PMPC Modified PAMAM Dendrimer Enhances Brain Tumor‐Targeted Drug Delivery,Macromolecular Bioscience

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PMPC Modified PAMAM Dendrimer Enhances Brain Tumor‐Targeted Drug Delivery
Macromolecular Bioscience ( IF 4.4 ) Pub Date : 2021-01-27 , DOI: 10.1002/mabi.202000392
Jiamin Ban ₁ , Sidi Li _{1,

2} , Qi Zhan ₁ , Xuepin Li ₁ , Huike Xing ₁ , Ning Chen ₁ , Lixia Long ₁ , Xin Hou ₁ , Jin Zhao ₁ , Xubo Yuan ₁

Affiliation

The excellent biocompatibility drug delivery system for effective treatment of glioma is still greatly challenged by the existence of blood–brain barrier, blood–brain tumor barrier, and the tissue toxicity caused by chemotherapy drugs. In this study, poly(2‐methacryloyloxyethyl phosphorylcholine) (PMPC) is used for the first time for modifying third‐generation poly(amidoamine) (PAMAM) to enhance their brain tumor‐targeted drug delivery ability as well as simultaneously reducing the toxicity of PAMAM dendrimers and the tissue toxicity of the loaded doxorubicin (DOX). The cytotoxicity, the therapeutic ability in vitro, and the brain tumor‐targeted ability of the PMPC modified PAMAM nanoparticles are further studied. Results indicate that PMPC, as a dual‐functional modifier, can significantly reduce the cytotoxicity of PAMAM dendrimers, while efficiently target the brain tumor. In addition, the therapeutic effect of DOX‐loaded PAMAM‐PMPC in mice inoculated with U‐87 is also studied in vivo. In comparison with DOX solution, DOX‐loaded PAMAM‐PMPC alleviates weight loss of tumor‐inoculated mice and reduces the cardiotoxicity of DOX. The tumor growth inhibition, in vivo, is significantly increased up to (80.76 ± 1.66)%. In conclusion, this strategy of PMPC dual‐functional targeted nanocarrier provides a new method for the delivery of chemotherapeutic drugs to treat glioma.

中文翻译：

PMPC 修饰的 PAMAM 树枝状聚合物增强脑肿瘤靶向药物递送

血脑屏障、血脑肿瘤屏障的存在以及化疗药物引起的组织毒性，对有效治疗胶质瘤的优良生物相容性药物递送系统仍然存在很大挑战。本研究首次使用聚（2-甲基丙烯酰氧基乙基磷酰胆碱）（PMPC）修饰第三代聚（酰胺胺）（PAMAM）以增强其脑肿瘤靶向药物递送能力，同时降低其毒性。 PAMAM 树枝状聚合物和负载多柔比星 (DOX) 的组织毒性。进一步研究了 PMPC 修饰的 PAMAM 纳米粒子的细胞毒性、体外治疗能力和脑肿瘤靶向能力。结果表明，PMPC 作为一种双功能改性剂，可以显着降低 PAMAM 树枝状聚合物的细胞毒性，同时有效靶向脑肿瘤。此外，还在体内研究了载有 DOX 的 PAMAM-PMPC 对接种 U-87 的小鼠的治疗效果。与 DOX 溶液相比，负载 DOX 的 PAMAM-PMPC 减轻了肿瘤接种小鼠的体重减轻并降低了 DOX 的心脏毒性。体内肿瘤生长抑制显着增加至 (80.76 ± 1.66)%。总之，PMPC双功能靶向纳米载体的这种策略为递送化疗药物治疗胶质瘤提供了一种新方法。在体内，显着增加到（80.76±1.66）％。总之，PMPC双功能靶向纳米载体的这种策略为递送化疗药物治疗胶质瘤提供了一种新方法。在体内，显着增加到（80.76±1.66）％。总之，PMPC双功能靶向纳米载体的这种策略为递送化疗药物治疗胶质瘤提供了一种新方法。

更新日期：2021-01-27

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