title: Comparative evaluation of rivastigmine permeation from a transdermal system in the Franz cell using synthetic membranes and pig ear skin with in vivo-in vitro correlation.
abstract: In the present study, in vitro permeation experiments in a Franz diffusion cell were performed using different synthetic polymeric membranes and pig ear skin to evaluate a rivastigmine (RV) transdermal drug delivery system. In vitro-in vivo correlations (IVIVC) were examined to determine the best model membrane. In vitro permeation studies across different synthetic membranes and skin were performed for the Exelon(®) Patch (which contains RV), and the results were compared. Deconvolution of bioavailability data using the Wagner-Nelson method enabled the fraction of RV absorbed to be determined and a point-to-point IVIVC to be established. The synthetic membrane, Strat-M™, showed a RV permeation profile similar to that obtained with pig ear skin (R(2)=0.920). Studies with Strat-M™ resulted in a good and linear IVIVC (R(2)=0.991) when compared with other synthetic membranes that showed R(2) values less than 0.90. The R(2) for pig ear skin was 0.982. Strat-M™ membrane was the only synthetic membrane that adequately simulated skin barrier performance and therefore it can be considered to be a suitable alternative to human or animal skin in evaluating transdermal drug transport, potentially reducing the number of studies requiring human or animal samples.
authors: Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro, Av. Carlos Chagas Filho, 373, CCS, Bss, sl15, Rio de Janeiro, RJ, 21941-902, Brazil.
authors: Alice
authors: A
authors: Simon
authors: School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Dublin 2, Ireland.
authors: Maria Inês
authors: MI
authors: Amaro
authors: School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Dublin 2, Ireland.
authors: Anne Marie
authors: AM
authors: Healy
authors: Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro, Av. Carlos Chagas Filho, 373, CCS, Bss, sl15, Rio de Janeiro, RJ, 21941-902, Brazil.
authors: Lucio Mendes
authors: LM
authors: Cabral
authors: Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro, Av. Carlos Chagas Filho, 373, CCS, Bss, sl15, Rio de Janeiro, RJ, 21941-902, Brazil. Electronic address: valeria@pharma.ufrj.br.
authors: Valeria Pereira
authors: VP
authors: de Sousa
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D004431:Ear, External / Q000378:metabolism*; D066298:In Vitro Techniques; D008567:Membranes, Artificial; D010539:Permeability; D000068836:Rivastigmine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption; D013552:Swine; D057968:Transdermal Patch
chemical_list: D008567:Membranes, Artificial; D000068836:Rivastigmine
keywords: Franz diffusion cell; In vivo-in vitro correlation; Permeation; Point-to-point IVIVC; Rivastigmine; Strat-M™; Synthetic membrane; Transdermal drug delivery system