Influence of different formulation variables on the performance of transdermal drug delivery system containing tizanidine hydrochloride: in vitro and ex vivo evaluations

  • Maryam Shabbir The University of Lahore. Faculty of Pharmacy
  • Sajid Ali The University of Lahore. Faculty of Pharmacy
  • Irfan Hamid The University of Lahore. Faculty of Pharmacy
  • Ali Sharif The University of Lahore. Faculty of Pharmacy
  • Muhammad Furqan Akhtar The University of Lahore. Faculty of Pharmacy
  • Moosa Raza The University of Lahore. Faculty of Pharmacy
  • Shoaib Ahmed The University of Lahore. Faculty of Pharmacy
  • Sohaib Peerzada The University of Lahore. Faculty of Pharmacy
  • Muhammad Umair Amin The University of Lahore. Faculty of Pharmacy
Keywords: Ex-vivo permeation, Eudragit L100, Permeation enhances, Transdermal matrix patch, Monolithic system

Abstract

The present study was aimed at preparation of transdermal patches of tizanidine HCl, evaluation of the effect of polymers on in vitro release pattern of the drug, and the effect of permeation enhancers on the penetration of the drug through the rabbit skin. Various proportions of hydrophilic (HPMC) and hydrophobic (Eudragit L-100) polymers were used with PEG 400 as film-forming agent, and Span 20 or DMSO as permeation enhancer. The formulations were assessed for physicochemical characteristics and in vitro drug release studies using USP paddle over disc method in phosphate buffered saline (pH 7.4) at 32.0±1°C. On the basis of in vitro studies and physicochemical evaluations, S03-A and S04-A were selected at Eudragit : HPMC ratios of 8 : 2 and 7 : 3, respectively, for further ex vivo analysis. The effects of different concentrations of Span 20 and DMSO were evaluated on excised rabbit skin using Franz diffusion cell. Cumulative drug permeation, flux, permeability coefficient, target flux, and enhancement ratio were calculated and compared with the control formulations. Kinetic models and Tukey’s multiple comparison test were applied to evaluate the drug release patterns. Formulation SB03- PE containing Eudragit L-100:HPMC (7:3) with Span 20 (15% w/w) produced the highest enhancement in drug permeation, and followed zero order kinetic model with super case-II drug release mechanism.

Downloads

Download data is not yet available.
Published
2018-12-20
How to Cite
Shabbir, M., Ali, S., Hamid, I., Sharif, A., Akhtar, M., Raza, M., Ahmed, S., Peerzada, S., & Amin, M. (2018). Influence of different formulation variables on the performance of transdermal drug delivery system containing tizanidine hydrochloride: in vitro and ex vivo evaluations. Brazilian Journal of Pharmaceutical Sciences, 54(4), e00130. https://doi.org/10.1590/s2175-97902018000400130
Section
Articles