Design of Cilostazol Nanocrystals for Improved Solubility
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The purpose of this study is to achieve enhanced solubility of cilostazol (CLT) by nanocrystal (NC) formation. CLT-NC was prepared by nanoprecipitation without the use of surfactant.
To optimize particle size, we controlled four parameters, including the speed or power in the homogenizer or probe-sonicator, respectively, the processing temperature, drug concentration, and collection method. CLT-NC with a mean size of 500–600 nm was successfully prepared by a simple method.
The small particle size was optimized by probe-sonication (200 W) at a low temperature (4 °C), drug concentration (4 mg/mL), and filtration (collecting method). The DSC thermograms and crystallinity of CLT exhibited a slight shift of on CLT-NC. The solubility of CLT-NC significantly increased 10.7-/7.6-/10.0-fold compared with that of CLT in different media (distilled water (DW), pH 1.2 and pH 6.8 buffers, respectively) for 24 h. Moreover, CLT-NC did not show the toxicity characteristic of CLT in the Caco-2 cells, and the nanocrystals were well maintained in 25 °C and 4 °C for 3 months.
We developed CLT-NC with high solubility and non-toxic characteristics, which is expected to have high bioavailability in animals.
KeywordsCilostazol Nanocrystal Solubility Cytotoxicity Stability
Field emission scanning electron microscopy
Differential scanning calorimetry
This work was supported by a research program funded by Chodang University in 2018.
Compliance with Ethical Standards
Conflict of Interest
The author declares that there are no conflicts of interest.
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