Design, Formulation and in Vitro Drug Release From Transdermal Patches Containing Imipramine Hydrochloride as Model Drug

Abstract

Objective: The aim of the present investigation was to form matrix type transdermal patches containing imipramine hydrochloride were prepared using two polymers by solvent evaporation technique to minimise the dose of the drug for lesser side effect and increase the bioavailability of a drug. Methods:In the present study, drug loaded matrix type transdermal films of imipramine hydrochloride were prepared by the solvent evaporation method with the help of polymers along with polyethene glycol (PEG) 400 was used as plasticizer and dimethyl sulfoxide (DMSO) was used as penetration enhancer. Drug-polymer interactions determine by FTIR and a standard calibration curve of imipramine hydrochloride was determined by using UV estimation. Results:The formulated transdermal patch by using PVP K-30, HPMC K100M showed good physical properties. All prepared formulations indicated good physical stability. The formulation F-1 gave the most suitable transdermal film with all desirable physicochemical properties. The thickness of the patches was varied from 0.263±0.67 mm to 0.301±0.61 mm, uniformity of patches showed that patches prepared by solvent evaporation while low standard deviation values ensued by thickness measurements of the film, and weights ranged between 50.5±0.75 mg and 52.15±2.15 mg, which indicates that different batches patch weights, were comparatively similar. Folding endurance was found to be>200 that is satisfactory for the patches, drug content was found to be 5.33±0.14 mg to 5.57±0.095 mg. In vitro, drug permeation studies of formulations were performed by using K-C diffusion cells using abdomen skin of the albino rat. The results were best in in-vitro skin permeation through rat skin as compared to all other formulations prepared with a hydrophilic polymer containing permeation enhancer. The formulation, F1 is considered as the best formulation, since it shows maximum in vitro drug release as 84.71±3.07 % at 24 h. The drug release kinetics studies showed that the majority of formulations were governed by Higuchi model and mechanism of release was non-Fickian mediated. Conclusion:In conclusion, controlled release transdermal drug delivery system (TDDS) patches of imipramine hydrochloride can be prepared using the polymer combinations, with plasticizer and enhancer. The release rate of drug through patched increased simultaneously as the concentration of hydrophilic polymer was increased. However, the mechanism of drug release of all formulations was non-Fickian. The properties of a film did not change during the period of study.

Effect of Polymers on the Physicochemical and Drug Release Properties of Transdermal Patches of Atenolol

“…Formulation batches F1 to F3 gave higher percentage cumulative drug release because they had a higher proportion of hydrophilic polymer as compared to formulation batches F4 to F6. The same result with hydrophilic polymers is also obtained by Hardainiyan et al [19] and Sadhasivam et al [20]. High polymer content in patches provides faster polymer matrix dissolution in aqueous media thus give higher drug release.…”

Effect of Hydrophilic and Hydrophobic Polymer Matrix on the Transdermal Drug Delivery of Ethinylestradiol and Medroxyprogesterone Acetate

“…The in vitro permeation experiment indicated that when the hydrophilic polymer concentration increased, the amount of drug permeation increased. As described by Rao and Diwan, initial rapid dissolution of the hydrophilic polymers occurs when the patch is in contact with the hydrated skin, resulting in the accumulation of high amounts of the drug on the skin surface and thus leading to the saturation of the skin with drug molecules at all times [20,22].…”

Design and Performance Verification of Newly Developed Disposable Static Diffusion Cell for Drug Diffusion/Permeability Studies

“…The donor chamber comprises a plastic ring (1) to which is attached a membrane sac (2), such that the interior of the plastic ring and the open end of the membrane sac are in flow communication with each other. This semi-permeable membrane could be replaced by animal's skin or, any other cellular membrane.…”

“…Among the drug delivery systems, transdermal drug delivery offers avoidance of first-pass metabolism, decreased toxicity, fewer side effects, as well as greater patient compliance [1,2]. To evaluate the performance of prepared transdermal formulation in vitro static diffusion cells are used.…”