Suppr超能文献

用于乳腺癌靶向的PLGA-SPC3功能化吉非替尼介孔二氧化硅纳米支架的研发:生物分布及细胞毒性分析

Development of PLGA-SPC3 functionalized gefitinib mesoporous silica nano-scaffolds for breast cancer targeting: biodistribution and cytotoxicity analysis.

作者信息

Sah Ravi Kumar, Kumar B Sajeev

机构信息

Nirmal Lama Polytechnique Institute, Mahottari, Nepal.

Professor, Department of Pharmaceutics, College of Pharmaceutical Sciences, Dayananda Sagar University, Harohalli, India.

出版信息

Pharm Dev Technol. 2025 Feb;30(2):160-176. doi: 10.1080/10837450.2025.2460732. Epub 2025 Feb 13.

Abstract

The exploration of novel carriers for cancer treatments is on the rise, as drugs are often hindered by ineffective delivery. In the present study, Mesoporous silica nano scaffolds were developed by a novel heat assisted hydrolysis (HAH) technique, and were functionalized using PLGA. These carriers were further loaded with nanosized Gefitinib (GTB). The surface properties of MSNs (GTB-PEG-PLGA-MSN) were enhanced using 1-oleoyl-2-hydroxy-sn-glycero-3-phosphocholine (SPC3). The MSNs were characterized for pore volume, particle size, zeta potential (ZP), surface area, entrapment efficiency (%EE), and drug content. The drug release kinetics, cytotoxicity analysis, and biodistribution studies were performed in optimized MSN using Albino Wistar rats. The result shows an increase in surface area, pore volume, %EE, and drug loading in MSN. cytotoxicity of optimized F5-GTB-PEG-PLGA-SPC3-MSN demonstrated a higher antitumor activity (43.84 ± 0.63%,  0.05) in comparison to free drug. A higher GTB was detected in the liver (29,415 ± 126 ng) indicating significant biodistribution ( > 0.05). The studies in the MCF-7 cell line signify an increase in cell viability demonstrating its efficacy in breast cancer. Optimized F5-GTB-PEG-PLGA-SPC3-MSN offers improved cellular uptake, biodistribution, and higher antitumor suppression with less toxicity. To conclude, the HAH technique produced stable MSNs, and PLGA-SPC3 functionalized MSN nano scaffolds could be an ideal carrier for cancer drug delivery.

摘要

由于药物递送效率低下常常阻碍药物发挥作用,新型癌症治疗载体的探索日益兴起。在本研究中,通过一种新型热辅助水解(HAH)技术制备了介孔二氧化硅纳米支架,并使用聚乳酸-羟基乙酸共聚物(PLGA)对其进行功能化修饰。这些载体进一步负载了纳米尺寸的吉非替尼(GTB)。使用1-油酰基-2-羟基-sn-甘油-3-磷酸胆碱(SPC3)增强了介孔二氧化硅纳米颗粒(GTB-PEG-PLGA-MSN)的表面性质。对介孔二氧化硅纳米颗粒的孔体积、粒径、zeta电位(ZP)、表面积、包封率(%EE)和药物含量进行了表征。在白化Wistar大鼠体内对优化后的介孔二氧化硅纳米颗粒进行了药物释放动力学、细胞毒性分析和生物分布研究。结果显示,介孔二氧化硅纳米颗粒的表面积、孔体积、%EE和药物负载量均有所增加。与游离药物相比,优化后的F5-GTB-PEG-PLGA-SPC3-MSN的细胞毒性表现出更高的抗肿瘤活性(43.84 ± 0.63%,P < 0.05)。在肝脏中检测到较高的GTB含量(29,415 ± 126 ng),表明其具有显著的生物分布(P > 0.05)。在MCF-7细胞系中的研究表明细胞活力增加,证明了其对乳腺癌的疗效。优化后的F5-GTB-PEG-PLGA-SPC3-MSN具有更好的细胞摄取、生物分布,以及更高的抗肿瘤抑制作用和更低的毒性。总之,HAH技术制备出了稳定的介孔二氧化硅纳米颗粒,PLGA-SPC3功能化的介孔二氧化硅纳米支架可能是癌症药物递送的理想载体。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验