Abstract
DESIGN AND EVALUATION OF TOLTERODINE TARTARATE TRANSDERMAL DELIVERY SYSTEMS: ENHANCEMENT OF PERMEABILITY VIA PHYSICAL AND CHEMICAL TECHNIQUES

Dr. Shayeda*, D. Rajani, D. Sathish and Nusrat Ayesha

ABSTRACT

The aim of the present investigation was to develop transdermal patches of Tolterodine tartarate(TT) and improve the permeation using physical (Iontophoresis) and chemical (d-Limonene) permeation enhancement techniques.The matrix type transdermal patches of TT were prepared using solvent casting technique. Ten formulations(composed of Hydroxy propyl methyl cellulose(HPMC) in the ratios of 1:12.5,1:10 and 1:15 in the formulations F1,F2 & F3, HPMC and Eudragit RL100 in the ratios of 4:4, 5:3, 6:2 and 7:1 in the formulations F4, F6, F7 & F9 and HPMC and Eudragit RS 100 in the ratios of 5:3, 6:2 & 7:1 in the formulations F5, F8 & F10)were prepared. In all formulations 17% PEG 400 was used as plasticizer. All formulations were evaluated for in-vitro release studies, water absorption, water content, water vapor transmission rate studies (WVTR) and Mechanical properties. The physicochemical interaction between TT and polymers were investigated by Differential Scanning Calorimetry (DSC).Effect of different concentrations of d-Limonene (6%, 8% and 10%), different current densities (0.075, 0.15 & 0.3 mA/cm2) and combination of both the techniques on the optimized formulations were studied through ex-vivo permeation studies.The maximum drug release was obtained in the formulations F1 (72.72% in 12 hrs), F9 (81.69% in 24hrs) and F10 (73.95% in 24hrs). These formulations were used in further experiments for the improvement of flux. Little improvement in the flux (F1 (Control: 30.79μg/hr/cm2, d-Limonene: 46.36 μg/hr/cm2), F9 (Control: 28.02 μg/hr/cm2, d-Limonene:53.24μg/hr/cm2) and F10 (Control:25.60μg/hr/cm2, d-Limonene:39.44 μg/hr/cm2 )was observed with 8% of d-Limonene. Significant improvement in flux was obtained with iontophoresis using 0.15mA/cm2 (F1:167.12 μg/hr/cm2, F9:114.34 μg/hr/cm2 & F10:55.72 μg/hr/cm2). Required flux (260 μg/hr/cm2) was obtained with combination of both the techniques in the formulations F1: 253.28 μg/hr/cm2 & F9: 177.50 μg/hr/cm2.

Keywords: Tolterodine tartarate, iontophoresis, d-Limonene, transdermal patch.


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