Development of Zwitterionic Polypeptide Nanoformulation with High Doxorubicin Loading Content for Targeted Drug Delivery.,Langmuir

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Development of Zwitterionic Polypeptide Nanoformulation with High Doxorubicin Loading Content for Targeted Drug Delivery.
Langmuir ( IF 3.7 ) Pub Date : 2018-07-10 , DOI: 10.1021/acs.langmuir.8b00851
Weifeng Lin ₁ , Guanglong Ma ₁ , Zhefan Yuan ₁ , Haofeng Qian ₁ , Liangbo Xu ₁ , Elie Sidransky ₂ , Shengfu Chen _{1,

3}

Affiliation

Much attention has been drawn to targeted nanodrug delivery systems due to their high therapeutic efficacy in cancer treatment. In this work, doxorubicin (DOX) was incorporated into a zwitterionic arginyl-glycyl-aspartic acid (RGD)-conjugated polypeptide by an emulsion solvent evaporation technique with high drug loading content (45%) and high drug loading efficiency (95%). This zwitterionic nanoformulation showed excellent colloidal stability at high dilution and in serum. The pH-induced disintegration and enzyme-induced degradation of the nanoformulation were confirmed by dynamic light scattering and gel permeation chromatography. Efficient internalization of DOX in the cells and high antitumor activity in vitro was observed. Compared with the free drug, this nanoformulation showed higher accumulation in tumor and lower systemic toxicity in vivo. The DOX-loaded zwitterionic RGD-conjugated polypeptide vesicles show potential application for targeted drug delivery in the clinic.

中文翻译：

具有高阿霉素负载量的两性离子多肽纳米配方的开发，用于靶向药物递送。

由于靶向纳米药物递送系统在癌症治疗中的高治疗功效，因此已经引起了很多关注。在这项工作中，通过乳剂溶剂蒸发技术将阿霉素（DOX）掺入两性离子精氨酰基-甘氨酰-天冬氨酸（RGD）结合的多肽中，该方法具有高载药量（45％）和高载药率（95％）。该两性离子纳米制剂在高稀释度和血清中显示出优异的胶体稳定性。通过动态光散射和凝胶渗透色谱法证实了pH诱导的纳米制剂的崩解和酶诱导的降解。观察到细胞中DOX的有效内在化和体外高抗肿瘤活性。与游离药物相比，这种纳米制剂在肿瘤中显示出更高的蓄积性和更低的体内全身毒性。

更新日期：2018-06-22

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