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用于癌症靶向治疗的表柔比星赖氨酸修饰固体脂质纳米粒

Lysine Decorated Solid Lipid Nanoparticles of Epirubicin for Cancer Targeting and Therapy.

作者信息

Bayat Parvaneh, Pakravan Parvaneh, Salouti Mojtaba, Ezzati Nazhad Dolatabadi Jafar

机构信息

Department of Chemistry, Zanjan Branch, Islamic Azad University, Zanjan, Iran.

Nanobiotechnology Research Center, Zanjan Branch, Islamic Azad University, Zanjan, Iran.

出版信息

Adv Pharm Bull. 2021 Jan;11(1):96-103. doi: 10.34172/apb.2021.010. Epub 2020 Nov 7.

Abstract

Cancer is an example of the most important growing diseases in human society and scientists are trying to treat it without considerable side effects on patient's health. Solid lipids are colloidal nanoparticles that were used in drug delivery due to their several advantages. In this work, surface modified targeted solid lipid nanoparticles (SLNs) were fabricated by nano-homogenizer using tripalmitin glyceride and stearic acid as lipid constituents. The size of nanoparticles and morphological evaluations were surveyed using particle size analyzer, scanning electron microscopy; Fourier transforms infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). The particle size of 148.5 and appropriate polydispersity index were achieved for lipid nanoparticles with an entrapment efficiency of 86.1%. The FT-IR analysis confirmed the coupling of lysine to the free functional group of SLNs. DSC proved the conjugation of amino acid to the surface of carriers. The epirubicin (EPI) release test exhibited the further controlled release phenomenon for the lysine conjugated nanoparticles. The cytotoxicity assay showed lower IC50 of lysine conjugated SLNs of EPI on the investigated cell line. These studies showed that the fabricated targeted carrier has a very remarkable anticancer effect on breast cancer cell lines in comparison with pure drug.

摘要

癌症是人类社会中最重要的不断增长的疾病之一,科学家们正在努力在不对患者健康产生重大副作用的情况下对其进行治疗。固体脂质是胶体纳米颗粒,由于其多种优点而被用于药物递送。在这项工作中,使用三棕榈酸甘油酯和硬脂酸作为脂质成分,通过纳米均质器制备了表面改性的靶向固体脂质纳米颗粒(SLN)。使用粒度分析仪、扫描电子显微镜、傅里叶变换红外光谱(FT-IR)和差示扫描量热法(DSC)对纳米颗粒的尺寸和形态进行了评估。脂质纳米颗粒的粒径为148.5,具有合适的多分散指数,包封率为86.1%。FT-IR分析证实了赖氨酸与SLN的游离官能团偶联。DSC证明了氨基酸与载体表面的共轭。表柔比星(EPI)释放试验显示赖氨酸共轭纳米颗粒具有进一步的控释现象。细胞毒性试验表明,EPI的赖氨酸共轭SLN对所研究的细胞系具有较低的IC50。这些研究表明,与纯药物相比,所制备的靶向载体对乳腺癌细胞系具有非常显著的抗癌作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1559/7961234/847f3e566cab/apb-11-96-g006.jpg

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