Synthesis of Poly(ethylene glycol) Block Copolymers as Potential Water-Soluble Drug Carriers

1995 ◽  
Vol 60 (10) ◽  
pp. 1765-1780 ◽  
Author(s):  
Michal Pechar ◽  
Jiří Strohalm ◽  
Karel Ulbrich

The synthesis of a model water-soluble drug carrier based on poly(ethylene glycol) (PEG) block copolymers is described. In the copolymers, two blocks of PEG are linked by a biodegradable oligopeptide or amino acid linkage containing the glutamic acid residue. 4-Nitroaniline as a drug model is attached to the γ-carboxyl group of glutamic acid of the polymer carrier via an enzymatically degradable oligopeptide spacer. The oligopeptides used were potential substrates for chymotrypsin. The relationship between the structure of oligopeptides linking two PEG blocks and the rate of chymotrypsin-catalyzed polymer chain degradation as well as the relationship between the structure of the spacer and kinetics of drug model release from the carrier after incubation in chymotrypsin solution is discussed in detail. The results showed that by modifying the structure of oligopeptides in the polymer construct, changes in the rates of both polymer degradation and the drug model release can be achieved in a very broad range.

RSC Advances ◽  
2014 ◽  
Vol 4 (78) ◽  
pp. 41588-41596 ◽  
Author(s):  
Lixin Yang ◽  
Xiuli Hu ◽  
Weiqi Wang ◽  
Shi Liu ◽  
Tingting Sun ◽  
...  

The nano polymer drugs based on Y-shaped block copolymer mPEG2-PGA show a great potential on the treatment for solid tumors.


2010 ◽  
pp. n/a-n/a ◽  
Author(s):  
Helene Nouailhas ◽  
Feng Li ◽  
Abdelsalm El Ghzaoui ◽  
Suming Li ◽  
Jean Coudane

2020 ◽  
Vol 324 ◽  
pp. 228-237 ◽  
Author(s):  
Katia Maso ◽  
Antonella Grigoletto ◽  
Lucia Raccagni ◽  
Marino Bellini ◽  
Ilaria Marigo ◽  
...  

2008 ◽  
Vol 8 (5) ◽  
pp. 2362-2368 ◽  
Author(s):  
Ming-Fa Hsieh ◽  
Nguyen Van Cuong ◽  
Chao-Hsuan Chen ◽  
Yung Tsung Chen ◽  
Jui-Ming Yeh

The amphiphilic block copolymers methoxy poly(ethylene glycol)-poly(ε-caprolactone) was grafted to 2-hydroxyethyl cellulose to produce the water-soluble copolymers. Doxorubicin loaded nanoparticles were prepared by dialysis method and the sizes of nanoparticles were determined by dynamic light scattering in solution and atomic force microscopes. As results the sizes were detected in a range of 197.4 to 340.7 nm. The in-vitro release of Dox was studied in phosphate and acetate buffered solution at 37 °C. The results showed that 43 and 53% of Dox remained after an incubation period of 7 days. The cytotoxicity of Dox loaded micelles was investigated in two different human MCF-7/wild type and MCF-7/Adriamycin drug resistant cells lines. The Dox-loaded micelles showed reduced cytotoxicity compared to free Dox in MCF-7/wild type and MCF-7/Adriamycin drug resistant cells.


Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 230 ◽  
Author(s):  
Xingzheng Liu ◽  
Rongrong Fan ◽  
Boting Lu ◽  
Yuan Le

Methoxy-poly(ethylene glycol)-poly(l-glutamic acid)-poly(l-phenylalanine) triblock polymers with different architecture were synthesized as drug carrier to obtain sustained and controlled release by tuning the composition. These triblock polymers were prepared by ring opening polymerization and poly(ethylene glycol) was used as an initiator. Polymerization was confirmed by 1H NMR, FT-IR and gel penetration chromatography. The polymers can self-assemble to form micelles in aqueous medium and their critical micelle concentrations values were examined. The micelles were spherical shape with size of 50–100 nm and especially can arranged in a regular manner. Sorafenib was selected as the model drug and the drug loading performance was dependent on the composition of the block copolymer. In vitro drug release indicated that the polymers can realize controlled and sustained drug release. Furthermore, in vitro cytotoxicity assay showed that the polymers were biocompatible and the drug-loaded micelles can increase toxicity towards tumor cells. Confocal fluorescence microscopy assays illustrated that the micelles can be uptaken quickly and release drug persistently to inhibit tumor cell growth.


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