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Minoxidil–2-hydroxypropyl-β-cyclodextrin inclusion complexes: characterization and in vivo evaluation of an aqueous solution for hair growth in rats

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Abstract

Minoxidil dissolved in organic solvents is commonly used in the treatment of androgenic alopecia because it is hydrophobic and poorly soluble in water. The aim of this investigation was to develop an aqueous minoxidil solution without addition of organic solvents. To this end, minoxidil was encapsulated in 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) to form a minoxidil–HP-β-CD inclusion complex with aqueous solubility higher than that of pure minoxidil. Minoxidil–HP-β-CD inclusion complexes were prepared using a freeze-drying method from minoxidil and HP-β-CD at a molar ratio of 1:1. Complex formation was confirmed by nuclear magnetic resonance, thermogravimetric analysis, and thin layer chromatography. The structure of the complex was determined using two-dimensional rotating frame overhauser effect spectroscopy. Minoxidil–HP-β-CD inclusion complexes were dissolved in water to form a homogeneous aqueous solution, and its effect on the hair cycle of mice was evaluated in vivo. The results support the feasibility of using HP-β-CD to prepare an aqueous minoxidil solution to replace organic solvent-based solutions.

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Authors and Affiliations

  1. Graduate Institute of Chinese Medicine, China Medical University, Taichung, Taiwan

    Ta Chen Chen, Song-Cu Yu, Chin-Mu Hsu & Yuhsin Tsai

  2. School of Chinese Medicine, China Medical University, Taichung, Taiwan

    Ta Chen Chen, Song-Cu Yu, Chin-Mu Hsu, Fuu-Jen Tsai & Yuhsin Tsai

  3. Department of Medical Research, China Medical University Hospital, Taichung, Taiwan

    Chin-Mu Hsu

  4. Department of Medical Genetics, Pediatrics and Medical Research, China Medical University Hospital, Taichung, Taiwan

    Fuu-Jen Tsai

  5. Department of Biotechnology, Asia University, Taichung, Taiwan

    Fuu-Jen Tsai

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  1. Ta Chen Chen
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  2. Song-Cu Yu
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  3. Chin-Mu Hsu
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  5. Yuhsin Tsai
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Correspondence to Yuhsin Tsai.

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Chen, T.C., Yu, SC., Hsu, CM. et al. Minoxidil–2-hydroxypropyl-β-cyclodextrin inclusion complexes: characterization and in vivo evaluation of an aqueous solution for hair growth in rats. J Incl Phenom Macrocycl Chem 88, 27–34 (2017). https://doi.org/10.1007/s10847-017-0705-9

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  • DOI: https://doi.org/10.1007/s10847-017-0705-9

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