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乳糖化 IR820/DOX 共组装纳米药物用于协同抗肿瘤治疗。

Lactosylated IR820/DOX Co-Assembled Nanodrug for Synergetic Antitumour Therapy.

机构信息

Department of Pharmaceutics, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong Province, People's Republic of China.

Department of Pharmacy, Third Affiliated Hospital of Zhengzhou University, Zhengzhou, People's Republic of China.

出版信息

Int J Nanomedicine. 2020 Jun 22;15:4431-4440. doi: 10.2147/IJN.S247617. eCollection 2020.

DOI:10.2147/IJN.S247617
PMID:32606687
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7320228/
Abstract

INTRODUCTION

Synergistic treatment integrating photothermal therapy (PTT) and chemotherapy is a promising strategy for hepatocellular carcinoma (HCC). However, the most commonly used photothermal agent, IR820, and chemotherapeutic drug, doxorubicin hydrochloride (DOX), are both hydrophilic molecules that suffer from the drawbacks of a short circulation time, rapid elimination and off-target effects.

METHODS AND RESULTS

Herein, a novel nanodrug that combined HCC-targeted IR820 and DOX was developed based on excipient-free co-assembly. First, lactosylated IR820 (LA-IR820) was designed to target HCC. Then, the LA-IR820/DOX nanodrug (LA-IR820/DOX ND) was purely self-assembled without excipient assistance. The physicochemical properties and the chemo-photothermal antitumour activity of the excipient-free LA-IR820/DOX ND were evaluated. More importantly, the obtained LA-IR820/DOX ND exhibited 100% drug loading, remarkable HCC targeting and excellent antitumour efficacy.

CONCLUSION

This excipient-free LA-IR820/DOX ND may be a promising candidate for the synchronous delivery and synergistic targeting of IR820 and DOX as a combined chemo-photothermal therapy.

摘要

简介

整合光热疗法（PTT）和化疗的协同治疗是肝细胞癌（HCC）的一种很有前途的策略。然而，最常用的光热剂 IR820 和化疗药物盐酸多柔比星（DOX）都是亲水性分子，它们存在循环时间短、快速消除和脱靶效应等缺点。

方法和结果

本文基于无赋形剂共组装，开发了一种将 HCC 靶向的 IR820 和 DOX 结合在一起的新型纳米药物。首先，设计了乳糖化 IR820（LA-IR820）以靶向 HCC。然后，LA-IR820/DOX 纳米药物（LA-IR820/DOX ND）在没有赋形剂辅助的情况下完全自组装。评估了无赋形剂 LA-IR820/DOX ND 的理化性质和化学-光热抗肿瘤活性。更重要的是，所得到的 LA-IR820/DOX ND 具有 100%的载药量、显著的 HCC 靶向性和优异的抗肿瘤效果。

结论

这种无赋形剂的 LA-IR820/DOX ND 可能是一种很有前途的候选药物，可用于同步递药和协同靶向 IR820 和 DOX 作为联合化学-光热治疗。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/384d/7320228/60759e7a450f/IJN-15-4431-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/384d/7320228/4c8623638995/IJN-15-4431-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/384d/7320228/7766ef5e1216/IJN-15-4431-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/384d/7320228/140b040a41fd/IJN-15-4431-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/384d/7320228/f486736daf03/IJN-15-4431-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/384d/7320228/60759e7a450f/IJN-15-4431-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/384d/7320228/4c8623638995/IJN-15-4431-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/384d/7320228/7766ef5e1216/IJN-15-4431-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/384d/7320228/140b040a41fd/IJN-15-4431-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/384d/7320228/f486736daf03/IJN-15-4431-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/384d/7320228/60759e7a450f/IJN-15-4431-g0005.jpg

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