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학술저널
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한국약제학회 Journal of Pharmaceutical Investigation Journal of Pharmaceutical Investigation 제49권 제4호
발행연도
2019.1
수록면
477 - 483 (7page)

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Purpose Itraconazole, which has been widely used as an antifungal-agent, is revisited as an anticancer drug but its low solubility still remains a major hurdle. Methods Inclusion complex was used to enhance the solubility of itraconazole, followed by encapsulating into liposome for glioblastoma. Results Itraconazole-inclusion complex was well formed at 1:1, 1:2 and 1:3 molar ratios of itraconazole: hydroxypropyl-β- cyclodextrin (HP-β-CD) as determined by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and Fourier transform infrared spectroscopy (FT-IR) analyses. Itraconazole-HP-β-CD inclusion complex was then encapsulated in liposome and its size was 120.5 ± 53.1 nm in diameter with 50% encapsulation efficiency. Stem cell-like property, as determined by the population ratio of CD90+/ CD133+, was decreased from 3.38 to 1.46% when the U87-MG-TL cells were treated with 100 μM itraconazole/HP-β-CD-loaded liposome. Anti-proliferative effect of itraconazole/HP-β-CD-loaded liposome on U87-MG-TL cells was slightly better than that of free itraconazole ( IC50 of 17 μM vs. 26 μM). Moreover, antiproliferative effect of Itraconazole/HP-β-CD-loaded liposome on U87-MG-TL cells was higher than that of free itraconazole when the cells were co-treated with temozolomide ( IC50 of 1.58 mM vs. 2.35 mM). Conclusions Therefore, itraconazole/HP-β-CD-loaded liposomal formulation could serve as a promising strategy for targeting the glioblastoma multiforme.

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