title: Activity and stability studies of verbascoside, a novel antioxidant, in dermo-cosmetic and pharmaceutical topical formulations.
abstract: We here report the results of our investigations carried out on verbascoside, a phenylpropanoid glycoside known for its antioxidant, anti-inflammatory and photoprotective actions. Verbascoside was obtained from Buddleia davidii meristematic cells, obtained in turn using a sustainable biotechnology platform which employs an in vitro plant cell culture technology. Verbascoside was first investigated to assess the behaviour of the active ingredient in solution or in finished preparations, in view of its potential topical use, especially in skin protection. Stability studies were performed by HPLC, and a PCL assay was adopted to determine the radical scavenging activity toward superoxide anion. The high hydrophilic character of verbascoside, suggested in a somewhat limited range of possible applications, leading us to explore its derivatization to obtain the semi-synthetic derivative VPP, an acyl derivative of verbascoside, with an improved range of applications due to its lower hydrophilic profile. Alone, VPP revealed increased antioxidant activity, both as an active ingredient and in dermocosmetic preparations. Stability studies showed a greater stability of VPP in lipophilic vehicles, whereas the parent verbascoside proved more stable in an O/W emulsions. Verbascoside was also stable in suppositories, an interesting pharmaceutical form for possible applications in treatment of inflammation of the intestinal mucosa.
authors.affiliation: Department of Pharmaceutical Sciences, University of Ferrara, Via Fossato di Mortara 17-19, 44121 Ferrara, Italy. vrs@unife.it
authors.forename: Silvia
authors.initials: S
authors.lastname: Vertuani
authors.forename: Erika
authors.initials: E
authors.lastname: Beghelli
authors.forename: Emanuela
authors.initials: E
authors.lastname: Scalambra
authors.forename: Gemma
authors.initials: G
authors.lastname: Malisardi
authors.forename: Stefano
authors.initials: S
authors.lastname: Copetti
authors.forename: Roberto
authors.initials: R
authors.lastname: Dal Toso
authors.forename: Anna
authors.initials: A
authors.lastname: Baldisserotto
authors.forename: Stefano
authors.initials: S
authors.lastname: Manfredini
mesh_terms: D000287:Administration, Topical; D000975:Antioxidants / Q000737:chemistry / Q000494:pharmacology; D032861:Buddleja / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002851:Chromatography, High Pressure Liquid; D003358:Cosmetics / Q000737:chemistry / Q000494:pharmacology; D004355:Drug Stability; D004655:Emulsions / Q000737:chemistry / Q000494:pharmacology; D005079:Excipients / Q000737:chemistry; D005960:Glucosides / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007249:Inflammation / Q000188:drug therapy / Q000473:pathology; D007413:Intestinal Mucosa / Q000187:drug effects / Q000473:pathology; D049449:Luminescence; D008163:Luminescent Measurements; D010636:Phenols / Q000737:chemistry / Q000494:pharmacology; D012867:Skin / Q000187:drug effects / Q000473:pathology; D012871:Skin Diseases / Q000188:drug therapy / Q000473:pathology; D012995:Solubility; D013481:Superoxides / Q000037:antagonists & inhibitors / Q000378:metabolism; D013488:Suppositories / Q000737:chemistry; D059808:Polyphenols
chemical_list: D000975:Antioxidants; D003358:Cosmetics; D004655:Emulsions; D005079:Excipients; D005960:Glucosides; D010636:Phenols; D013481:Superoxides; D013488:Suppositories; C058956:acteoside; D059808:Polyphenols