in vivo antitumor activity
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2022 ◽  
Vol 1249 ◽  
pp. 131556
Surendra Gulla ◽  
Vajra C. Reddy ◽  
Prasanna Babu Araveti ◽  
Dakshayani Lomada ◽  
Anand Srivastava ◽  

Small ◽  
2021 ◽  
pp. 2104034
Jiao Yang Lu ◽  
Wei Tao Huang ◽  
Kexuan Zhou ◽  
Xiaoli Zhao ◽  
Shuqing Yang ◽  

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1464
Yang Yang ◽  
Fuwei Yang ◽  
Xiaotian Shan ◽  
Jiamin Xu ◽  
Wenjie Fang ◽  

At present, the drug is still difficult to release completely and quickly only with single stimulation. In order to promote the rapid release of polymeric micelles at tumor site, pH/reduction sensitive polymers (PCT) containing disulfide bonds and orthoester groups were synthesized. The PCT polymers can self-assemble in water and entrap doxorubicin to form drug-loaded micelles (DOX/PCT). In an in vitro drug release experiment, the cumulative release of DOX/PCT micelles in the simulated tumor microenvironment (pH 5.0 with GSH) reached (89.7 ± 11.7)% at 72 h, while it was only (16.7 ± 6.1)% in the normal physiological environment (pH 7.4 without GSH). In addition, pH sensitive DOX loaded micellar system (DOX/PAT) was prepared as a control. Furthermore, compared with DOX/PAT micelles, DOX/PCT micelles showed the stronger cytotoxicity against tumor cells to achieve an effective antitumor effect. After being internalized by clathrin/caveolin-mediated endocytosis and macropinocytosis, DOX/PCT micelles were depolymerized in intercellular acidic and a reductive environment to release DOX rapidly to kill tumor cells. Additionally, DOX/PCT micelles had a better inhibitory effect on tumor growth than DOX/PAT micelles in in vivo antitumor activity studies. Therefore, pH/reduction dual sensitive PCT polymers have great potential to be used as repaid release nanocarriers for intercellular delivery of antitumor drugs.

2021 ◽  
Vol 266 ◽  
pp. 118132
Xingchen Zhai ◽  
Chaonan Li ◽  
Difeng Ren ◽  
Jing Wang ◽  
Chao Ma ◽  

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