Preparation and characterization of trifluoperazine loaded transdermal patches for sustained release

Abstract

Objective: The purpose of the present study was to formulate and evaluate the polymeric transdermal delivery system of antipsychotic drug Trifluoperazine (TFP) for sustained drug release. Methods: A transdermal patch loaded with (TFP) was formulated by solvent casting technique. Polyvinyl pyrrolidone (PVP) K-30 and ethyl cellulose (EC) was used as a polymeric matrix with different ratios. Di n-butyl phthalate was used as a plasticizer. The parameters such as thickness, folding endurance and weight variation of the prepared patches were studied. The interaction study by attenuated total reflectance-infrared (ATR-IR) spectroscopy, X-ray diffraction and thermal analysis by differential scanning calorimetry (DSC) were performed. In vitro drug release study was performed by modified paddle over-disc technique. Results: The infrared spectroscopic study confirmed the absence of any chemical interaction between TFP and selected polymers. All the prepared formulations showed folding endurance values ranging from 130-162 and a satisfactory drug loading of 90-95%. In in vitro drug release study, formulations PE-3 and PE-4 exhibited a sustained and stable cumulative release of 54 % and 48% respectively, at the end of 24 h. The DSC and XRD analysis proved the partial conversion of the drug from crystalline to amorphous form when integrated into the polymeric matrix. Conclusion: The prepared transdermal formulations using polymers PVP and ethyl cellulose demonstrated their ability to sustain the release of TFP. The developed formulation could be exploited for multiday therapy of TFP for the effective treatment of schizophrenia with a simplified dosing regimen and enhanced patient compliance.