title: Inhibition of skin inflammation by baicalin ultradeformable vesicles.
abstract: The topical efficacy of baicalin, a natural flavonoid isolated from Scutellaria baicalensis Georgi, which has several beneficial properties, such as antioxidative, antiviral, anti-inflammatory and antiproliferative, is hindered by its poor aqueous solubility and low skin permeability. Therefore, its incorporation into appropriate phospholipid vesicles could be a useful tool to improve its local activity. To this purpose, baicalin at increasing concentrations up to saturation, was incorporated in ultradeformable vesicles, which were small in size (∼67nm), monodispersed (PI<0.19) and biocompatible, regardless of the concentration of baicalin, as confirmed by in vitro studies using fibroblasts. On the other hand, transdermal flux through human epidermis was concentration dependent. The in vivo results showed the significant anti-inflammatory activity of baicalin loaded nanovesicles irrespective of the concentration used, as they were able to reduce the skin damage induced by the phorbol ester (TPA) application, even in comparison with dexamethasone, a synthetic drug with anti-inflammatory properties. Overall results indicate that ultradeformable vesicles are promising nanosystems for the improvement of cutaneous delivery of baicalin in the treatment of skin inflammation.
authors.affiliation: Dept. Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Valencia, Spain. Electronic address: silmirpa@gmail.com.
authors.forename: Silvia
authors.initials: S
authors.lastname: Mir-Palomo
authors.affiliation: Dept. Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Valencia, Spain; Institute of Molecular Recognition and Technological Development, Inter-Universitary Institute from Polytechnic University of Valencia and University of Valencia, Spain.
authors.forename: Amparo
authors.initials: A
authors.lastname: Nácher
authors.affiliation: Dept. Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Valencia, Spain; Institute of Molecular Recognition and Technological Development, Inter-Universitary Institute from Polytechnic University of Valencia and University of Valencia, Spain.
authors.forename: Octavio
authors.initials: O
authors.lastname: Díez-Sales
authors.affiliation: Dept. Physics and Chemistry, Faculty of Pharmacy, University of Valencia, Spain.
authors.forename: M A
authors.initials: MA
authors.lastname: Ofelia Vila Busó
authors.affiliation: Dept. Farmaco Chimico Tecnologico, University of Cagliari, Cagliari 09124, Italy.
authors.forename: Carla
authors.initials: C
authors.lastname: Caddeo
authors.affiliation: Dept. Farmaco Chimico Tecnologico, University of Cagliari, Cagliari 09124, Italy.
authors.forename: Maria Letizia
authors.initials: ML
authors.lastname: Manca
authors.affiliation: Dept. Farmaco Chimico Tecnologico, University of Cagliari, Cagliari 09124, Italy.
authors.forename: Maria
authors.initials: M
authors.lastname: Manconi
authors.affiliation: Dept. Farmaco Chimico Tecnologico, University of Cagliari, Cagliari 09124, Italy.
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Fadda
authors.affiliation: Dept. of Pathology, University of Valencia, Avda Blasco Ibañez 17, 46010 Valencia, Spain.
authors.forename: Amparo Ruiz
authors.initials: AR
authors.lastname: Saurí
mesh_terms: D016475:3T3 Cells; D000279:Administration, Cutaneous; D000328:Adult; D000818:Animals; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D003872:Dermatitis / Q000188:drug therapy* / Q000378:metabolism* / Q000473:pathology; D004337:Drug Carriers / Q000008:administration & dosage / Q000378:metabolism; D005260:Female; D005419:Flavonoids / Q000008:administration & dosage* / Q000378:metabolism*; D006801:Humans; D051379:Mice; D008875:Middle Aged; D012869:Skin Absorption / Q000187:drug effects* / Q000502:physiology
chemical_list: D004337:Drug Carriers; D005419:Flavonoids; C038044:baicalin
keywords: Baicalin; Mice; Skin; Topical delivery; Ultradeformable vesicles