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KMID : 1146920190490040477
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Journal of Pharmaceutical Investigation
2019 Volume.49 No. 4 p.477 ~ p.483
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Liposomal itraconazole formulation for the treatment of glioblastoma using inclusion complex with HP-β-CD
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Yoon Sung-Won
Shin Dae-Hwan
Kim Jin-Seok
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Abstract
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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, anti-proliferative 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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KEYWORD
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Itraconazole, Inclusion complex, Liposome, Glioblastoma multiforme, Cyclodextrin
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