Optimization of propofol loaded niosomal gel for transdermal delivery

Abstract

Propofol is an oily liquid widely used for rapid onset of anaesthesia via intravenous route, which shows major limitations of hypersensitivity, anaphylactic reactions and pain. The aim of the present work was to bypass the above issues by formulating tailored niosomal gel to deliver propofol via non-invasive transdermal route. The niosomes were prepared by film hydration method and sonication using cholesterol and Span 80. The Box Behnken design (BBD) was applied to optimize the size (93.5 nm) and the entrapment efficacy (81.5%) of the niosomes by selecting cholesterol at 139 mg, Span 80 at 0.525% and sonication time at 5.13 min. The scanning electron microscopy image showed spherical shape niosomes with smooth surface without aggregation. The ex vivo release data showed significant improvement in the propofol release (92.2% after 10 h) using niosomes in comparison to the control propofol gel (with 30% methanol) without niosomes (25.3% after 10 h). The in vivo pharmacokinetic parameters in the rat model confirmed the improvement in the relative bioavailability with optimized niosomal gel (relative bioavailability = 12.12) in comparison to the control propofol gel. In conclusion, the niosomal gel offered a potential alternative non-invasive route to deliver propofol for procedural sedation especially in pediatric population.