Abstract:
The aim of the current investigation is to evaluate the transdermal potential of novel vesicular carrier, liposomes, ethosomes, transferosomes, having thiocolchicoside, a potent, water soluble muscle relaxant drug with lesser transdermal permeation. Drug loaded liposomes, ethosomes, transferosomes had been prepared using phospholipid and ethanol, were optimized and characterized for entrapment efficiency, vesicular size, zeta potential, in vitro skin permeation and stability. The ethosomal formulation having 10 mg of phospholipid and 10 ml of ethanol showing the greatest entrapment efficiency (23.16 ± 1%) with small particle size (502 ± 5nm) then liposomes, and transferosomes. The skin permeation studies were performed on ethosomal formulation, liposomal formulation, transferosomes formulation, aqueous drug solution. Among them, ethosomal formulation showed higher cumulative percentage of drug permeation (90 ± 5%) after 24 hours than the other formulations. Differential scanning colorimetery shows no intraction between lipid and drug. Zeta seizer revealed that the ethosomes has smaller vesicular size than the liposomes and transferosomes. FT‐IR studies revealed no interaction between the drug and membrane components. The ethosomes, liposomes, transferosomes vesicles muscle relaxant efficiency was compared with the marketed thiocolchicoside gel. The pharmacodynamic studies showed that the muscle relaxant activity of ethosomes was more then liposomes, transferosomes suspension and less than the marketed gel formulation. Our results suggest that the ethosomes are an efficient carrier for dermal and transdermal delivery of thiocolchicoside.

Keywords: Transdermal, Ethosomes, Phospholipid, Liposomes, Thiocolchicoside.