Trombino Sonia, Malivindi Rocco, Barbarossa Giuseppe, Sole Roberta, Curcio Federica, Cassano Roberta
Department of Pharmacy, Health and Nutritional Science, University of Calabria, Arcavacata, 87036 Rende, Italy.
Azienda Sanitaria Provinciale, Via Alimena, 87100 Cosenza, Italy.
Pharmaceutics. 2023 Apr 29;15(5):1375. doi: 10.3390/pharmaceutics15051375.
Classical melanoma therapy has several side effects that are responsible for a decrease in the final therapeutic efficacy. It is possible that the drug is degraded before reaching the target site and is metabolized by the body itself, resulting in repeated doses being administered throughout the day and a decrease in patient compliance. Drug delivery systems avoid degradation of the active ingredient, improve release kinetics, prevent the drug from being metabolized before reaching the site of action, and improve the safety and efficacy profiles of adjuvant cancer therapy. The solid lipid nanoparticles (SLNs) based on hydroquinone esterified with stearic acid realized in this work represent a chemotherapeutic drug delivery system that is useful in the treatment of melanoma. The starting materials were characterized by FT-IR and H-NMR, while the SLNs were characterized by dynamic light scattering. In efficacy studies, their ability to influence anchorage-dependent cell proliferation was tested on COLO-38 human melanoma cells. Furthermore, the expression levels of proteins belonging to apoptotic mechanisms were determined by analyzing the role of SLNs in modulating the expression of p53 and p21WAF1/Cip1. Safety tests were conducted to determine not only the pro-sensitizing potential but also the cytotoxicity of SLNs, and studies were conducted to assess the antioxidant and anti-inflammatory activity of these drug delivery.
传统的黑色素瘤治疗方法有多种副作用,这些副作用会导致最终治疗效果下降。药物有可能在到达靶点之前就被降解,并被人体自身代谢,导致需要全天重复给药,患者的依从性降低。药物递送系统可避免活性成分降解,改善释放动力学,防止药物在到达作用部位之前被代谢,并改善辅助癌症治疗的安全性和疗效。在这项工作中实现的基于硬脂酸酯化对苯二酚的固体脂质纳米粒(SLNs)代表了一种对治疗黑色素瘤有用的化疗药物递送系统。起始材料通过傅里叶变换红外光谱(FT-IR)和氢核磁共振(H-NMR)进行表征,而SLNs则通过动态光散射进行表征。在疗效研究中,在COLO-38人黑色素瘤细胞上测试了它们影响贴壁依赖性细胞增殖的能力。此外,通过分析SLNs在调节p53和p21WAF1/Cip1表达中的作用,确定了属于凋亡机制的蛋白质的表达水平。进行了安全性测试,以确定SLNs的促致敏潜力和细胞毒性,并开展研究以评估这些药物递送的抗氧化和抗炎活性。