permeability

Tyrosine kinase inhibitors have shown to be effective in the treatment of chronic myeloid leukemia. These drugs generally belong to the Biopharmaceutical Classification System Class II or IV, indicating that their oral bioavailability is less due to its poor solubility, permeability, or both. Dasatinib is a tyrosine kinase inhibitor and the present study was aimed to overcome these limitations associated with it. Thus, a transdermal system comprising of the drug loaded into a self-microemulsifying drug delivery system was formulated. The study started by selecting the right combination of the oil (oleic acid), surfactant (Labrasol®), and cosurfactant (polyethylene glycol 400) by performing solubility and emulsification ability studies. The ternary phase diagrams were constructed to identify the microemulsion region. The liquid system was converted into an easy-to-handle gel form using 1% w/w Carbopol ETD 2020 as the gelling agent. The final system had a droplet size of 76.42 ± 1.2 nm, a narrow polydispersity index, and a high zeta potential. The thermodynamic stability studies, dispersibility and dilution tests proved that the formulation would be unaffected and would form the microemulsion instantaneously. In vitro dissolution confirmed close to 100% drug release could be obtained within 30 mins as opposed to the plain drug showing only 50 – 60 % release. In vitro permeability studies, revealed a 1.6-times enhancement in the permeation of the drug. Preparation of a self-microemulsifying drug delivery system and loading it into a topical gel could address the issues associated with the effective delivery of dasatinib.