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Oleic Acid Copolymer as A Novel Upconversion Nanomaterial to Make Doxorubicin-Loaded Nanomicelles with Dual Responsiveness to pH and NIR.
Pharmaceutics ( IF 5.4 ) Pub Date : 2020-07-20 , DOI: 10.3390/pharmaceutics12070680
Jin Zhang 1 , Xiaoyue Tang 1 , Chuanqing Huang 1 , Zeyu Liu 1 , Yong Ye 1
Affiliation  

Oleic acid (OA) as main component of plant oil is an important solvent but seldom used in the nanocarrier of anticancer drugs because of strong hydrophobicity and little drug release. In order to develop a new type of OA nanomaterial with dual responses to pH and near infrared light (NIR) to achieve the intelligent delivery of anticancer drugs. The novel OA copolymer (mPEG-PEI-(NBS, OA)) was synthesized by grafting OA and o-nitrobenzyl succinate (NBS) onto mPEGylated polyethyleneimine (mPEG-PEI) by amidation reaction. It was further conjugated with NaYF4:Yb3+/Er3+ nanoparticles, and encapsulated doxorubicin (DOX) through self-assembly to make upconversion nanomicelles with dual response to pH and NIR. Drug release behavior of DOX, physicochemical characteristics of the nanomicelles were evaluated, along with its cytotoxic profile, as well as the degree of cellular uptake in A549 cells. The encapsulation efficiency and drug loading capacity of DOX in the nanomicelles were 73.84% ± 0.58% and 4.62% ± 0.28%, respectively, and the encapsulated DOX was quickly released in an acidic environment exposed to irradiation at 980 nm. The blank nanomicelles exhibited low cytotoxicity and excellent biocompatibility by MTT assay against A549 cells. The DOX-loaded nanomicelles showed remarkable cytotoxicity to A549 cells under NIR, and promoted the cellular uptake of DOX into the cytoplasm and nucleus of cancer cells. OA copolymer can effectively deliver DOX to cancer cells and achieve tumor targeting through a dual response to pH and NIR.

中文翻译:

油酸共聚物是一种新型的上转换纳米材料,可制备对pH和NIR具有双重响应的负载阿霉素的纳米菌素。

作为植物油主要成分的油酸(OA)是重要的溶剂,但由于疏水性强且药物释放少,因此很少用于抗癌药物的纳米载体中。为了开发一种新型的OA纳米材料,该材料对pH和近红外光(NIR)都具有双重反应,以实现抗癌药物的智能传递。通过酰胺化反应将OA和硝基苄基琥珀酸酯(NBS)接枝到mPEG化聚乙烯亚胺(mPEG-PEI)上,合成了新型OA共聚物(mPEG-PEI-(NBS,OA))。进一步与NaYF 4:Yb 3+ / Er 3+共轭。纳米颗粒,并通过自组装封装了阿霉素(DOX),以制成对pH和NIR具有双重响应的上转换纳米胶束。评估了DOX的药物释放行为,纳米胶束的理化特性,以及其细胞毒性谱以及A549细胞的细胞摄取程度。在纳米胶束中,DOX的包封效率和载药量分别为73.84%±0.58%和4.62%±0.28%,并且在暴露于980 nm的酸性环境中,该DOX可以快速释放。通过针对A549细胞的MTT分析,空白纳米胶束显示出低细胞毒性和出色的生物相容性。载有DOX的纳米胶束在NIR下对A549细胞表现出显着的细胞毒性,并促进了DOX进入癌细胞的细胞质和细胞核的细胞摄取。
更新日期:2020-07-20
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