KMID : 0043320150380040534
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Archives of Pharmacal Research 2015 Volume.38 No. 4 p.534 ~ p.542
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Enhanced skin permeation of 5¥á-reductase inhibitors entrapped into surface-modified liquid crystalline nanoparticles
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Madheswaran Thiagarajan
Baskaran Rengarajan Sundaramoorthy Pasupathi Yoo Bong-Kyu
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Abstract
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The objective of this study is to enhance skin permeation of finasteride and dutasteride for the treatment of androgenetic alopecia using surface-modified liquid crystalline nanoparticle (sm-LCN) dispersion. LCN entrapped with the drugs was prepared by using monoolein as a liquid crystal former, and surface modification was performed by treatment of the LCN dispersion with same volume of 1 % v/v acetic acid solution containing chitosan. Physicochemical properties of the LCN¡¯s were studied with regard to particle size, polydispersity index, zeta potential, and release of the drugs. Skin permeation of drugs entrapped into the LCN and sm-LCN was investigated with porcine abdominal skin using Franz diffusion cell. Cytotoxicity of the LCN¡¯s was also studied using human skin keratinocytes. The particle size and zeta potential of the LCN were 197.9 ¡¾ 2.5 nm and ?20.2 ¡¾ 1.9 mV, respectively, and sm-LCN showed slightly bigger size and positive zeta potential due to the presence of thin coating on the surface of the nanoparticles. Compared to LCN, sm-LCN resulted in significantly enhanced skin permeation of the drugs whereas in vitro release was significantly reduced. Cell viability as a measure of cytotoxicity was above 80 % up to 20 ¥ìg/ml concentration of both LCN and sm-LCN. In conclusion, sm-LCN may provide a strategy to maximize therapeutic efficacy minimizing unwanted systemic side effects associated with the use of the drugs for the treatment of androgenetic alopecia.
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KEYWORD
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Liquid crystalline nanoparticles, Chitosan, Finasteride, Dutasteride, Skin permeation
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