Synthesis and evaluation of transdermal rosuvastatin-loaded ultradeformable vesicles: Restoring the serum lipid profile in poloxamer 407-caused hyperlipidemia

The present study aimed to design, optimize and characterize rosuvastatin calcium-loaded transfersomes (ROS-TFs) for potential transdermal application and improved the antihyperlipidemic effect of ROS. ROS-TFs were prepared by the lipid thin film hydration method using soy phosphatidylcholine (SPC) to form lipid bilayers and tween 80 (T80) or sodium cholate (SC) as an edge activator (EA). The ROS-TFs were optimized for several parameters, including the proportions of SPC and EA, the particle size (PS) and the entrapment efficiency (EE%). The optimized formulation showed a PS of 169 ± 0.7 nm, zeta potential (ZP) of −19.05 ± 0.4 mV, polydispersity index (PDI) of 0.19 ± 0.02 and EE% of 72.71 ± 1.77. The optimized formulation was further incorporated into a Carbopol 940 gel to obtain a rosuvastatin calcium-loaded transfersomal gel (ROS-TFG) to prolong its residence time on skin. The resulting ROS-TFs exhibited sustained drug release followed by ROS-TFG after 2 h at a pH of 7.4. Skin permeation studies showed enhanced skin permeation of ROS-TFs compared to that of the plain drug gel at a pH of 7.4. In vivo antihyperlipidemic results demonstrated a significant improvement in the lipid profile of the ROS-TFG group in contrast to that of the plain drug gel group. Taken together, these findings indicate that ROS-TFs could be promising nanocarriers for transdermal drug delivery with enhanced antihyperlipidemic effects in the treatment of hyperlipidemia.