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载布地奈德巯基化海藻酸钠纳米粒的制备、表征及药物释放行为:一种潜在的治疗炎症性肠病的药物传递系统。

Preparation, characterization, and drug release behavior of thiolated alginate nanoparticles loaded budesonide as a potential drug delivery system toward inflammatory bowel diseases.

机构信息

College of Marine Life Sciences, Ocean University of China, Qingdao, P.R. China.

School of Pharmacy, Binzhou Medical University, Yantai, P.R. China.

出版信息

J Biomater Sci Polym Ed. 2020 Dec;31(18):2299-2317. doi: 10.1080/09205063.2020.1803034. Epub 2020 Sep 3.

Abstract

For site-specific drug delivery in inflammatory bowel disease, reducible sodium alginate nanoparticles cross-linked with disulfide linkage were developed. Nanoparticles were synthesized in deionized water through self-assembly of amphiphilic thiolated sodium alginate Alg-Cys and subsequently produced cross-linking of disulfide bonds. TEM image showed a spherical core-shell configuration with a size of about 430 nm for the nanoparticles. Dynamic light scattering (DLS) showed high stability, narrow size distribution, and pH-dependent swelling transition for the nanoparticles. Cytotoxicity study showed that there was no evident cell inhibition among the nanoparticles. Also, the size of the nanoparticles increased in 10 mM glutathione (GSH) solution due to the cleavage of disulfides within their network structures. Compared to that in GSH-free buffer, there was a remarkable increase in drug release in pH 7.4 buffer with GSH from drug-loaded nanoparticles, indicating that the nanoparticles could be used for colon-specific drug delivery.

摘要

为了在炎症性肠病中进行靶向药物传递,开发了可还原的带有二硫键交联的海藻酸钠纳米粒子。纳米粒子通过两亲性巯基化海藻酸钠 Alg-Cys 的自组装在去离子水中合成,随后产生二硫键的交联。TEM 图像显示,纳米粒子具有约 430nm 的球形核壳结构。动态光散射(DLS)表明,纳米粒子具有高稳定性、窄粒径分布和 pH 依赖性溶胀转变。细胞毒性研究表明,纳米粒子之间没有明显的细胞抑制作用。此外,由于其网络结构中二硫键的断裂,纳米粒子在 10mM 谷胱甘肽(GSH)溶液中的尺寸增大。与无 GSH 的缓冲液相比,载药纳米粒子在 pH7.4 缓冲液中的药物释放显著增加,表明纳米粒子可用于结肠特异性药物传递。

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