Electrospinning for ribociclib drug for transdermal medicationdevelopment of carrier systems, drug release and in vitro efficacy studies

Ribociclib, used in breast cancer treatment, acts as a cyclin-dependent kinase (CDK) inhibitor and causes serious side effects when used in high doses. Therefore, transdermal patch systems have been developed to reduce the side effects, prolong the half-life and reduce the effective dose of Ribociclib. In this study, transdermal patches were prepared from biocompatible polycaprolactone/chondroitin sulfate (PCL/CS) polymers in nanofiber membrane form by electrospinning method. CS was microbially produced. Optimization studies were performed for patches and 3 different patches (reservoir and drug release layer) were selected. The ratio of PCL in each patch was fixed and the amount of CS was adjusted as 1%, 2% and 4%. Structural and morphological characterization was carried out by FTIR, TGA, DSC and SEM analysis. Swelling degree, patch thickness, folding endurance and weight uniformity tests were then performed. Ribociclib was incorporated into the patch and release studies were performed using HPLC and release in the range of 95% to 96% was obtained. At this stage, in vitro biocompatibility studies were performed with the L929 (mouse fibroblast) cell line and biocompatibility in the range of 90% and 95% was obtained. In vitro cytotoxicity test was performed with MCF-7 (human breast cancer) cell line and cytotoxicity in the range of 93-94% was observed. Finally, the patches were coated with tannic acid to give them an adhesive form and ex vivo diffusion test showed drug permeability in the range of 70-80% in 48 hours on rat skin. Finally, a 5-layer patch formulation was obtained, which consisted of a non-permeable back layer, an electrospun drug reservoir layer, an electrospun drug release layer, an adhesive layer and a protective layer. In this study, transdermal patch systems that are easy to manufacture, low cost, biocompatible and provide large surface area were developed.