Ceccarini Maria Rachele, Puccetti Matteo, Pagano Cinzia, Nocchetti Morena, Beccari Tommaso, di Michele Alessandro, Ricci Maurizio, Perioli Luana
Department of Pharmaceutical Sciences, University of Perugia, 06123 Perugia, Italy.
Department of Physics and Geology, University of Perugia, 06123 Perugia, Italy.
Pharmaceuticals (Basel). 2022 Jun 23;15(7):784. doi: 10.3390/ph15070784.
The knowledge about the effect of hydrotalcites (HTlcs), largely used in pharmaceutics, on non-malignant cell lines is limited. The effect of MgAl-HTlc-and ZnAl-HTlc- (NO3−/Cl−/CO32−) on the cell viability of HaCat, fibroblasts and HepG2 was studied by MTT assay. Cells were incubated either with HTlc suspensions in the culture media and with the supernatant obtained from the suspension being centrifuged. MgAl-HTlcs suspensions resulted in being cytotoxic. As SEM and TEM analyses showed the presence of sub-micrometric particles in all the MgAl-HTlc examined, it could be hypothesized that this fraction can be internalized into cells reducing the viability. MgAl-HTlc-NO3 is the most cytotoxic probably due to the additional effect of NO3− anions. ZnAl-HTlcs are cytotoxic, especially for HaCat and HepG2 cells (viability <60% at all the concentrations assayed). The effect is attributable both to the sub-micrometric fraction (identified by TEM) and to the high Zn2+ levels found in the culture medium by ICP-OES analysis, suggesting that ZnAl-HTlcs are less stable than MgAl-HTlc in the used media. The obtained results suggest that it is very important to perform ad hoc studies in order to evaluate HTlc safety before to be introduced in a formulation.
关于水滑石（HTlcs）（广泛应用于制药领域）对非恶性细胞系影响的知识有限。通过MTT法研究了MgAl-HTlc-和ZnAl-HTlc-（NO3−/Cl−/CO32−）对HaCat、成纤维细胞和HepG2细胞活力的影响。细胞分别与培养基中的HTlc悬浮液以及离心悬浮液得到的上清液孵育。MgAl-HTlcs悬浮液具有细胞毒性。扫描电子显微镜（SEM）和透射电子显微镜（TEM）分析表明，在所检测的所有MgAl-HTlc中均存在亚微米级颗粒，由此推测该部分可被细胞内化，从而降低细胞活力。MgAl-HTlc-NO3的细胞毒性最大，可能是由于NO3−阴离子的额外作用。ZnAl-HTlcs具有细胞毒性，尤其是对HaCat和HepG2细胞（在所有检测浓度下细胞活力均<60%）。这种作用既归因于亚微米级部分（通过TEM鉴定），也归因于电感耦合等离子体发射光谱法（ICP-OES）分析在培养基中发现的高Zn2+水平，这表明在所用培养基中ZnAl-HTlcs比MgAl-HTlc更不稳定。所得结果表明，在将HTlc引入制剂之前，进行专门研究以评估其安全性非常重要。
