Aim of this work was the development of mixed matrix membranes as potential devices for transdermal controlled release of gemfibrozil (2,2-dimethyl-5-(2,5-dimethylphenoxy) pentanoic acid). The effect of the hydrophilic NaX zeolite and of drug loading on the release kinetics of the drug was investigated. The material used as membrane matrix was polydimethylsiloxane. Scanning electron microscopy analysis showed as zeolite crystals were well embedded into the polymeric matrix. Membrane characterizations by means of swelling ratio, moisture uptake, and erosion degree determination indicated low swelling degree and moisture uptake, and the absence of erosion. This results confirmed as these membranes did not promote bacterial growth and skin irritation. The performance of the membranes was evaluated by performing in vitro release studies and percutaneous tests through the stratum corneum taken from the skin of rabbit ear. In vitro experiments indicated as the best system was the membrane containing 12 wt % of zeolite and 2.6 wt % of gemfibrozil (PDMS-2.6GEM-12NaX) and so it was used in the percutaneous tests. In this case, the permeation rate was lower owing to the presence of an additional resistance applied by rabbit skin. An interesting result was the linear behavior indicating that the permeation of the drug thorough the device occurred with zero-order kinetic which is the feature of the transdermal controlled delivery systems.