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新型共轭亚油酸(CLA)包覆的超顺磁性氧化铁纳米颗粒(SPIONs)的合成及其用于紫杉醇递送并增强对A549肺癌细胞的体外抗增殖活性

Synthesis of Novel Conjugated Linoleic Acid (CLA)-Coated Superparamagnetic Iron Oxide Nanoparticles (SPIONs) for the Delivery of Paclitaxel with Enhanced In Vitro Anti-Proliferative Activity on A549 Lung Cancer Cells.

作者信息

Ngema Lindokuhle M, Adeyemi Samson A, Marimuthu Thashree, Ubanako Philemon, Wamwangi Daniel, Choonara Yahya E

机构信息

Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, 7 York Road, Parktown, Johannesburg 2193, South Africa.

School of Physics, Materials Physics Research Institute, University of the Witwatersrand, Private Bag 3, WITS, Johannesburg 2050, South Africa.

出版信息

Pharmaceutics. 2022 Apr 11;14(4):829. doi: 10.3390/pharmaceutics14040829.

Abstract

The application of Superparamagnetic Iron Oxide Nanoparticles (SPIONs) as a nanomedicine for Non-Small Cell Lung Carcinoma (NSCLC) can provide effective delivery of anticancer drugs with minimal side-effects. SPIONs have the flexibility to be modified to achieve enhanced oading of hydrophobic anticancer drugs such as paclitaxel (PTX). The purpose of this study was to synthesize novel -10, -12 conjugated linoleic acid (CLA)-coated SPIONs loaded with PTX to enhance the anti-proliferative activity of PTX. CLA-coated PTX-SPIONs with a particle size and zeta potential of 96.5 ± 0.6 nm and -27.3 ± 1.9 mV, respectively, were synthesized. The superparamagnetism of the CLA-coated PTX-SPIONs was confirmed, with saturation magnetization of 60 emu/g and 29 Oe coercivity. CLA-coated PTX-SPIONs had a drug loading efficiency of 98.5% and demonstrated sustained site-specific in vitro release of PTX over 24 h (i.e., 94% at pH 6.8 mimicking the tumor microenvironment). Enhanced anti-proliferative activity was also observed with the CLA-coated PTX-SPIONs against a lung adenocarcinoma (A549) cell line after 72 h, with a recorded cell viability of 17.1%. The CLA-coated PTX-SPIONs demonstrated enhanced suppression of A549 cell proliferation compared to pristine PTX, thus suggesting potential application of the nanomedicine as an effective site-specific delivery system for enhanced therapeutic activity in NSCLC therapy.

摘要

超顺磁性氧化铁纳米颗粒(SPIONs)作为一种用于非小细胞肺癌(NSCLC)的纳米药物,能够以最小的副作用有效递送抗癌药物。SPIONs具有可修饰的灵活性,以实现对疏水性抗癌药物如紫杉醇(PTX)的增强负载。本研究的目的是合成负载PTX的新型-10、-12共轭亚油酸(CLA)包被的SPIONs,以增强PTX的抗增殖活性。合成了粒径和zeta电位分别为96.5±0.6 nm和-27.3±1.9 mV的CLA包被的PTX-SPIONs。证实了CLA包被的PTX-SPIONs的超顺磁性,其饱和磁化强度为60 emu/g,矫顽力为29 Oe。CLA包被的PTX-SPIONs的载药效率为98.5%,并在24小时内显示出PTX在体外的持续位点特异性释放(即在pH 6.8模拟肿瘤微环境下为94%)。72小时后,CLA包被的PTX-SPIONs对肺腺癌(A549)细胞系也观察到增强的抗增殖活性,记录的细胞活力为17.1%。与原始PTX相比,CLA包被的PTX-SPIONs对A549细胞增殖的抑制作用增强,因此表明该纳米药物作为一种有效的位点特异性递送系统在NSCLC治疗中增强治疗活性具有潜在应用价值。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6096/9031641/bd0db879d98c/pharmaceutics-14-00829-g001.jpg

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