Abstract
Objective: The objective of the study was to prepare simvastatin transdermal films for the treatment of atherosclerosis and to evaluate the effect of concentration of polymer on penetration enhancement.Methods: Solvent evaporation technique was employed for the preparation of films and the prepared films were evaluated for various physicochemical properties of films such as tensile strength, thickness, surface pH, swellability, drug content, moisture content and folding endurance. In vitro drug, release study and release kinetics were also studied.Results: Tensile strength ranged from 3.56±0.343 to 4.56±0.12 (N/mm²). The films were of uniform weight. Thickness varied from 0.2±0.3 mm to 0.2±0.8 mm. Surface pH ranged from 6.6±0.14 to 6.9±0.16. Percentage swellability ranged from12.1±0.36 to 16.3±0.22. Percentage drug content ranged from 88.4±0.7% to 90.5±0.6% in all the formulation. Percentage moisture content ranged from 0.864 to 1.03%. Moisture uptake was from 2.6±0.24 to 2.9±0.072. The folding endurance test gave satisfactory results and F3 formulation showed maximum drug release.Conclusion: From the study, it was concluded that out of various formulations, the F3 formulation was found to be the optimum formulation with 88% drug release at the fourteenth hour.Keywords: Simvastatin, Transdermal film, Solvent evaporation, Penetration enhancer, Swellability
Highlights
The transdermal film is the most innovative research area in drug delivery, and it is aimed to provide a continuous supply of medication through the skin into systemic circulation
Statins can lower LDL level by 30-50% in maximum doses [5]. It is lipophilic in nature, and due to extensive first-pass metabolism, the plasma half-life of simvastatin is 2h with an oral bioavailability of 5% [6]
Simvastatin is an ideal candidate for the preparation of transdermal films as it has low molecular weight (418.56 g/mol), high lipid solubility, low melting point (129 °C), effective in low plasma concentration as well as a high degree of first-pass metabolism [8]
Summary
The transdermal film is the most innovative research area in drug delivery, and it is aimed to provide a continuous supply of medication through the skin into systemic circulation It has several advantages like maintaining constant drug level in blood, fewer side effects and improved bioavailability and patient compliance [1] being an alternative for the oral route it prevents the gastrointestinal pH and enzymatic deactivation of the drug along with minimizing the steps involved in the metabolising pathway [2]. Statins can lower LDL level by 30-50% in maximum doses [5] It is lipophilic in nature, and due to extensive first-pass metabolism, the plasma half-life of simvastatin is 2h with an oral bioavailability of 5% [6]. The thermal breakdown of drugs can be stopped since organic solvent evaporation occurs at low temperature [9]
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