Development and characterization of nano-emulsions and nano-emulgels for transdermal delivery of statins

Oral administration of statins for the treatment of familial hypercholesterolemia results in poor therapeutic outcomes and patient compliance. An alternative administration route is proposed to circumvent the current limitations. This research is aimed at developing nano-emulsions and nano-emulgels as the ultimate potential delivery systems of statins for administration via the transdermal route.

Oil-in-water (o/w) nano-formulations (nano-emulsions and nano-emulgels) containing 2% (w/w) of the selected statin and 8% apricot kernel oil as oil phase were formulated. The nano-formulations were characterized using transmission electron microscopy (TEM), pH, viscosity, droplet size and zeta-potential.

Nano-emulsions' and nano-emulgels' droplet size ranged between 114.23-169.83 nm and 149.83-267.53 nm, respectively. The addition of Carbopol® Ultrez 20 increased the nano-emulsions' viscosity (3.59-8.38 cP) resulting in the formation of nano-emulgels (viscosity: 1911.00-46,090.00 cP). The entrapment efficiency (90.77-99.55%) confirmed the incorporation of the statins. Membrane release studies indicated that statins were released at higher flux values in nano-emulsions compared to their respective nano-emulgels. Ex vivo (skin diffusion) studies indicated higher median values in the nano-emulgels compared to their nano-emulsion counterparts.

The results indicate the benefits of nano-emulsions and nano-emulgels as potential alternative delivery systems for the transdermal delivery of statins.