Nikpour Mehrnoosh, Karami Zahra, Rafieenia Samaneh, Adibifar Arghavan, Yazdani Shaghayegh, Saghatchi Zanjani Fatemeh, Mortezazadeh Tohid, Abdi Zahra, Rostamizadeh Kobra
Pharmaceutical Nanotechnology Research Center, Zanjan University of Medical Sciences, Zanjan, Iran.
Department of Pharmaceutical Nanotechnology, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran.
Pharm Dev Technol. 2025 Jan;30(1):57-68. doi: 10.1080/10837450.2024.2448335. Epub 2025 Jan 10.
Chemotherapeutic agents are widely used to combat breast cancer. However, due to their non-selective biodistribution, their usage is associated with severe adverse effects on healthy tissues. In this study, a chitosan-stabilized nanoemulsion (CSNE) was prepared for the codelivery of curcumin (CUR) and methotrexate (MTX). The mean diameter and polydispersity index of CUR-MTX-CSNEs were 194.63 ± 6.7 nm and 0.27 ± 0.06, respectively. Modifying the nanoemulsion surface with chitosan decreased the drug release at pH 7.4 compared to pH 5.8. The MTT test demonstrated that CUR-MTX-CSNEs were more successful in reducing the cell viability of 4T1 cells than both bare formulation and free drugs. Moreover, compared to the free drug-treated group, a 2.6 times reduction of the relative tumor volume was witnessed in CUR-MTX-CSNEs-receiving mice. Histopathological studies confirmed a more substantial inhibitory effect on tumor growth and pulmonary metastasis of developed nanostructures than free CUR/MTX. While there was no noticeable toxicity in the vital organs of CUR-MTX-CSNEs-receiving mice, free drugs resulted in severe toxicity in the liver, kidney, lung and spleen. Overall, the pH-dependent drug release, improved anti-tumor activity and reduced organ toxicity suggest that CUR-MTX-CSNE may be promising in breast cancer therapy.
化疗药物被广泛用于对抗乳腺癌。然而,由于其非选择性的生物分布,其使用会对健康组织产生严重的副作用。在本研究中,制备了一种壳聚糖稳定的纳米乳剂(CSNE)用于姜黄素(CUR)和甲氨蝶呤(MTX)的共递送。CUR-MTX-CSNE的平均直径和多分散指数分别为194.63±6.7nm和0.27±0.06。与pH 5.8相比,用壳聚糖修饰纳米乳剂表面可降低pH 7.4时的药物释放。MTT试验表明,CUR-MTX-CSNE在降低4T1细胞的细胞活力方面比单纯制剂和游离药物都更成功。此外,与游离药物治疗组相比,接受CUR-MTX-CSNE的小鼠相对肿瘤体积减少了2.6倍。组织病理学研究证实,与游离CUR/MTX相比,所开发的纳米结构对肿瘤生长和肺转移具有更显著的抑制作用。虽然接受CUR-MTX-CSNE的小鼠重要器官没有明显毒性,但游离药物导致肝脏、肾脏、肺和脾脏出现严重毒性。总体而言,pH依赖的药物释放、改善的抗肿瘤活性和降低的器官毒性表明CUR-MTX-CSNE在乳腺癌治疗中可能具有前景。