Liposomal itraconazole formulation for the treatment of glioblastoma using inclusion complex with HP-β-CD
- Authors
- Yoon, Sung-Won; Shin, Dae Hwan; Kim, Jin-Seok
- Issue Date
- Mar-2019
- Publisher
- Springer Netherlands
- Keywords
- Cyclodextrin; Glioblastoma multiforme; Inclusion complex; Itraconazole; Liposome
- Citation
- Journal of Pharmaceutical Investigation, v.49, no.4, pp 477 - 483
- Pages
- 7
- Journal Title
- Journal of Pharmaceutical Investigation
- Volume
- 49
- Number
- 4
- Start Page
- 477
- End Page
- 483
- URI
- https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/2957
- DOI
- 10.1007/s40005-019-00432-4
- ISSN
- 2093-5552
2093-6214
- Abstract
- 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. © 2019, The Korean Society of Pharmaceutical Sciences and Technology.
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