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 prolonged release of coumarin contained in the phytocomplex. Two types of methacrylic patches (patch 1 based on a blend of Eudragit E100 and Eudragit NE; patch 2 based on Eudragit L100) were prepared. Both patches were equivalent in terms of coumarin release and ex vivo skin permeation profiles. The two patches 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 melilot extract with analogous patches containing synthetic coumarin, no melilot phytocomplex enhancer effect was shown. The data of the ex vivo coumarin skin permeation and those obtained by the in vivo stripping technique showed a good correlation (r(2)=0.9727 for patch 1, r(2)=0.9835 for patch 2).
Minghetti
P
P
Istituto di Chimica Farmaceutica e Tossicologica, Università degli Studi di Milano, Viale Abruzzi 42, 20131, Milan, Italy. paola.minghetti@unimi.it
Casiraghi
A
A
Cilurzo
F
F
Montanari
L
L
D000268:Adhesiveness; D000287:Administration, Topical; D000328:Adult; D002851:Chromatography, High Pressure Liquid; D003374:Coumarins / Q000494:pharmacology*; D004338:Drug Combinations; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D010936:Plant Extracts / Q000494:pharmacology*; D012116:Resins, Plant / Q000494:pharmacology*; D012431:Rutin / Q000494:pharmacology*; D012869:Skin Absorption / Q000187:drug effects*; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet
D003374:Coumarins; D004338:Drug Combinations; D010936:Plant Extracts; D012116:Resins, Plant; D012431:Rutin; C001157:coumarin, resin, rutin, volatile oil drug combination