Evaluation of biorelevant media to investigate the dissolution properties on flurbiprofen and to assess cytotoxicity effects on Caco-2 cell line

Diren Sarısaltık Yaşın, S. Yılmaz, Z. Teksin
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引用次数: 2

Abstract

DOI : 10.26650/IstanbulJPharm.2018.180013 Biorelevant media are used to simulate the physiological conditions in terms of components, pH, osmolality and buffer capacity of the human stomach and intestine in both fasted and fed states  In this study, we aim to apply the biorelevant media to Caco-2 cell lines to investigate the cytotoxicity effects via the cell viability ratio and to compare the solubilizing effects of various dissolution media on a poorly soluble model drug. Flurbiprofen (Biopharmaceutics Classification System, BCS Class 2) was selected as a model drug. In dissolution studies the pH effects were predominant at higher pH values, while bile salt effects were dominant at lower pH values. The preparation method, bile salts and the phospholipids did not show any additional effect on Caco-2 cell viability. In the cytotoxicity test, fed state media caused an additional 10-15% decrease in cell viability, compared to the fasted state. Similar results were obtained when using the blank of these media which did not include the bile salt or phospholipid. From this, it is evident that this decrease resulted from the pH values, not the components. In conclusion, the cytotoxicity assessment showed that all the biorelevant media were compatible with 70-90% of cell viability for at least 24 h, and this ratio might be increased by modifying the pH.
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评价生物相关介质对氟比洛芬的溶出特性及对Caco-2细胞株的细胞毒性作用
生物相关介质用于模拟空腹和进食状态下人体胃和肠的成分、pH、渗透压和缓冲能力等生理条件。本研究旨在将生物相关介质应用于Caco-2细胞系,通过细胞活力比研究细胞毒性作用,并比较各种溶解介质对难溶性模型药物的增溶作用。选择氟比洛芬(生物制药分类系统,BCS第2类)作为模型药物。在溶解研究中,pH效应在高pH值下占主导地位,而胆盐效应在低pH值下占主导地位。制备方法、胆盐和磷脂对Caco-2细胞活力没有额外的影响。在细胞毒性试验中,与禁食状态相比,饲喂状态培养基导致细胞活力额外下降10-15%。当使用不含胆盐或磷脂的这些培养基的空白时,获得了类似的结果。由此可见,这种减少是由pH值引起的,而不是由组分引起的。综上所述,细胞毒性评价表明,所有生物相关培养基与70-90%的细胞活力兼容至少24 h,并且可以通过改变pH来提高这一比例。
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