Ngema Lindokuhle M, Adeyemi Samson A, Marimuthu Thashree, Ubanako Philemon, Wamwangi Daniel, Choonara Yahya E
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.
Pharmaceutics. 2022 Apr 11;14(4):829. doi: 10.3390/pharmaceutics14040829.
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.
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。