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卡培他滨载药尼奥斯omes 的制备、表征及评价。

Formulation, Characterization and and Evaluation of Capecitabine Loaded Niosomes.

机构信息

Institute of Research and Development, GFSU, Opposite to Directorate of Forensic Science, Sector-9, Gandhinagar- 382 007, Gujarat, India.

出版信息

Curr Drug Deliv. 2020;17(3):257-268. doi: 10.2174/1567201817666200214111815.

Abstract

BACKGROUND

Nanocarriers improve the efficacy of drugs by facilitating their specific delivery and protecting them from external environment resulting in a better performance against diseases.

OBJECTIVE

In this study, it was aimed to improve the efficacy of capecitabine against colorectal cancer by its entrapment in niosomes. Ether injection method was used to prepare niosomes composed of span 20 and cholesterol.

METHODS

Niosomes were evaluated by evaluating the entrapment efficiency, drug release and cytotoxicity of capecitabine loaded niosomes. Niosomes were characterized by particle size analysis, transmission electron microscopy, Fourier transform infrared spectroscopy and differential scanning calorimetry for surface morphology and drug excipient interactions.

RESULTS

High encapsulation efficiency (90.55%) was observed, which is anticipated to resolve the multi-drug resistance problem. Reported particle size was 180.9 + 5 nm with a negative zeta potential - 21 + 0.5 mV and the kinetic study showed a concentration-dependent release of the drug from the niosome. DSC study proved entrapment of the entire drug and its non-covalent bonding with the excipients. Cytotoxicity study of niosomes on CaCO2 cell line showed an improved IC value as compared to the free drug.

CONCLUSION

Enhanced cytotoxicity observed in the results further supports the suitability of niosome as a nanocarrier for pharmaceutical drug delivery.

摘要

背景

纳米载体通过促进药物的特异性递送并保护其免受外部环境的影响,从而提高药物的疗效,使其在对抗疾病方面表现更出色。

目的

本研究旨在通过将卡培他滨包封于脂质体中,提高其对结直肠癌的疗效。采用乙醚注入法制备由司盘 20 和胆固醇组成的脂质体。

方法

通过评估包封效率、药物释放和载有卡培他滨的脂质体的细胞毒性来评价脂质体。通过粒径分析、透射电子显微镜、傅里叶变换红外光谱和差示扫描量热法对脂质体的表面形态和药物赋形剂相互作用进行表征。

结果

观察到高包封效率(90.55%),有望解决多药耐药问题。报道的粒径为 180.9 ± 5nm,zeta 电位为负-21 ± 0.5mV,动力学研究表明药物从脂质体中呈浓度依赖性释放。DSC 研究证明了药物的全部包封及其与赋形剂的非共价结合。与游离药物相比,脂质体对 CaCO2 细胞系的细胞毒性研究显示出改善的 IC 值。

结论

结果中观察到的增强的细胞毒性进一步支持了脂质体作为药物传递的纳米载体的适用性。

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