Enhancement of follicular delivery of finasteride by liposomes and niosomes 1. In vitro permeation and in vivo deposition studies using hamster flank and ear models

Abstract

Finasteride is indicated orally in the treatment of androgenetic alopecia and some other pilosebaceous unit (PSU) disorders. We wished to investigate whether topical application of finasteride-containing vesicles (liposomes and niosomes) could enhance drug concentration at the PSU, as compared to finasteride hydroalcoholic solution (HA). Liposomes consisted of phospholipid (dimyristoyl phosphatidylcholine (DMPC) or egg lecithin):cholesterol:dicetylphosphate (8:2:1, mole ratio). Niosomes were comprising non-ionic surfactant (polyoxyethylene alkyl ethers (Brij series) or sorbitan monopalmitate):cholesterol:dicetylphosphate (7:3:1, mole ratio). Vesicles were prepared by the film hydration technique and characterized with regard to the size, drug entrapment efficiency and gel-liquid transition temperature (T(c)). In vitro permeation of (3)H-finasteride through hamster flank skin was faster from hydroalcoholic solution (0.13 microg/cm(2)h) compared to vesicles (0.025-0.058 microg/cm(2)h). In vivo deposition of (3)H-finasteride vesicles in hamster ear showed that liquid-state vesicle, i.e. those made of DMPC or Brij97:Brij76 (1:1), were able to deposit 2.1 or 2.3% of the applied dose to the PSU, respectively. This was significantly higher than drug deposition by gel-state vesicles (0.35-0.51%) or HA (0.76%). Both in vitro permeation and in vivo deposition studies, demonstrated the potentials of liquid-state liposomes and niosomes for successful delivery of finasteride to the PSU.