4.7 Article

A curcumin-loaded liquid crystal precursor mucoadhesive system for the treatment of vaginal candidiasis

Journal

INTERNATIONAL JOURNAL OF NANOMEDICINE
Volume 10, Issue -, Pages 4815-4824

Publisher

DOVE MEDICAL PRESS LTD
DOI: 10.2147/IJN.S82385

Keywords

nanostructured drug delivery systems; liquid crystalline systems; mucoadhesive polymers; vaginal administration; Candida albicans

Funding

  1. Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP)
  2. Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq)
  3. Programa de Apoio ao Desenvolvimento Cientifico (PADC)

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Women often develop vaginal infections that are caused primarily by organisms of the genus Candida. The current treatments of vaginal candidiasis usually involve azole-based anti-fungals, though fungal resistance to these compounds has become prevalent. Therefore, much attention has been given to molecules with antifungal properties from natural sources, such as curcumin (CUR). However, CUR has poor solubility in aqueous solvents and poor oral bioavailability. This study attempted to overcome this problem by developing, characterizing, and evaluating the in vitro antifungal action of a CUR-loaded liquid crystal precursor mucoadhesive system (LCPM) for vaginal administration. A low-viscosity LCPM (F) consisting of 40% wt/wt polyoxpropylene(5)-polyoxyethylene-(20)-cetyl alcohol, 50% wt/wt oleic acid, and 10% wt/wt chitosan dispersion at 0.5% with the addition of 16% poloxamer 407 was developed to take advantage of the lyotropic phase behavior of this formulation. Notably, F could transform into liquid crystal systems when diluted with artificial vaginal mucus at ratios of 1: 3 and 1: 1 (wt/wt), resulting in the formation of F30 and F100, respectively. Polarized light microscopy and rheological studies revealed that F behaved like an isotropic formulation, whereas F30 and F100 behaved like an anisotropic liquid crystalline system (LCS). Moreover, F30 and F100 presented higher mucoadhesion to porcine vaginal mucosa than F. The analysis of the in vitro activity against Candida albicans revealed that CUR-loaded F was more potent against standard and clinical strains compared with a CUR solution. Therefore, the vaginal administration of CUR-loaded LCPMs represents a promising platform for the treatment of vaginal candidiasis.

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