Liposomal formulations for waterproofing mucosal membranes

Abstract

Liposome formulations consisting of lipids contained in the stratum corneum have been recently demonstrated to</p><p>decrease the permeability of mucosae. The permeability barrier of the mucosa is dependent on the presence of</p><p>specific lipids. The main objective of this work is to reinforce the barrier effect of the oral mucosa with liposomal</p><p>formulations to decrease permeation. Due to the high similarity in composition and structure between lanolin</p><p>and human stratum corneum lipids, liposomes were formed with lipids contained in the stratum corneum with</p><p>two kinds of ceramide or with lanolin. Transmembrane water loss of the two formulations was assessed,</p><p>obtaining an important diminution for both liposomal formulations. Caffeine, lidocaine, ketoprofen and ivermectin</p><p>and a virus model were tested on mucosa and on modified mucosa to evaluate the liposomal efficacy.</p><p>A somewhat consistent permeation pattern was obtained for the different membranes: caffeine > lidocaine ></p><p>ketoprofen > ivermectin. For all drugs and for the virus model, the most effective formulation was the liposomal</p><p>formulation, consisting of lipids found in the horny layer of the skin. The effect of the lanolin on the transmembrane</p><p>water loss is not reflected on the drug permeation. Therefore, it is demonstrated the main role of</p><p>ceramides in the barrier function for drugs and a virus model. Strengthening the barrier function of the mucosa</p><p>promotes the prevention or reduction of the permeation of different actives, which could be to extrapolate to</p><p>harmful actives like viruses, pollutants, toxins, contaminants, etc.