In-vitro; ex-vivo assessment of anti-inflammatory Tapentadol loaded non-ionic surfactant vesicular systems for effective transdermal delivery

Abstract

AHMED S. ABDUL JABBAR.

Tapentadol is an anti-inflammatory drug and mostly used rheumatoid arthritis commonly at 200mg an oral dose twice daily. Because of its first-pass metabolism, its bioavailability is low (32%).To overcome this problem, the transdermal route appear to be the optimal route for tapentadol administration. The present work focuses on developing niosomes for transdermal delivery of tapentadol for relieving pain and exploring possible mechanism of better skin permeation of niosomes. Niosomes were prepared by ethanol injection technique and characterized for various physicochemical parameters. Niosomes were in size range of (268±1.02 to 750±1.02nm). The lowest particles size (268 nm), highest entrapment efficiency (75.25%±1.32) and zeta potential -38.8 mV found for N8 niosomal batch. The stability profile of niosomal suspension after 8 weeks showed that 68±0.25% of drug was retained in the system. In vitro skin permeation studies of niosomes showed 98.92±1.2% of permeation over 24 hrs. N8 niosomal batch was incorporated in 1.5% Carbopol 931NF and carried out the ex vivo rat skin permeated studies states that niosomal suspension shows maximum flux (30µg/cm2/hr) comparatively niosomal gel (26.29µg/cm2/hr) and plain gel (20.84 µg/cm2/hr). These improvements in tapentadol formulation may be useful in developing a more effective NSAIDS therapy.