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他莫昔芬偶联的、环保的、基于琼脂的混合磁性纳米粒子的制备及其在乳腺癌治疗中的潜在应用评估

Preparation and Evaluation of Tamoxifen-Conjugated, Eco-Friendly, Agar-Based Hybrid Magnetic Nanoparticles for Their Potential Use in Breast Cancer Treatment.

作者信息

Khan Zanib, Sattar Sadia, Abubakar Muhammad, Arshed Muhammad Javed, Aslam Roohi, Shah Syed Tahir Abbas, Javed Sundus, Tariq Aamira, Manzoor Shumaila, Bostan Nazish

机构信息

Molecular Virology Labs, Department of Biosciences, COMSATS University Islamabad, Islamabad Campus, Islamabad 45550, Pakistan.

National Veterinary Laboratory, National Agricultural Research Centre, Park Road, Islamabad 45300, Pakistan.

出版信息

ACS Omega. 2023 Jul 14;8(29):25808-25816. doi: 10.1021/acsomega.3c00844. eCollection 2023 Jul 25.

Abstract

Tamoxifen is the drug of choice as hormonal therapy for hormone receptor-positive breast cancers and can reduce the risk of breast cancer recurrence. However, oral tamoxifen has a low bioavailability due to liver and intestinal metabolic passes. To overcome this problem and utilize the potential of this drug to its maximum, inorganic nanoparticle carriers have been exploited and tested to increase its bioavailability. Biocompatibility and unique magnetic properties make iron oxide nanoparticles an excellent choice as a drug delivery system. In this study, we developed and tested a "green synthesis" approach to synthesize iron nanoparticles from green tea extract and coated them with agar for longer stability (AG-INPs). Later, these hybrid nanoparticles were conjugated with tamoxifen (TMX). By using this approach, we synthesized stable agar-coated tamoxifen-conjugated iron nanoparticles (TMX-AG-INPs) and characterized them with Fourier-transform infrared (FTIR) spectroscopy. The average particle size of AG-INPs was 26.8 nm, while the average particle size of tamoxifen-loaded iron nanoparticles, TMX-AG-INPs, was 32.1 nm, as measured by transmission and scanning electron microscopy. The entrapment efficiency of TMX-AG-INPs obtained by the drug release profile was 88%, with a drug loading capacity of 43.5%. TMX-AG-INPs were significantly ( < 0.001) efficient in killing breast cancer cells when tested on the established breast cancer cell line MCF-7 by cell viability assay, indicating their potential to control cell proliferation.

摘要

他莫昔芬是激素受体阳性乳腺癌激素治疗的首选药物,可降低乳腺癌复发风险。然而,由于肝脏和肠道的代谢过程,口服他莫昔芬的生物利用度较低。为克服这一问题并充分发挥该药物的潜力,人们已开发并测试了无机纳米颗粒载体以提高其生物利用度。生物相容性和独特的磁性使氧化铁纳米颗粒成为药物递送系统的理想选择。在本研究中,我们开发并测试了一种“绿色合成”方法,即从绿茶提取物中合成铁纳米颗粒并用琼脂包被以提高稳定性(AG-INPs)。随后,将这些杂化纳米颗粒与他莫昔芬(TMX)偶联。通过这种方法,我们合成了稳定的琼脂包被的他莫昔芬偶联铁纳米颗粒(TMX-AG-INPs),并用傅里叶变换红外(FTIR)光谱对其进行了表征。通过透射电子显微镜和扫描电子显微镜测量,AG-INPs的平均粒径为26.8 nm,而载有他莫昔芬的铁纳米颗粒TMX-AG-INPs的平均粒径为32.1 nm。通过药物释放曲线获得的TMX-AG-INPs的包封率为88%,载药量为43.5%。通过细胞活力测定法在已建立的乳腺癌细胞系MCF-7上进行测试时,TMX-AG-INPs在杀死乳腺癌细胞方面具有显著效率(<0.001),表明它们具有控制细胞增殖的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bbc/10372931/05c7f7172f7a/ao3c00844_0002.jpg

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