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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.
Int J Pharm 2016; 512(1):234-241IJ

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+Show Affiliations

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.School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Dublin 2, Ireland.School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Dublin 2, Ireland.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.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.

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

27568498

Citation

Simon, Alice, et al. "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." International Journal of Pharmaceutics, vol. 512, no. 1, 2016, pp. 234-241.
Simon A, Amaro MI, Healy AM, et al. 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. Int J Pharm. 2016;512(1):234-241.
Simon, A., Amaro, M. I., Healy, A. M., Cabral, L. M., & de Sousa, V. P. (2016). 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. International Journal of Pharmaceutics, 512(1), pp. 234-241. doi:10.1016/j.ijpharm.2016.08.052.
Simon A, et al. 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. Int J Pharm. 2016 Oct 15;512(1):234-241. PubMed PMID: 27568498.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - 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. AU - Simon,Alice, AU - Amaro,Maria Inês, AU - Healy,Anne Marie, AU - Cabral,Lucio Mendes, AU - de Sousa,Valeria Pereira, Y1 - 2016/08/26/ PY - 2016/05/25/received PY - 2016/08/18/revised PY - 2016/08/24/accepted PY - 2016/8/30/entrez PY - 2016/8/30/pubmed PY - 2017/7/5/medline KW - Franz diffusion cell KW - In vivo-in vitro correlation KW - Permeation KW - Point-to-point IVIVC KW - Rivastigmine KW - Strat-M™ KW - Synthetic membrane KW - Transdermal drug delivery system SP - 234 EP - 241 JF - International journal of pharmaceutics JO - Int J Pharm VL - 512 IS - 1 N2 - 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. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/27568498/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_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(16)30802-X DB - PRIME DP - Unbound Medicine ER -