In this study the effect of the membrane preparation methods on the release of theophylline through cellulose acetate (CA) membranes was studied at in vitro conditions. CA/acetone binary and CA/acetone/water ternary systems were used as casting solutions and poly(ethylene glycol) (PEG) was used as the pore forming, plasticizing agent in the study. Membranes were characterized by FTIR, SEM, and DSC analysis. It was determined that pH, temperature and drug concentration affected the release of theophylline. A decrease in pH, increase in temperature and drug concentration increased the permeated amount of theophylline through the membranes. In addition, receiver solution circulation at a capillary blood rate increased the permeation of theophylline. As a result of the study, it was concluded that the release of theophylline could be controlled for a prolonged period of time and modified CA membranes prepared in the study could be as an advisable membrane material for potential release of theophylline at transdermal conditions.