Safwat Sally, Ishak Rania A H, Hathout Rania M, Mortada Nahed D
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Ther Deliv. 2025 Jan;16(1):43-61. doi: 10.1080/20415990.2024.2433938. Epub 2024 Nov 26.
Breast cancer is the second leading cause of death worldwide. Conventional chemotherapeutic therapies lack the specific targeting effect toward the cancerous cells resulting in extensive side effects. Our current study endeavors to prepare novel bioinspired folic acid-functionalized caffeic acid (CA)-loaded casein nanoparticles (CS NPs) for curbing breast cancer.
CA-CS NPs were prepared by simple coacervation method followed by lyophilization. Functionalized CS NPs were achieved using folic acid as the targeting moiety. Entire comparative characterization between unconjugated and conjugated NPs were implemented in terms of size, polydispersity index, surface charge, H-NMR, surface morphology, drug release, sterilization, cytotoxicity, and animal studies.
Conjugated NPs attained PS = 157.23 ± 2.64 nm, PDI = 0.309 ± 0.199, ZP = -25.53 ± 2.31 mV and IC50 = 40 ± 2.9 µg/ml. Significant reduction in the biochemical marker levels of Carcino-embryonic antigen, carbohydrate antigen 15-3, and malondialdehyde while increased superoxide dismutase levels were achieved in the tumor -induced rats treated by the conjugated NPs. Histopathological examinations showed great improvement in the mammary and necrotic regions.
The present work paves the road of 'back to nature' approach in designing biocompatible bioinspired conjugated nanocarriers for the diagnosis and treatment of various diseases.
乳腺癌是全球第二大致死原因。传统化疗方法对癌细胞缺乏特异性靶向作用，会产生广泛的副作用。我们目前的研究致力于制备新型的受生物启发的叶酸功能化的负载咖啡酸（CA）的酪蛋白纳米颗粒（CS NPs）来抑制乳腺癌。
通过简单的凝聚法制备CA-CS NPs，然后进行冻干。使用叶酸作为靶向部分制备功能化的CS NPs。从未缀合和缀合的纳米颗粒之间的整体比较表征在尺寸、多分散指数、表面电荷、H-NMR、表面形态、药物释放、灭菌、细胞毒性和动物研究方面进行。
缀合的纳米颗粒的粒径为PS = 157.23±2.64 nm，多分散指数为PDI = 0.309±0.199，表面电位为ZP = -25.53±2.31 mV，半数抑制浓度为IC50 = 40±2.9 μg/ml。在接受缀合纳米颗粒治疗的肿瘤诱导大鼠中，癌胚抗原、糖类抗原15-3和丙二醛的生化标志物水平显著降低，而超氧化物歧化酶水平升高。组织病理学检查显示乳腺和坏死区域有很大改善。
目前的工作为设计用于各种疾病诊断和治疗的生物相容性受生物启发的缀合纳米载体铺平了“回归自然”方法的道路。
