title: Semisolid formulations containing cetirizine: human skin permeation and topical antihistaminic evaluation in a rabbit model.
abstract: Cetirizine dihydrochloride (CTZ) is a second-generation histamine H1 antagonist, effective for the treatment of a wide range of allergic diseases. It has been utilized for managing the symptoms of chronic urticaria and atopic skin conditions. Thus, two novel semisolid formulations, nanoemulsion (NE) and hydrogel (HG) were developed to study their potential utility as vehicles including cetirizine (CTZ) and evaluate the potential use as topical H1-antihistamines agents. The physicochemical and stability properties of both vehicles were tested. Drug release kinetics and human skin permeation studies were performed using Franz cells. The antihistaminic activity was assayed in New Zealand rabbits and compared with two commercial first generation antihistamines. Both formulations were stable and provided a sustained drug release. Amounts of CTZ remaining in the skin were higher for HG, showing the maximum biological effect at 30 min, similar to topical first generation H1-antihistamines commercially available. These results suggest that CTZ-HG could be a promising system for the treatment of topical allergy bringing rapid antihistaminic relief.
authors.affiliation: Biopharmaceutical and Pharmacokinetics Unit, School of Pharmacy, University of Barcelona, Av. Joan XXIII, 08028, Barcelona, Spain.
authors.forename: Claudia
authors.initials: C
authors.lastname: Ciurlizza
authors.forename: Francisco
authors.initials: F
authors.lastname: Fernández
authors.forename: Ana Cristina
authors.initials: AC
authors.lastname: Calpena
authors.forename: Raquel
authors.initials: R
authors.lastname: Lázaro
authors.forename: Alexander
authors.initials: A
authors.lastname: Parra
authors.forename: Beatriz
authors.initials: B
authors.lastname: Clares
mesh_terms: D000287:Administration, Topical; D000818:Animals; D002478:Cells, Cultured; D017332:Cetirizine / Q000008:administration & dosage* / Q000009:adverse effects; D004655:Emulsions; D039563:Histamine H1 Antagonists, Non-Sedating / Q000008:administration & dosage* / Q000009:adverse effects; D006801:Humans; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate / Q000008:administration & dosage*; D008297:Male; D049329:Nanostructures / Q000008:administration & dosage*; D011817:Rabbits; D012869:Skin Absorption / Q000187:drug effects*
chemical_list: D004655:Emulsions; D039563:Histamine H1 Antagonists, Non-Sedating; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate; D017332:Cetirizine