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.
Highlights
Trifluoperazine (TFP) is an antipsychotic drug; it is widely used to treat psychotic conditions of acute and chronic schizophrenia, since 1950s
The formulations were prepared by solvent casting method varying the ratio of Polyvinyl pyrrolidone (PVP): ethyl cellulose (EC)
The infrared spectrum of PVP is characterized by a strong C=O absorption peak from the amide group of PVP at 1650 cm-1, C–N group appeared at 1287 cm-1, C–H stretching and bending vibrations were observed at 2800-3000 and 1420-1460 cm-1, respectively
Summary
Trifluoperazine (TFP) is an antipsychotic drug; it is widely used to treat psychotic conditions of acute and chronic schizophrenia, since 1950s. TFP still remains to be an inexpensive and widely used drug in the management of schizophrenia and anxiety. Psychiatric disorders often demand long term drug treatment, and compliance with the prescribed medication is a severe issue for mental illness people. Nonadherence to prescribed medication in psychiatric patients is mainly due to factors like undesirable side effects, dosing regimen, route of administration, nature of illness, belief systems and personal attributes [3]. The approach of developing antipsychotics in the form of a sustained release transdermal patch is promising as the occurrence of non compliance with medication and relapse is high in patients with mental illness [3]
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