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他莫昔芬导向介孔硅纳米粒子的概念设计、研制和初步物理化学特性研究。

Concept Design, Development and Preliminary Physical and Chemical Characterization of Tamoxifen-Guided-Mesoporous Silica Nanoparticles.

机构信息

Clinical and Health Sciences, University of South Australia, North Terrace, Adelaide, SA 5000, Australia.

Future Industry Institute, University of South Australia, Mawson Lakes, SA 5095, Australia.

出版信息

Molecules. 2021 Jan 4;26(1):219. doi: 10.3390/molecules26010219.

Abstract

Conventional chemotherapies used for breast cancer (BC) treatment are non-selective, attacking both healthy and cancerous cells. Therefore, new technologies that enhance drug efficacy and ameliorate the off-target toxic effects exhibited by currently used anticancer drugs are urgently needed. Here we report the design and synthesis of novel mesoporous silica nanoparticles (MSNs) equipped with the hormonal drug tamoxifen (TAM) to facilitate guidance towards estrogen receptors (ERs) which are upregulated in breast tumours. TAM is linked to the MSNs using a poly-ʟ-histidine (PLH) polymer as a pH-sensitive gatekeeper, to ensure efficient delivery of encapsulated materials within the pores. XRD, HR-TEM, DLS, SEM, FT-IR and BET techniques were used to confirm the successful fabrication of MSNs. The MSNs have a high surface area (>1000 m/g); and a mean particle size of 150 nm, which is an appropriate size to allow the penetration of premature blood vessels surrounding breast tumours. Successful surface functionalization was supported by FT-IR, XPS and TGA techniques, with a grafting ratio of approximately 29%. The outcomes of this preliminary work could be used as practical building blocks towards future formulations.

摘要

用于乳腺癌 (BC) 治疗的常规化疗是非选择性的,会攻击健康细胞和癌细胞。因此,迫切需要新的技术来提高药物疗效,并改善目前使用的抗癌药物所表现出的脱靶毒性作用。在这里,我们报告了一种新型介孔硅纳米粒子 (MSNs) 的设计和合成,该粒子配备了激素药物他莫昔芬 (TAM),以促进向在乳腺癌中上调的雌激素受体 (ER) 引导。TAM 与 MSNs 相连,使用聚 -L-组氨酸 (PLH) 聚合物作为 pH 敏感的关守物,以确保在孔内有效输送封装材料。XRD、HR-TEM、DLS、SEM、FT-IR 和 BET 技术用于确认 MSNs 的成功制造。MSNs 的比表面积>1000 m/g,平均粒径为 150nm,这是一个合适的尺寸,可以允许穿透围绕乳腺癌的早期血管。FT-IR、XPS 和 TGA 技术支持成功的表面功能化,接枝率约为 29%。这项初步工作的结果可以作为未来制剂的实际构建块。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cf31/7795496/973d93698a03/molecules-26-00219-sch001.jpg

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