Central Composite Design (CCD) for the Optimisation of Ethosomal Gel Formulation of Punica granatum Extract: In Vitro and In Vivo Evaluations

Abstract

This research manuscript’s objective was to develop the Punica granatum extract ethosome gel. The use of nanotechnology can improve transdermal drug delivery permeation of its major bioactive compound β-sitosterol. The optimised and developed formulations were further studied in vitro and in vivo. The assessment of the anti-inflammatory activity of the gel was performed in Albino rats. Methanolic extract was prepared and developed into an ethosome suspension and an ethosome gel. To optimise the formulation’s response in terms of particle size (nm) and entrapment efficiency (%), the central composite design (CCD) was used in 22 levels. The effects of factors such as lecithin (%) and ethanol (mL) in nine formulations were observed. Characterisation of ethosome gel was performed and the results showed the particle size (516.4 nm) and mean zeta potential (−45.4 mV). Evaluations of the gel formulation were performed. The results were good in terms of pH (7.1), viscosity (32,158 cps), spreadability (31.55 g cm/s), and no grittiness. In an in vitro study, the percentages of β-sitosterol release of ethosome gel (91.83%), suspension (82.74%), and extracts (68.15%) at 279 nm were recorded. The effects of the formulated gel on formalin-induced oedema in Albino rats showed good results in terms of anti-inflammatory activity. The comparative anti-inflammatory activity of Punica granatum extract and gel showed that the gel action was good for their topical application.