Pharmacokinetic evaluation of the synergistic effect of raloxifene loaded transfersomes for transdermal delivery
Document Type
Article
Publication Date
6-1-2021
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.
Keywords
Raloxifene, Transfersomes, Span 80, Span 85, Synergist, Transdermal delivery
Divisions
phartech
Funders
Ministry of Higher Education (MOE), Malaysia (FRGS-13-091-0332)
Publication Title
Journal of Drug Delivery Science and Technology
Volume
63
Publisher
Elsevier
Publisher Location
RADARWEG 29, 1043 NX AMSTERDAM, NETHERLANDS