Karaküçük Alptuğ, Taşhan Emine, Öztürk Naile, Çelebi Nevin
Gazi University Faculty of Pharmacy, Department of Pharmaceutical Technology, Ankara, Turkey
Ankara Medipol University Faculty of Pharmacy, Department of Pharmaceutical Technology, Ankara, Turkey
Turk J Pharm Sci. 2021 Apr 20;18(2):223-227. doi: 10.4274/tjps.galenos.2020.67366.
The current study focused on the evaluation of the cytotoxic effect and permeability of ziprasidone hydrochloride monohydrate (ZHM) nanocrystals on Caco-2 cells.
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. 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.
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.
Nanocrystal technology helps to increase the permeability of drug particles by increasing the saturation solubility.
本研究聚焦于评估盐酸齐拉西酮一水合物（ZHM）纳米晶体对Caco-2细胞的细胞毒性作用及通透性。
在聚乙烯吡咯烷酮作为稳定剂的情况下，通过微流化法制备ZHM纳米晶体。在表征研究中测量粒径（PS）、粒径分布（PDI）和zeta电位（ZP）值。使用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐试验研究ZHM纳米晶体的细胞毒性作用。用ZHM粗粉和纳米晶体的制剂进行Caco-2转运研究。
获得了粒径为400 - 600 nm、粒径分布为0.1 - 0.4且zeta电位值>20 mV的纳米晶体。所有样品组的细胞活力均保持在100%。与ZHM粗粉相比，ZHM纳米晶体通过Caco-2细胞的通透性值增加了2.3倍。在取样期结束时，累积药物转运也增加了。
纳米晶体技术通过提高饱和溶解度有助于增加药物颗粒通透性。
