scholarly journals Active targeting co-delivery system based on pH-sensitive methoxy-poly(ethylene glycol)2K-poly(ε-caprolactone)4K-poly(glutamic acid)1K for enhanced cancer therapy

2016 ◽  
Vol 472 ◽  
pp. 90-98 ◽  
Author(s):  
Nuannuan Li ◽  
Chunzhi Huang ◽  
Yuxia Luan ◽  
Aixin Song ◽  
Yunmei Song ◽  
...  
2018 ◽  
Vol 33 (2) ◽  
pp. 119-133 ◽  
Author(s):  
Jing Xu ◽  
Benkai Qin ◽  
Shujuan Luan ◽  
Peilan Qi ◽  
Yingying Wang ◽  
...  

Biodegradable pH-sensitive amphiphilic block polymer (mPEG-Hyde-PLGA) was synthesized via ring-opening polymerization, initiated from a hydrazone-containing macro-initiator. In this way, a pH-sensitive hydrazone bond was inserted into the backbone of block copolymer, linking hydrophilic poly(ethylene glycol) segment and hydrophobic poly(lactic-co-glycolic acid) segment. The copolymer self-assembled to form stable micelles with mean diameters below 100 nm and served as a drug delivery system for doxorubicin, with drug loading content of 5.3%. pH sensitivity of the hydrazone-containing micelles was investigated by changes in diameter and size distribution observed by dynamic light scattering measurements when the micelles were encountered to acidic medium. Small pieces and larger aggregates were found by transmission electron microscopy resulting from the disassociation of the micelles in acidic conditions. It was also noted that doxorubicin release from the pH-sensitive micelles is significantly faster at pH 4.0 and pH 5.0 compared to pH 7.4, while almost no difference was detected in the case of pH non-sensitive micelles. MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assays on HepG-2 and MCF-7 cells revealed that doxorubicin-loaded pH-sensitive micelles had higher antitumor activity than pH-insensitive ones. This pH-sensitive drug delivery system based on hydrazone-containing block copolymer has been proved as a promising drug formulation for cancer therapy.


2013 ◽  
Vol 3 (2) ◽  
pp. 261-272 ◽  
Author(s):  
Chun-Yang Sun ◽  
Shuang Dou ◽  
Jin-Zhi Du ◽  
Xian-Zhu Yang ◽  
Ya-Ping Li ◽  
...  

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