Proniosomal Vesicles as an Effective Strategy to Optimize Naproxen Transdermal Delivery

Abstract

The oral administration of naproxen, a non-steroidal analgesic, antipyretic, anti-inflammatory drug, is associated with various gastrointestinal side effects including peptic ulcer and gastritis. The objective of the present research was to evaluate the prospective of transdermal delivery of naproxen using proniosomes as a vesicular carrier and its comparison with oral therapy. Drug loaded proniosomes were prepared by coacervation phase separation, which comprising of spans/tweens, lecithin, and cholesterol. The influence of formulation components was evaluated to assess their impact on the entrapment efficiency, vesicle size, zeta potential, in vitro release and ex vivo permeation. The results signify that the type of surfactant influenced the entrapment efficiency, vesicle size and zeta potential values of prepared proniosomes. All formulations displayed nano-sized vesicles with small polydispersity index value showing narrow particle size distribution. Hydrophilic tweens produced larger vesicles and exhibited greater drug release than their hydrophobic spans counterparts. Prepared proniosomes exhibited distinct drug release profile (p < 0.05) as compared to control HPMC hydrogel. The proniosomal formulation (F3) containing span 60 showed superior transdermal flux (1.10 ± 0.24 μg cm􀀀 2 h􀀀 1) when compared to other non-ionic surfactants tested. In vivo data demonstrated both anti-inflammatory and antinociceptive efficiency of transdermal naproxen proniosome formulation (F3) was equivalent to the oral marketed naproxen tablets at same dose. Overall the results of present investigation suggest that proniosomes can be considered as a practicable and feasible alternative for oral naproxen delivery.