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Journal of microbiology and biotechnology v.17 no.12, 2007년, pp.1965 - 1969  
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After-Rinsing Hair Growth Promotion of Minoxidil-containing Amino ${\alpha}$-Cyclodextrins

Kim, Jin-Chul   (College of Bioscience & Biotechnology, Kangwon National University and Institute of Bioscience and BiotechnologyUU0000037  ); Kim, Myoung-Dong   (College of Bioscience & Biotechnology, Kangwon National University and Institute of Bioscience and BiotechnologyUU0000037  );
  • 초록

    Triamino ${\alpha}$ -cyclodextrin (CD) was synthesized and the inclusion complex with Minoxidil (MXD) was prepared. ${\alpha}$ -CD was azidated by modifying the 6-hydroxylmethyl CD rim with sodium azide. Then, mono-, di-, tri-, and tetra-azidocyclodextrins were separated by a flash column chromatography and reduced to the corresponding amines by hydrogenation with Pd/C. The substantivities of MXD included in either 2-hydroxypropyl ${\alpha}$ -CD (HP ${\alpha}$ -CD) or triamino ${\alpha}$ -CD were evaluated in vitro using hairless mice skins. After applying the preparations onto the skin and rinsing it, the amount of the drug left on the skin was determined using high-performance liquid chromatography (HPLC). It was the highest when the drug was included in triamino ${\alpha}$ -CD. The electrostatic interaction between the protonated amino CD and the negatively charged skin would be responsible for the relatively high substantivity. The in vivo hair growth promotion effect of each preparation was investigated, where the sample application onto the clipped backs of female mice (C57BL6) and the subsequent rinsing of the backs were done once a day for 30 days. Only MXD in triamino ${\alpha}$ -CD had hair growth promotion effect, possibly due to the significant substantivity.


  • 주제어

    Minoxidil .   triamino ${\alpha}$-cyclodextrin .   inclusion complex .   substantivity .   hair growth.  

  • 참고문헌 (12)

    1. Kim, J.-C., M.-H. Lee, and M.-J. Rang. 2002. Minoxidilcontaining dosage forms: Substantivity and after-rinsing hair growth promotion. Drug Deliv. 10: 119-123 
    2. Lee, J.-H., D.-H. Lee, J. H. Son, J.-K. Park, and S.-K. Kim. 2005. Optimization of chitosan-alginate encapsulation process using pig hepatocytes for development of bioartificial liver. J. Microbiol. Biotechnol. 15: 7-13     
    3. Park, K.-H., D. M. Kang, and K. Na. 2006. Physicochemical characterization and carcinoma cell interaction of selforganized nanogels prepared from polysaccharide/biotin conjugates for development of anticancer drug carrier. J. Microbiol. Biotechnol. 16: 1369-1376     
    4. Poulos, C. W., G. M. Brenner, L. V. Allen Jr., V. A. Prabhu, and P. L. Huerta Jr. 1994. Method for simulating hair growth with cationic derivative of minoxidil using therapeutic iontophoresis. USP. 5,466,695 
    5. Tsai, J.-C., M. J. Cappel, G. L. Flynn, N. D. Weiner, J. Kreuter, and J. J. Ferry. 1992. Drug and vehicle deposition from topical applications: Use of in vitro mass balance technique with minoxidil solutions. J. Pharm. Sci. 81: 736- 743 
    6. Ferry, J. J., J. H. Shepard, and G. J. Szpunar. 1990. Relationship between contact time of applied dose and percutaneous absorption of minoxidil from a topical solution. J. Pharm. Sci. 79: 483-486 
    7. Hanessian, S., A. Benalil, and C. Laferriere. 1995. The synthesis of functionalized cyclodextrins as scaffolds and templates for molecular diversity, catalysis, and inclusion phenomena. J. Org. Chem. 60: 4786-4797 
    8. Kim, C.-J., S.-A. Jun, N.-K. Lee, K.-T. Kim, S. K. Lee, C.-H. Kim, and H.-D. Paik. 2006. Encapsulation of Bacillus polyfermenticus SCD with alginate-methylcellulose and evaluation of survival in artificial conditions of large intestine. J. Microbiol. Biotechnol. 16: 443-449     
    9. Touitou, E., N. Dayan, L. Bergelson, B. Godin, and M. Eliaz. 2000. Ethosomes - novel vesicular carriers for enhanced delivery: Characterization and skin penetration properties. J. Control. Release 65: 403-418 
    10. Tsai, J.-C., G. L. Flynn, N. Weiner, and J. J. Ferry. 1993. Effect of minoxidil concentration on the deposition of drug and vehicle into the skin. Int. J. Pharm. 96: 111-117 
    11. Tata, S., G. L. Flynn, and N. D. Weiner. 1995. Penetration of minoxidil from ethanol/propylene glycol solution: Effect of application volume and occlusion. J. Pharm. Sci. 84: 688- 691 
    12. Tata, S., N. Weiner, and G. Flynn. 1994. Relative influence of ethanol and propylene glycol cosolvents on deposition of minoxidil into the skin. J. Pharm. Sci. 83: 1508-1510 

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