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논문 기본 정보

자료유형
학술저널
저자정보
Nguyen Thu Nhan (College of Pharmacy Chungnam National University) Tran Phuong (College of Pharmacy Chungnam National University) Choi Yeong-Eun (College of Pharmacy Chungnam National University) 박정숙 (충남대학교)
저널정보
한국약제학회 Journal of Pharmaceutical Investigation Journal of Pharmaceutical Investigation 제53권 제3호
발행연도
2023.5
수록면
443 - 455 (13page)
DOI
10.1007/s40005-023-00616-z

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Purpose This study aimed to prepare a solid dispersion (SD) formulation of MBZ to improve dissolution and oral bioavailability. Methods A SD formulation of mebendazole (MBZ) was prepared using sodium dodecyl sulfate (SDS) as a carrier via lyophilization method. Powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM) were used to confirm the structural properties and morphology of the MBZ-SD formulation. Dissolution study was conducted in an acidic medium (0.1 M HCl), and pharmacokinetic study was conducted in rats. In addition, the in vitro anticancer effects of MBZ-SD were also investigated in various cancer cell lines. Results From the results of PXRD, DSC, FTIR, and SEM assessments, there was an interaction between MBZ and SDS in the MBZ-SD. MBZ-SD significantly improved the aqueous solubility of MBZ (approximately 15,982-fold) and the dissolution of MBZ at 5 min (1.5-fold) as compared to that of pure MBZ. The area under the curve (AUC 0–24) and the maximum concentration (Cmax) of the MBZ-SD formulation showed a 3.56- and 3.30-fold increased values compared to pure MBZ. The anticancer effects of MBZ with IC50 value were in the order of A549 > MDA-MB-231 > HepG2 > MCF-7 > NCI-H1299 > HeLa. At safe concentrations in normal cells, the MBZ-SD formulation exhibited the superior anticancer efficacy in HeLa cells. Conclusion The obtained results in the present study suggests that SD is a good candidate for improving the bioavailability and anticancer effects of MBZ.

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