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A Self-assembled Nanoparticle Platform Based on Amphiphilic Oleanolic Acid Polyprodrug for Cancer Therapy
Chinese Journal of Polymer Science ( IF 4.1 ) Pub Date : 2020-04-22 , DOI: 10.1007/s10118-020-2401-2
Ying-Sa Wang , Gui-Liang Li , Shang-Bin Zhu , Fan-Chen Jing , Run-Dong Liu , Sai-Sai Li , Jing He , Jian-Du Lei

Oleanolic acid (OA) is a pentacyclic triterpenoid compound with extensive biological effects, such as anti-inflammatory and anticancer activities. However, the application of OA in chemotherapy is hampered by its poor solubility and severe adverse effects. To solve the problems, we developed a self-assembled nanoparticle platform based on amphiphilic oleanolic acid polyprodrug, poly[oligo(ethylene glycol) methyl ether methacrylate]-b-poly[oleanolic acid methacrylate] (POEGMA-b-POAMA), encapsulating 10-hydroxycamptothecin (HCPT) to achieve efficient cancer therapy. The polyprodrug was prepared via reversible addition-fragmentation chain transfer polymerization (RAFT), and could self-assemble to prepare POEGMA-b-POAMA/HCPT nanoparticles (NPs). The obtained nanoparticles exhibited appropriate particle size, excellent drug stability, good drug loading capacity, and high drug loading efficiency. In vitro drug release indicated that the drug release was prolonged to 132 h. The POEGMA-b-POAMA/HCPT NPs enhanced cell cytotoxicity in 4T1 cells and MCF-7 cells and could be efficiently uptaken by 4T1 cells. Furthermore, in vivo antitumor efficiency showed that the POEGMA-b-POAMA/HCPT NPs had great antitumor efficiency with considerably low adverse effects in the treatment of the 4T1 mouse breast tumor xenograft tumor. Therefore, POEGMA-b-POAMA/HCPT NPs provide great potential as a platform for drug delivery applications.



中文翻译:

基于两亲齐墩果酸多前体药物的自组装纳米粒子平台。

齐墩果酸(OA)是一种五环三萜类化合物,具有广泛的生物学作用,例如抗炎和抗癌活性。然而,OA在化学疗法中的应用由于其不良的溶解性和严重的副作用而受到阻碍。为了解决这些问题,我们开发了一种基于两亲齐墩果酸聚前药,聚[低聚(乙二醇)甲基醚甲基丙烯酸甲酯] -b-聚[聚甲基丙烯酸油醇酯](POEGMA- b -POAMA)的自组装纳米颗粒平台,其封装为10 -羟基喜树碱(HCPT)实现有效的癌症治疗。所述polyprodrug制备经由可逆加成-断裂链转移聚合(RAFT),并且可以自组装以制备POEGMA- b-POAMA / HCPT纳米粒子(NP)。所获得的纳米颗粒表现出适当的粒径,优异的药物稳定性,良好的载药量和较高的载药效率。体外药物释放表明药物释放被延长至132小时。POEGMA- b- POAMA / HCPT NPs增强了4T1细胞和MCF-7细胞的细胞毒性,可以被4T1细胞有效摄取。此外,体内抗肿瘤效率显示,POEGMA -b -POAMA / HCPT NP在治疗4T1小鼠乳腺肿瘤异种移植肿瘤中具有很高的抗肿瘤效率,且不良反应极低。因此,POEGMA -b -POAMA / HCPT NP作为药物输送应用的平台具有巨大的潜力。

更新日期:2020-04-23
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