A TRANSDERMAL DRUG DELIVERY SYSTEM CONTAINING DEFERIOXAMINE MESYLATE FOR THE TREATMENT OF BETA-THALASSAEMIA MAJOR

Patients with beta-thalassaemia major need blood transfusion frequently during their whole life. However, frequent transfusions will eventually lead to the accumulation of trivalent iron, resulting in iron overload. To reduce iron overload, patients are administered regularly with intravenous or subcutaneous infusion of deferioxamine mesylate (DFO). Nevertheless, high costs of medication, poor patient compliance, and side effects limit its use and patient's acceptance. To overcome such drawbacks, we developed a novel transdermal delivery system to administer the DFO instead of traditional injections. We assayed the feasibility of fabricating a transdermal DFO patch using the single-layer drug-in-adhesive drug delivery system. We used the pressure-sensitive adhesives and hydrogels as the drug reservoirs and studied the release profile of DFO from the transdermal patches in vitro. In order to enhance the transdermal delivery rate, chemical enhancers, polysorbate 80 and oleic acid, and physical enhancer, ultrasound, were incorporated into the monolith DFO patches. Experimental results showed that the combination of polysorbate 80 and oleic acid in the pressure-sensitive adhesives enhanced the penetration efficiency through nude mice skin. The pretreatment of nude mice skin with ultrasound temporally changed the diffusional resistance and facilitated DFO penetration through the skin. We expect that the new delivery system can enable the drug to penetrate through skin at a stable rate and reach the circulation system successfully, thus allowing the concentration of drug to achieve the therapeutic effect.