Department Foundation Sciences, School of Dental Medicine, East Carolina University, Greenville, NC, USA.
Department of Physiological Sciences, Piracicaba Dental School, University of Campinas (UNICAMP), Piracicaba, SP, Brazil.
J Pharm Pharmacol. 2018 Jul;70(7):874-882. doi: 10.1111/jphp.12917. Epub 2018 Apr 6.
Squamous cell carcinoma (SCC) is a malignant disease that affects the oral cavity. Lidocaine has shown antiproliferative and cytotoxic activity on several cell types. The rapid dispersion is a limitation issue; however, the complexation in cyclodextrin improved pharmacological features and modified the drug release. This study investigated the effects of lidocaine (lido) complexed with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD-lido) on cell viability and proliferation of human tongue squamous cell carcinoma SCC9 and SCC25.
The complex formation was confirmed by differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). Cells SCC9 and SCC25 were exposed to lido and HP-β-CD-lido (40-4000 μm), and the effects on cell viability (MTT) and antiproliferative activity (SRB) were tested.
Differential scanning calorimetry and SEM results demonstrated the occurrence of host-guest interaction. Lido and HP-β-CD-lido (4000 μm) significantly reduced the viability of SCC9 cells to 83% and 63%, respectively. The viability of SCC25 treated with lido, and HP-β-CD-lido (4000 μm) was 71% and 44%, respectively. Lido (4000 μm) reduced the proliferation of SCC9 and SCC25 to 39.5% and 23.7%, respectively. HP-β-CD-lido (4000 μm) was cytotoxic for both cell lines.
HP-β-CD was able to potentiate the in vitro cytotoxic effects of lidocaine on human squamous cell carcinoma.
鳞状细胞癌（SCC）是一种影响口腔的恶性疾病。利多卡因已显示出对几种细胞类型的抗增殖和细胞毒性活性。快速分散是一个限制问题；然而，环糊精的络合改善了药理学特性并改变了药物释放。本研究调查了利多卡因（利多）与 2-羟丙基-β-环糊精（HP-β-CD-利多）复合物对人舌鳞状细胞癌 SCC9 和 SCC25 的细胞活力和增殖的影响。
通过差示扫描量热法（DSC）和扫描电子显微镜（SEM）确认复合物的形成。将 SCC9 和 SCC25 细胞暴露于利多卡因和 HP-β-CD-利多（40-4000μm），并测试其对细胞活力（MTT）和抗增殖活性（SRB）的影响。
差示扫描量热法和 SEM 结果表明存在主体-客体相互作用。利多卡因和 HP-β-CD-利多（4000μm）分别使 SCC9 细胞的活力显著降低至 83%和 63%。用利多卡因和 HP-β-CD-利多（4000μm）处理的 SCC25 细胞的活力分别为 71%和 44%。利多卡因（4000μm）使 SCC9 和 SCC25 的增殖分别降低至 39.5%和 23.7%。HP-β-CD-利多（4000μm）对两种细胞系均具有细胞毒性。
HP-β-CD 能够增强利多卡因对人鳞状细胞癌的体外细胞毒性作用。
