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载橙皮苷 PLGA 的体外评价:对纳米递药系统的深入了解。

In vitro evaluation of PLGA loaded hesperidin on colorectal cancer cell lines: an insight into nano delivery system.

机构信息

Faculty of Pharmacy and Pharmaceutical Sciences, Tehran Medical Sciences, Islamic Azad University, Tehran, Iran.

Farhikhtegan Medical Convergence Sciences Research Center, Farhikhtegan Hospital Tehran Medical Sciences, Islamic Azad University, Tehran, Iran.

出版信息

BMC Biotechnol. 2024 Aug 2;24(1):52. doi: 10.1186/s12896-024-00882-1.

Abstract

BACKGROUND

Colorectal cancer is a common disease worldwide with non-specific symptoms such as blood in the stool, bowel movements, weight loss and fatigue. Chemotherapy drugs can cause side effects such as nausea, vomiting and a weakened immune system. The use of antioxidants such as hesperidin could reduce the side effects, but its low bioavailability is a major problem. In this research, we aimed to explore the drug delivery and efficiency of this antioxidant on the HCT116 colorectal cancer cell line by loading hesperidin into PLGA nanoparticles.

MATERIALS AND METHODS

Hesperidin loaded PLGA nanoparticles were produced by single emulsion evaporation method. The physicochemical properties of the synthesized hesperidin-loaded nanoparticles were determined using SEM, AFM, FT-IR, DLS and UV-Vis. Subsequently, the effect of the PLGA loaded hesperidin nanoparticles on the HCT116 cell line after 48 h was investigated by MTT assay at three different concentrations of the nanoparticles.

RESULT

The study showed that 90% of hesperidin were loaded in PLGA nanoparticles by UV-Vis spectrophotometry and FT-IR spectrum. The nanoparticles were found to be spherical and uniform with a hydrodynamic diameter of 76.2 nm in water. The release rate of the drug was about 93% after 144 h. The lowest percentage of cell viability of cancer cells was observed at a concentration of 10 µg/ml of PLGA nanoparticles loaded with hesperidin.

CONCLUSION

The results indicate that PLGA nanoparticles loaded with hesperidin effectively reduce the survival rate of HCT116 colorectal cancer cells. However, further studies are needed to determine the appropriate therapeutic dosage and to conduct animal and clinical studies.

摘要

背景

结直肠癌是一种常见的全球疾病,具有非特异性症状,如粪便带血、排便习惯改变、体重减轻和疲劳。化疗药物会引起恶心、呕吐和免疫系统减弱等副作用。使用桔皮苷等抗氧化剂可以减少副作用,但生物利用度低是一个主要问题。在这项研究中,我们旨在通过将桔皮苷载入 PLGA 纳米粒来探索这种抗氧化剂在 HCT116 结直肠癌细胞系中的药物传递和效率。

材料和方法

通过单乳液蒸发法制备桔皮苷负载的 PLGA 纳米粒。使用 SEM、AFM、FT-IR、DLS 和 UV-Vis 测定合成的桔皮苷负载纳米粒的物理化学性质。随后,通过 MTT 测定法在三个不同浓度的纳米粒作用 48 h 后,研究 PLGA 负载桔皮苷纳米粒对 HCT116 细胞系的影响。

结果

研究表明,通过 UV-Vis 分光光度法和 FT-IR 光谱,90%的桔皮苷被载入 PLGA 纳米粒中。纳米粒呈球形且均匀,水相中水动力学直径为 76.2nm。药物释放率在 144 h 后约为 93%。载有桔皮苷的 PLGA 纳米粒浓度为 10μg/ml 时,癌细胞的存活率最低。

结论

结果表明,PLGA 纳米粒负载桔皮苷可有效降低 HCT116 结直肠癌细胞的存活率。然而,需要进一步研究确定适当的治疗剂量,并进行动物和临床研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ad6e/11297711/a60da64dff5b/12896_2024_882_Fig1_HTML.jpg

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