Skin Permeation of Rosiglitazone from Transdermal Matrix Patches - Pharmaceutical Technology

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Skin Permeation of Rosiglitazone from Transdermal Matrix Patches
The authors demonstrate that sustained-release delivery can help avoid the risk of sudden higher-blood concentration of a drug to avoid toxicity.

Pharmaceutical Technology
Volume 34, Issue 5, pp. 56-72

Scanning electron microscopy (SEM). The external morphology of the transdermal patches and the dorsal and ventral sides of the skin surface before the in vitro skin permeation study and 50 h after in vitro skin permeation were analyzed with a scanning electron microscope (JSM 6100, JEOL, Tokyo). The experimental samples were cut into small parts, mounted onto stubs, and coated with gold before SEM analysis (12).

Thickness measurement. The thickness of the backing membrane and of the whole patch (i.e., the adhesive matrix with drug plus backing membrane) were measured using digital calipers (Digmatic Masschieber, model CD-6 CS, Mitutoyo, Tokyo). The average thicknesses of the backing membrane and the whole patch were determined. The average thickness of the adhesive matrix containing rosiglitazone maleate was determined using the following equation:

Area of the patches. The diameter, D, of each patch was measured using a millimeter scale, and the area (π [D/2]2) of each patch was calculated.

Moisture content. The film was weighed and kept in desiccators containing anhydrous calcium chloride for 24 h (12). The film was weighed repeatedly until it became constant. The percent moisture content was determined with the following equation:

Moisture uptake. A weighed film kept in a dessicator was exposed to relative humidity of 75% (saturated solution of sodium chloride) in a dessicator (12). The film was weighed until it showed a constant weight. Percent moisture uptake was determined as follows:

In vitro drug-release study. An in vitro drug-release study was conducted using a US Pharmacopeia-type V dissolution apparatus (Paddle over disc, Electro-lab, Chennai, India). The patches were placed between the stainless-steel disks (of which one side was mesh and one side plate stainless-steel disc meant for transdermal study). The backing membrane side was attached with double-sided adhesive tape (cut same in area as the patch) to the stainless-steel plate so that release could occur from one side only. The drug-release study was carried out at 37 0.5 C and 100 5 rpm in a dissolution jar holding 900 mL of 20% v/v PEG 400 in normal saline; 5 mL samples were withdrawn at various time intervals and replaced with 5 mL of 20% v/v PEG 400 in normal saline. Samples were analyzed with a UV–vis spectrophotometer at 318 nm against a blank (20% v/v PEG 400 in normal saline) using a validated method (15). The quantity of drug released over time was calculated from the calibration curve. The studies were conducted simultaneously by placing the patch with drug (i.e., the test) and the patch without the drug (i.e., the control) in separate baskets of the same dissolution apparatus. The difference between the test and control readings was the absorbance caused by the drug. In each case, the mean cumulative amount of drug released per square centimeter of patch was plotted against time.


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