Development and Evaluation of Ethyl Cellulose-Based Transdermal Films of Furosemide for Improved In Vitro Skin Permeation

Abstract

Abstract. Transdermal films of the furosemide were developed employing ethyl cellulose and hydroxypropyl methylcellulose as film formers. The effect of binary mixture of polymers and penetration enhancers on physicochemical parameters including thickness, moisture content, moisture uptake, drug content, drug-polymer interaction, and in vitro permeation was evaluated. In vitro permeation study was conducted using human cadaver skin as penetration barrier in modified Keshary-Chein diffusion cell. In vitro skin permeation study showed that binary mixture, ethyl cellulose (EC)/hydroxypropyl methylcellulose (HPMC), at 8.5:1.5 ratio provided highest flux and also penetration enhancers further enhanced the permeation of drug, while propylene glycol showing higher enhancing effect compared to dimethyl sulfoxide and isopropyl myristate. Different kinetic models, used to interpret the release kinetics and mechanism, indicated that release from all formulations followed apparent zero-order kinetics and nonFickian diffusion transport except formulation without HPMC which followed Fickian diffusion transport. Stability studies conducted as per International Conference on Harmonization guidelines did not show any degradation of drug. Based on the above observations, it can be reasonably concluded that blend of EC-HPMC polymers and propylene glycol are better suited for the development of transdermal delivery system of furosemide.

In vitro Permeation Study of Ketoprofen Patch with Combination of Ethylcellulose and Polyvynil Pyrrolidone as Matrix Polymers

“…Low humidity in the formulation is able to keep the preparation stable and the film not dry and fragile. 10 The moisture percentage can be seen in Table 3. Homogenity tests of ketoprofen content were performed to ensure that on each part in a patch had a uniform content of ketoprofen (Table 4).…”

“…EC is not only a polymer that has low solubility in water, not toxic, and not irritate but also it does not cause allergy and can form strong film layer. 10 Combination of 1,5% EC and dibutyl phthalate as a plasticizer can release 99.12% hydrophobic Amlodipine for 24 h but the percentage of drug released will decrease if the EC used is in high concentration. 11 In the other hand, Polyvynil pyrrolidone (PVP) is a low toxicity hydrophilic polymer.…”

Transdermal delivery of Diltiazem HCl from matrix film: Effect of penetration enhancers and study of antihypertensive activity in rabbit model

“…Different plasticizers such as glycerol, DBT and PG were incorporated at 20% w/w of polymer dry weight. Calculated amount of DTH was mixed with homogenous polymer solution and poured into a petri dish containing mercury [12,13]. A funnel was placed over the petri dish in inverted position to control the rate of evaporation.…”

“…The percentage of moisture uptake was calculated based on the difference between final and initial weight divided by initial weight [13].…”

“…The moisture absorption is a tool to indicate how the film would behave during the initial stage of drug release [13]. The result of moisture content and moisture absorption study is shown in Fig.…”