In Vitro Percutaneous Permeation and Skin Accumulation of Finasteride Using Vesicular Ethosomal Carriers

Abstract

Abstract. In order to develop a novel transdermal drug delivery system that facilitates the skin permeation of finasteride encapsulated in novel lipid-based vesicular carriers (ethosomes)finasteride ethosomes were constructed and the morphological characteristics were studied by transmission electron microscopy. The particle size, zeta potential and the entrapment capacity of ethosome were also determined. In contrast to liposomes ethosomes were of more condensed vesicular structure and they were found to be oppositely charged. Ethosomes were found to be more efficient delivery carriers with high encapsulation capacities. In vitro percutaneous permeation experiments demonstrated that the permeation of finasteride through human cadaver skin was significantly increased when ethosomes were used. The finasteride transdermal fluxes from ethosomes containing formulation (1.34±0.11 μg/cm 2 /h) were 7.4, 3.2 and 2.6 times higher than that of finasteride from aqueous solution, conventional liposomes and hydroethanolic solution respectively (P<0.01).Furthermore, ethosomes produced a significant (P<0.01) finasteride accumulation in the skin, especially in deeper layers, for instance in dermis it reached to 18.2±1.8 μg/cm 2 . In contrast, the accumulation of finasteride in the dermis was only 2.8± 1.3 μg/cm 2 with liposome formulation. The study demonstrated that ethosomes are promising vesicular carriers for enhancing percutaneous absorption of finasteride.

Penetration profile and human cadaver skin distribution of finasteride from vesicular nanocarriers

“…Ethosomes and liposomes were prepared and characterized as previously described (Rao et al, 2008). The SPL (3% w/w) and drug (0.2% w/w) were dissolved in ethanol in a sealed glass container, and then the water was added slowly in a constant stirring condition, keeping in mixing for 5 min.…”

“…The film was dispersed with water and completely hydrated. The final sample was processed with the method described in ethosomes preparation (Rao et al, 2008). Each time 20 mg drug was used for the preparation of 10 g formulation.…”

“…In previous study (Rao et al, 2008), a transdermal drug delivery system of finasteride-loaded ethosomes was developed. The influence of ethosomes on the percutaneous absorption of finasteride was studied.…”

“…In continuation with previous research (Rao et al, 2008), a study was initiated to qualitatively characterize the distribution of finasteride in human cadaver skin using modified Franz diffusion cells in vitro. The effects of ethosomes or liposomes on drug distribution in the different strata of the full-thickness human skin were evaluated.…”

Effect of Charge Carrier Lipid on Skin Penetration, Retention, and Hair Growth of Topically Applied Finasteride-Containing Liposomes

“…There have been several studies which showed that topical application of the drug might be better option to avoid the unwanted side effects encountered when orally administered (Tabbakhian et al, 2006;Kumar et al, 2007). Specifi cally, since the target tissue of FNS for the treatment of androgenetic alopecia is hair follicles in the scalp, various topical formulation of the drug was pursued using liposomes, ethosomes, niosomes, solid lipid nanoparticles, and nanostructured lipid carriers (Biruss and Valenta, 2006;Biruss et al, 2007;Rao et al, 2008;Balakrishnan et al, 2010).…”