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载雷帕霉素修饰表阿霉素和地奥心血康的共载脂质体通过限制营养供应抑制非小细胞肺癌生长。

RPV-modified epirubicin and dioscin co-delivery liposomes suppress non-small cell lung cancer growth by limiting nutrition supply.

机构信息

School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian, China.

Department of Pharmaceutical Engineering, Beijing Institute of Petrochemical Technology, Beijing, China.

出版信息

Cancer Sci. 2020 Feb;111(2):621-636. doi: 10.1111/cas.14256. Epub 2020 Jan 18.

DOI:10.1111/cas.14256
PMID:31777993
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7004549/
Abstract

Chemotherapy for non-small cell lung cancer (NSCLC) is far from satisfactory, mainly due to poor targeting of antitumor drugs and self-adaptations of the tumors. Angiogenesis, vasculogenic mimicry (VM) channels, migration, and invasion are the main ways for tumors to obtain nutrition. Herein, RPV-modified epirubicin and dioscin co-delivery liposomes were successfully prepared. These liposomes showed ideal physicochemical properties, enhanced tumor targeting and accumulation in tumor sites, and inhibited VM channel formation, tumor angiogenesis, migration and invasion. The liposomes also downregulated VM-related and angiogenesis-related proteins in vitro. Furthermore, when tested in vivo, the targeted co-delivery liposomes increased selective accumulation of drugs in tumor sites and showed extended stability in blood circulation. In conclusion, RPV-modified epirubicin and dioscin co-delivery liposomes showed strong antitumor efficacy in vivo and could thus be considered a promising strategy for NSCLC treatment.

摘要

非小细胞肺癌 (NSCLC) 的化疗效果远不理想，主要是由于抗肿瘤药物靶向性差和肿瘤的自我适应。血管生成、血管生成拟态 (VM) 通道、迁移和侵袭是肿瘤获取营养的主要途径。在此，成功制备了 RPV 修饰的表阿霉素和薯蓣皂素共载脂质体。这些脂质体表现出理想的物理化学性质，增强了肿瘤靶向性和在肿瘤部位的积累，并抑制了 VM 通道形成、肿瘤血管生成、迁移和侵袭。脂质体还在体外下调了 VM 相关和血管生成相关蛋白。此外，在体内进行测试时，靶向共载脂质体增加了药物在肿瘤部位的选择性积累，并在血液循环中表现出延长的稳定性。总之，RPV 修饰的表阿霉素和薯蓣皂素共载脂质体在体内表现出很强的抗肿瘤功效，因此可以被认为是治疗 NSCLC 的一种有前途的策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/379a/7004549/6b856cf2d623/CAS-111-621-g009.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/379a/7004549/cc29aeb6a006/CAS-111-621-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/379a/7004549/7250dfa03bf9/CAS-111-621-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/379a/7004549/6b856cf2d623/CAS-111-621-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/379a/7004549/4eab47f68dd3/CAS-111-621-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/379a/7004549/e3966e0ea9cf/CAS-111-621-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/379a/7004549/a3b809e47e08/CAS-111-621-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/379a/7004549/2f0b8710af1b/CAS-111-621-g006.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/379a/7004549/6b856cf2d623/CAS-111-621-g009.jpg

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