Avaliação da permeação cutânea de 3OMQ isolada por HPCCC e incorporada em hidrogéis contendo diferentes ciclodextrinas

Abstract

The use of formulations for topical delivery is an excellent option for cutaneous therapy, especially for the treatment of infections caused by the Herpes Simplex virus (HSV-1). In this context, 3OMQ is a natural methoxyflavonoid with low solubility and pronounced antiviral activity. In this work, 3OMQ was isolated from the enriched flavonoid-aglycones fraction (FEF) of Achyrocline satureioides inflorescences by high performance countercurrent chromatography (HPCCC) to evaluate its cutaneous permeation from HPMC hydrogels containing the HP--CD, -CD and -CD. Permeation studies were performed using Franz type diffusion cells and revealed that the 3OMQ hydrogel in the absence of cyclodextrins obtained greater retention and permeation in the skin (6,71 μg/cm² in the stratum corneum, 0,98 μg/cm² in the epidermis and 1,62 μg/cm² in the dermis). 1H-NMR analysis and 2D-ROESY contour maps were performed suggesting inclusion complex formation between 3OMQ and cyclodextrins HP--CD and -CD, but not for -CD. Thus, the 3OMQ/HP--CD and 3OMQ/-CD formulations which showed complex formation, released less 3OMQ in cutaneous permeation studies. In the 3OMQ/-CD formulation, 3OMQ probably has been retained in the association of -CD with HPMC hydrophilic matrix, which also decrease its release from the hydrogel. Thus, cyclodextrins revealed a negative effect on 3OMQ permeation.