Effect of different anti-leishmanial drugs on the behavior of liposomes: elasticity and penetration through human skin

PERALTA M.F; GUZMÁN M.L.; PÉREZ A.P.; APEZTEGUIA G.; OLIVERO M.E.; ROMERO E.; CARRER, D. C.

Mar del Plata

Congreso; Reunión SAIC.SAI.SAFE.NANOMEDar.AACyTAL; 2016

Cutaneous Leishmaniasis is a parasitic orphan disease which causes ulcerative injuries and may induce serious complications. Topical treatments would minimize drugs side effects and enhance patient compliance. We propose the use of anti-Leishmania drugscarried on Soy phosphatidylcholine (SPC): sodium cholate (NaChol) liposomes for topical administration ofAmphotericinB (AmB), Imiquimod (Im) or Indole (Ind). The literature shows that liposomes penetration in the skin is related to their flexibility. We hypothesize a correlation between the drugs penetration and the liposomes flexibility. Hence, we measured the effect of the candidate drugs on the liposomes flexibility and their skin permeation capabilities. Liposomes flexibility was studied by extrusion. Skin penetration assays were performed in Franz Cells with abdominal human skin. The drugs permeability coefficient (Kp) was calculated. The quantity of drug retained in epidermis and dermis and the penetration depth were determined by validated methods. Drug suspensions at equivalent concentrations of the liposomes were used as references. D penetration ratio (DR) (liposome D µg / reference D µg) was calculated for comparison purposes.In comparison with the ultraflexible liposomes, the incorporation of Im did not produce significant changes in the flexibility (pIm>AmB. This order correlates with drugs penetration into the skin.