Development of local patches containing melilot extract and ex vivo-in vivo evaluation of skin permeation

Melilot extract could be effective in treating localised varicose syndrome or capillary fragility. The monolayer patch was selected to obtain a prolon ged release of coumarin contained in the phytocomplex. Two types of methacr ylic patches (patch 1 based on a blend of Eudragit E100 and Eudragit NE; pa tch 2 based on Eudragit L100) were prepared. Both patches were equivalent i n terms of coumarin release and ex vivo skin permeation profiles. The two p atches differed significantly as regards respective adhesive properties. At low peel rate only patch 1 showed adhesive failure as confirmed by the in vivo performance. When comparing the behaviour of the patches containing me lilot extract with analogous patches containing synthetic coumarin, no meli lot phytocomplex enhancer effect was shown. The data of the ex vivo coumari n skin permeation and those obtained by the in vivo stripping technique sho wed a good correlation (r(2)=0.9727 for patch 1, r(2)=0.9835 for patch 2). (C) 2000 Elsevier Science B.V. All rights reserved.