Pharmacokinetic evaluation of the synergistic effect of raloxifene loaded transfersomes for transdermal delivery.

Abstract

The current research work involves the comparative evaluation of the synergistic potential of transfersomes with span 80, span 85 for transdermal delivery of raloxifene hydrochloride (RXN). The prepared transfersomes were optimised using size, entrapment efficiency, transdermal flux, and further characterised for other physicochemical properties. The fate of the drug within the lipid vesicles was investigated by differential scanning calorimetry and X-rays diffraction. Morphology, shape and 3-D structure was evaluated using electron microscopy. 31PNMR was carried out to evaluate the formation of lipid bilayers in the prepared vesicles. Vesicles size were found in the range of 90–140 nm with particle size and acceptable zeta potential. The transdermal flux of synergistic transfersomes (TSP-80 + 85) was much higher when compared with individual span 80 and span 85 based transfersome formulations. On the comparative evaluation of bioavailability in a rat model with transfersomal gel, oral tablet solution and hydroethanolic gel of active drug revealed that TSP-80 + 85-5 had a significant enhancement in the transdermal bioavailability in contrast to the other formulations. The study provided new insight into synergistic use of surfactants for transfersomes with successful transdermal delivery and bioavailability enhancement of poorly soluble and high metabolic rate drugs like raloxifene hydrochloride.