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基于葡聚糖嵌段多肽共聚物的中空有机/无机杂化纳米粒子:双击反应合成与性能。

Hollow organic/inorganic hybrid nanoparticles from dextran-block-polypeptide copolymer: Double click reaction synthesis and properties.

机构信息

DSAPM Lab and PCFM Lab, School of Materials Science and Engineering, Sun Yat-sen University, Guangzhou 510275, China; Department of Radiology, Guangzhou First People's Hospital, School of Medicine, South China University of Technology, Guangzhou, Guangdong 510640, China.

DSAPM Lab and PCFM Lab, School of Materials Science and Engineering, Sun Yat-sen University, Guangzhou 510275, China.

出版信息

Int J Biol Macromol. 2021 Jun 30;181:1243-1253. doi: 10.1016/j.ijbiomac.2021.05.101. Epub 2021 May 20.

DOI:10.1016/j.ijbiomac.2021.05.101
PMID:34022305
Abstract

To increase the drug loading and prolong the drug release time, novel hollow organic/inorganic hybrid nanoparticles based on dextran-b-poly(L-glutamate-graft-3-mercaptopropyltrimethoxysilane) (Dex-b-P(ALG-g-MTPMS)) were prepared. First, a polysaccharide block polypeptide diblock copolymer, dextran-block-poly(γ-allyl-L-glutamate) (Dex-b-PALG) bearing allyl side-groups, has been synthesized by the combination of ring-opening polymerization and alkyne-azide [2 + 3] Huisgen's cycloaddition. Next, the allyl side-groups residing in the poly(γ-allyl-L-glutamate) block were further functionalized with 3-mercaptopropyltrimethoxysilane(MPTMS) by radical "thiol-ene" addition reactions. Finally, after a sol-gel process of the obtained copolymers, the novel organic/inorganic hybrid nanoparticles were prepared. The molecular structures, physicochemical, and self-assembly of these copolymers were characterized through FTIR, H NMR, dynamic light scattering (DLS), transmission electron microscopy (TEM), and scanning electron microscopy (SEM). The cross-linked hybrid nanoparticles have a higher drug loading ability and slower release rate as compared to the uncross-linked counterparts. The MTT evaluation demonstrated that the organic/inorganic hybrid nanoparticles with good biocompatibility.

摘要

为了提高载药量并延长药物释放时间,制备了基于葡聚糖-b-聚(L-谷氨酸接枝-3-巯丙基三甲氧基硅烷)(Dex-b-P(ALG-g-MTPMS))的新型中空有机/无机杂化纳米粒子。首先,通过开环聚合和炔基-叠氮化物[2 + 3] Huisgen 环加成反应合成了带有烯丙基侧基的多糖嵌段多肽两亲性嵌段共聚物,葡聚糖嵌段-聚(γ-烯丙基-L-谷氨酸)(Dex-b-PALG)。接下来,通过自由基“硫醇-烯”加成反应进一步将存在于聚(γ-烯丙基-L-谷氨酸)嵌段中的烯丙基侧基官能化与 3-巯丙基三甲氧基硅烷(MPTMS)。最后,通过获得的共聚物的溶胶-凝胶过程,制备了新型有机/无机杂化纳米粒子。通过傅里叶变换红外光谱(FTIR)、核磁共振氢谱(H NMR)、动态光散射(DLS)、透射电子显微镜(TEM)和扫描电子显微镜(SEM)对这些共聚物的分子结构、物理化学性质和自组装进行了表征。交联杂化纳米粒子具有更高的载药能力和较慢的释放速率,与未交联的相比。MTT 评价表明,具有良好生物相容性的有机/无机杂化纳米粒子。

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