研究动态
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5-氟尿嘧啶和抗EGFR抗体结构蛋白质壳聚糖稳定的皮克林乳液:配方、物理表征、对NCL-H226细胞的体外研究和对Wistar大鼠的体内研究,以增强对鳞状细胞癌的治疗效果。

5-Fluorouracil and Anti-EGFR antibody scaffold chitosan-stabilized Pickering emulsion: Formulations, physical characterization, in-vitro studies in NCL-H226 cells, and in-vivo investigations in Wistar rats for the augmented therapeutic effects against squamous cell carcinoma.

发表日期:2023 Sep 04
作者: Sankha Bhattacharya, Prafull Shinde, Amit Page, Satyam Sharma
来源: Int J Biol Macromol

摘要:

本研究旨在优化壳聚糖稳定的Pickering乳液(PE),其中含有5-氟尿嘧啶(5-FU)作为潜在的鳞癌治疗药物。同时,采用紫外-可见分光光度法和反相高效液相色谱法(RP-HPLC)对5-氟尿嘧啶进行了全面分析,结果显示具有良好的线性度、灵敏度、精密度和稳健性。表征技术揭示了Pickering乳液(PE)的形态学特征、固体凝胶性质、成功的包封效果和良好的抗癌效果。傅里叶变换红外光谱(FTIR)用于验证包封的效力,差示扫描量热仪(DSC)用于确认后包封药物的稳定性。0.6%壳聚糖稳定的PE表现出良好的稳定性和药物负载效率。开发了抗EGFR-5-FU-CS-PE凝胶以实现持续药物释放,用于鳞癌的治疗。体外实验证明,抗EGFR-5-FU-CS-PE表现出强大的抗癌效果,IC50低于5-FU和5-FU-CS-PE。基于壳聚糖的抗EGFR-5-FU-PE Pickering乳液的流变特性、细胞相互作用和治疗潜力进行了研究。两种乳液和凝胶在成功包封后表现出持续的体外药物释放。抗EGFR-5-FU-CS-PE可诱导细胞凋亡,降低线粒体膜电位,抑制癌细胞迁移。还对Wistar小鼠进行了安全性和抑制肿瘤生长的测试。所有配方都表现出出色的六个月稳定性。抗EGFR-5-FU-CS-PE表现为可行的治疗选择,需要进一步研究。版权所有 © 2023. Elsevier B.V. 发布。
This research seeks to optimize a chitosan-stabilized Pickering emulsion (PE) containing 5-fluorouracil (5-FU) as a potential Squamous Cell Carcinoma therapy. The 5-Fluorouracil was also thoroughly analysed using UV spectrophotometry and RP-HPLC, demonstrating exceptional linearity, sensitivity, precision, and robustness. The techniques of characterization revealed Pickering emulsion (PE) morphology, solid-like gel properties, successful encapsulation, and promising anticancer effects. FTIR was used to validate the efficacy of encapsulation, and DSC was used to confirm the post-encapsulation drug stability. The 0.6 % chitosan-stabilized PE showed exceptional stability and drug loading efficiency. Anti-EGFR-5-FU-CS-PE gel was developed for sustained drug release in the treatment of Squamous Cell Carcinoma. Anti-EGFR-5-FU-CS-PE demonstrated potent anticancer effects in vitro, with a lower IC50 than 5-FU and 5-FU-CS-PE. Anti-EGFR-5-FU-PE Pickering emulsions based on chitosan were investigated for their rheological properties, cellular interactions, and therapeutic potential. Both emulsions and gel exhibited sustained in vitro drug release after successful encapsulation. Anti-EGFR-5-FU-CS-PE induced apoptosis, decreased mitochondrial membrane potential, and inhibited the migration of cancer cells. Wistar mice were tested for safety and tumour growth inhibition. All formulations exhibited exceptional six-month stability. Anti-EGFR-5-FU-CS-PE emerges as a viable therapeutic option, necessitating additional research.Copyright © 2023. Published by Elsevier B.V.