Influence of Liposomes and Niosomes on the In Vitro Permeation and Skin Retention of Finasteride

Abstract

In this work we sought to determine whether vesicles (liposomes/niosomes) were able to enhance finasteride concentration in the dermis layer, including the pilosebaceous units (PSU). Such enhancement could be beneficial in the treatment of some androgen-related skin disorders. Hamster flank skin was used to study <span style="font-family: TimesNewRomanMS; font-size: xx-small;"><span style="font-family: TimesNewRomanMS; font-size: xx-small;">3</span></span><span style="font-family: TimesNewRomanMS;">Hfinasteride </span>permeation via vesicles and a hydroalcoholic solution (HA). The drug-containing vesicles were composed of dimyristoyl phosphatidylcholine (DMPC) or egg lecithin: cholesterol: dicetyl phosphate (liposomes) and polyoxyethylene alkyl ethers (Brij <span style="font-family: TimesNewRomanMS; font-size: xx-small;"><span style="font-family: TimesNewRomanMS; font-size: xx-small;">® </span></span><span style="font-family: TimesNewRomanMS;">series) or sorbitan monopalmitate (Span 40): </span>cholesterol: dicetyl phosphate (niosomes) and were prepared by the film hydration technique. Determination of finasteride content by HPLC showed 80-97% drug entrapment efficiency in the vesicles. The amount of <span style="font-family: TimesNewRomanMS; font-size: xx-small;"><span style="font-family: TimesNewRomanMS; font-size: xx-small;">3</span></span><span style="font-family: TimesNewRomanMS;">H-finasteride penetrated into </span>and permeated through hamster skin 24 h after topical application of vesicles ranged from 5.5 to 13% of the initial dose, compared to 24%, observed with HA ( <span style="font-family: TimesNewRomanItMS;">p</span><span style="font-family: TimesNewRomanMS;">Span 40 and lecithin vesicles was lower, when compared with liquid-state Brij97, Brij 76: Brij 97 and DMPC vesicles. The fraction of finasteride found in the dermis layer was greatest where DMPC liposomes were used (7.8%). The vesicles significantly reduced drug permeation as indicated by the flux of finasteride from vesicles (0.025-0.058 µg/cm <span style="font-family: TimesNewRomanMS; font-size: xx-small;"><span style="font-family: TimesNewRomanMS; font-size: xx-small;">2</span></span><span style="font-family: TimesNewRomanMS;">.h), where compared with the HA (0.13 µg/cm</span><span style="font-family: TimesNewRomanMS; font-size: xx-small;"><span style="font-family: TimesNewRomanMS; font-size: xx-small;">2</span></span><span style="font-family: TimesNewRomanMS;">.h),</span> (<span style="font-family: TimesNewRomanItMS;">p</span><span style="font-family: TimesNewRomanMS;">the percutaneous absorption of finasteride and increasing its concentration and retention in the dermis layer.</span></span>