Abstract
The aim of this work was to evaluate the effect of two chemically different edge activators, i.e., Tween® 80 and sodium deoxycholate, on (i) the physical, mechanical, and biological properties of ultradeformable vesicles, and (ii) the administration of naproxen sodium-loaded multidrug ultradeformable vesicles for the transdermal route in order to obtain therapeutically meaningful drug concentrations in the target tissues and to potentiate its anti-inflammatory effect by association with the antioxidant drug idebenone. The results obtained in this investigation highlighted a synergistic action between naproxen and idebenone in the treatment of inflammatory disease with a more pronounced anti-inflammatory effect in multidrug ultradeformable vesicles compared to the commercial formulation of Naprosyn® gel. Systems made up of Tween® 80 appeared to be the most suitable in terms of percutaneous permeation and anti-inflammatory activity due to the greater deformability of these vesicles compared to multidrug ultradeformable vesicles with sodium deoxycholate. Our findings are very encouraging and suggest the use of these carriers in the topical treatment of inflammatory diseases.
Highlights
Over the last decades, the possibility of using the transdermal route as the preferential way to administrate anti-inflammatory drugs for the treatment of local or systemic inflammatory states has been seriously considered [1]
This xerophobia [10] is strictly related to the composition of the carrier, made of polar lipids and an edge activator, i.e., a surfactant that destabilizes the membrane package making it elastic, allowing the carrier to deliver more than 50% of the drug through the skin barrier [11]; it is a significant value considering that the topical bioavailability of the most commercialized formulations is very low
dynamic light scattering (DLS) analysis evidenced that, after extrusion, all the formulations were characterized by a mean size lower than 150 nm and low values of polydispersity index (
Summary
The possibility of using the transdermal route as the preferential way to administrate anti-inflammatory drugs for the treatment of local or systemic inflammatory states has been seriously considered [1]. Ultradeformable carriers move from a dry environment to one with a higher content of water This xerophobia [10] is strictly related to the composition of the carrier, made of polar lipids and an edge activator, i.e., a surfactant that destabilizes the membrane package making it elastic, allowing the carrier to deliver more than 50% of the drug through the skin barrier [11]; it is a significant value considering that the topical bioavailability of the most commercialized formulations is very low (around 1%–5% of the applied amount). Their ability of obtaining a topical or a systemic effect [12] and their physical stability [13] represent important parameters in the context of their pharmaceutical development
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