Journal of Pharmaceutical Sciences, Early View
This work describes the preparation and characterization of mucoadhesive
thermoresponsive systems consisted of poloxamer 407 (P407), Carbopol® 934P
(C934P), and propolis to treat vulvovaginal candidiasis (VVC).
Systems were obtained with different percentages of P407 and
C934P to deliver propolis, a potent drug against VVC. Temperature of gelation,
hardness, compressibility, adhesiveness, elasticity, cohesiveness,
mucoadhesion, rheology (continuous flow and oscillatory), in vitro drug release,
and antimicrobial activity were evaluated. Increasing the polymer content or
temperature and the drug presence significantly increased mechanical properties
of formulations. These exhibited pseudoplastic flow and low degrees of
thixotropy.
In most samples, increasing the C934P content significantly
changed the oscillatory rheological properties. Formulations showed
thermoresponsive behavior, existing as a liquid at room temperature and gel at
34°C–37°C. Propolis release from formulations was controlled by phenomenon of
relaxation of polymer chains or displayed anomalous behavior, dependent of
concentration of each polymer.
The in vitro antimicrobial activity of preparations was
evaluated against microorganisms of vaginal importance (Candida albicans,
Candida glabrata, Candida parapsilosis, Candida tropicalis, and Saccharomyces
cerevisiae), displaying activity against all yeast tested.
The data obtained for these systems indicate a potentially
useful role in the treatment of VVC and suggest they are worthy of clinical
evaluation.
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