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Enhanced skin permeation of 5α-reductase inhibitors entrapped into surface-modified liquid crystalline nanoparticles

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Abstract

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 ± 2.5 nm and −20.2 ± 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 μg/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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Acknowledgments

This work was supported by the Gachon University research fund of 2014-M016.

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Authors and Affiliations

  1. College of Pharmacy, Yeungnam University, 214-1 Dae-dong, Gyeongsan, 712-749, South Korea

    Thiagarajan Madheswaran

  2. College of Pharmacy, Gachon University, 191 Hambakmoero, Incheon, 406-799, South Korea

    Rengarajan Baskaran, Pasupathi Sundaramoorthy & Bong Kyu Yoo

Authors
  1. Thiagarajan Madheswaran
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  2. Rengarajan Baskaran
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  3. Pasupathi Sundaramoorthy
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  4. Bong Kyu Yoo
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Corresponding author

Correspondence to Bong Kyu Yoo.

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R. Baskaran: Contributed same as first author.

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Madheswaran, T., Baskaran, R., Sundaramoorthy, P. et al. Enhanced skin permeation of 5α-reductase inhibitors entrapped into surface-modified liquid crystalline nanoparticles. Arch. Pharm. Res. 38, 534–542 (2015). https://doi.org/10.1007/s12272-014-0464-8

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  • DOI: https://doi.org/10.1007/s12272-014-0464-8

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