Russo Stefano, Torrisi Cristina, Cardullo Nunzio, Muccilli Vera, La Mantia Alfonsina, Castelli Francesco, Acquaviva Rosaria, Sarpietro Maria Grazia
Department of Drug and Health Sciences, University of Catania, Viale Andrea Doria 6, 95125 Catania, Italy.
Department of Chemical Sciences, University of Catania, Viale Andrea Doria 6, 95125 Catania, Italy.
Pharmaceutics. 2023 Jan 24;15(2):394. doi: 10.3390/pharmaceutics15020394.
Colorectal cancer is one of the most diffused tumoral diseases. Since most medicaments employed for its treatment are debilitating, the use of naturally derived products, which can be effective against the mutated cells and, in addition, can reduce most inflammatory-related effects, could be extremely beneficial for the continued treatment of this disease. In this research, ethyl protocatechuate (PCAEE), a protocatechuic acid prodrug, was encapsulated in solid lipid nanoparticles (SLN) (prepared without and with Tween 80), which were characterized in terms of size, polydispersity index (PDI), zeta potential and thermotropic behavior. Encapsulation efficiency, release profile and interaction with a model of biomembrane were also assessed. The nanoparticles were tested in vitro on both healthy cells and on a model of tumoral cells. SLN prepared with Tween 80 was promising in terms of physicochemical properties (z-average of 190 nm, PDI 0.150 and zeta potential around -20 mV) and encapsulation efficiency (56%); they showed a desirable release profile, demonstrated an ability to penetrate and release the encapsulated PCAEE into a biomembrane model and were nontoxic on healthy cells. In addition, they caused a greater dose-dependent decrease in the viability of CaCo-2 cells than PCAEE alone. In conclusion, the formulation could be proposed for further studies to assess its suitability for the treatment of colorectal cancer.
结直肠癌是最常见的肿瘤疾病之一。由于用于治疗该疾病的大多数药物都会使人虚弱，因此使用天然衍生产品可能对这种疾病的持续治疗极为有益，这些产品可以有效对抗突变细胞，此外，还可以减轻大多数与炎症相关的影响。在本研究中，原儿茶酸乙酯（PCAEE），一种原儿茶酸前药，被包裹在固体脂质纳米粒（SLN）中（分别在不添加和添加吐温80的情况下制备），并对其粒径、多分散指数（PDI）、zeta电位和热致行为进行了表征。还评估了包封率、释放曲线以及与生物膜模型的相互作用。纳米粒在健康细胞和肿瘤细胞模型上进行了体外测试。添加吐温80制备的SLN在物理化学性质（平均粒径190 nm，PDI 0.150，zeta电位约为-20 mV）和包封率（56%）方面表现良好；它们显示出理想的释放曲线，能够穿透并将包裹的PCAEE释放到生物膜模型中，且对健康细胞无毒。此外，与单独的PCAEE相比，它们对CaCo-2细胞活力的剂量依赖性降低作用更大。总之，该制剂可用于进一步研究，以评估其对结直肠癌治疗的适用性。
