metronidazole (MTZ)–polysaccharide(s) polyelectrolytes complexes were prepared to be used as a localized vaginal healthcare product. The prepared all-natural MPs were characterized using FTIR spectroscopy as well as scanning electron microscopy studies. The MPs were evaluated by determination of drug encapsulation efficiency (EE), particle size (PS), drug release parameters, and ex vivo bioadhesivity using vaginal mucosa. MP-D composed of (MTZ:alginate:polycarbophil = 1:0.5:0.5) attained the highest EE (97.67%) as well as the most extended drug release properties. Microbiological study comparing MP-D to the market product (Amrizole vaginal suppository) showed the superiority of MP-D by its capability to constantly inhibit fungal growth all-over 24 h, while Amrizole suppository was effective for only 8 h.

GRAPHICAL ABSTRACT

KEYWORDS:

• Antifungal
• biopolymers
• micropellets
• mucoadhesion
• vaginal