In Vitro Caco-2 Cell Permeability Studies of Ziprasidone Hydrochloride Monohydrate Nanocrystals

被引:4
作者
Karakucuk, Alptug [1 ,2 ]
Tashan, Emine [1 ,3 ]
Ozturk, Naile [4 ]
Celebi, Nevin [1 ,5 ]
机构
[1] Gazi Univ, Dept Pharmaceut Technol, Fac Pharm, Ankara, Turkey
[2] Ankara Medipol Univ, Dept Pharmaceut Technol, Fac Pharm, Ankara, Turkey
[3] Zoleant Pharmaceut Int, Istanbul, Turkey
[4] Inonu Univ, Dept Pharmaceut Technol, Fac Pharm, Malatya, Turkey
[5] Baskent Univ, Dept Pharmaceut Technol, Fac Pharm, Ankara, Turkey
关键词
Caco-2; cells; permeability; ziprasidone; nanocrystal; DRUG NANOCRYSTALS; NANOSUSPENSIONS; DELIVERY; OPTIMIZATION; DISSOLUTION; ABSORPTION; TRANSPORT; DESIGN;
D O I
10.4274/tjps.galenos.2020.67366
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Objectives: The current study focused on the evaluation of the cytotoxic effect and permeability of ziprasidone hydrochloride monohydrate (ZHM) nanocrystals on Caco-2 cells. Materials and Methods: ZHM nanocrystals were prepared by the microfluidization method in the presence of polyvinylpyrrolidone as a stabilizer. Particle size (PS), particle size distribution (PDI), and zeta potential (ZP) values were measured in characterization studies. In vitro cytotoxic effects of ZHM nanocrystals were investigated using the 3-(4,5-dimetylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test. Caco-2 transport studies were conducted with formulations of ZHM coarse powder and nanocrystals. Results: Nanocrystals were obtained with 400-600 nm PS, 0.1-0.4 PDI, and >20 mV ZP values. The cell viability remained 100% for all sample groups. The permeability value of ZHM nanocrystals through Caco-2 cells increased 2.3-fold in comparison with ZHM coarse powder. Cumulative drug transport also increased at the end of the sampling period. Conclusion: Nanocrystal technology helps to increase the permeability of drug particles by increasing the saturation solubility.
引用
收藏
页码:223 / 227
页数:5
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