Synthesis and cytotoxicity of brefeldin A conjugated monomethoxy-poly(ethylene glycol)-b-poly(L-lactide) polymeric micelles

2012 ◽  
Vol 24 (8) ◽  
pp. 986-998 ◽  
Author(s):  
Wanyun Liu ◽  
Junchao Wei ◽  
Ping Huo ◽  
Yunhua Lu ◽  
Yiwang Chen ◽  
...  
2019 ◽  
Vol 14 (3) ◽  
pp. 280-291 ◽  
Author(s):  
Jaleh Varshosaz ◽  
Farshid Hassanzadeh ◽  
Batool Hashemi-Beni ◽  
Mohsen Minaiyan ◽  
Saeedeh Enteshari

Background: Due to the low water solubility of Docetaxel (DTX), it is formulated with ethanol and Tween 80 with lots of side effects. For this reason, special attention has been paid to formulate it in new drug nano-carriers. Objective: The goal of this study was to evaluate the safety, antitumor activity and tissue distribution of the novel synthesized Raloxifene (RA) targeted polymeric micelles. Methods: DTX-loaded RA-targeted polymeric micelles composed of poly(styrene-maleic acid)- poly(amide-ether-ester-imide)-poly(ethylene glycol) (SMA-PAEE-PEG) were prepared and their antitumor activity was studied in MC4-L2 tumor-bearing mice compared with non-targeted micelles and free DTX. Safety of the micelles was studied by Hematoxylin and Eosin (H&E) staining of tumors and major organs of the mice. The drug accumulation in the tumor and major organs was measured by HPLC method. Results: The results showed better tumor growth inhibition and increased survival of mice treated with DTX-loaded in targeted micelles compared to the non-targeted micelles and free DTX. Histopathological studies, H&E staining of tumors and immunohistochemical examination showed the potential of DTX-loaded RA-targeted micelles to inhibit tumor cells proliferation. The higher accumulation of the DTX in the tumor tissue after injection of the micelles compared to the free DTX may indicate the higher uptake of the targeted micelles by the G-Protein-Coupled Estrogen Receptors (GPER). Conclusion: The results indicate that RA-conjugated polymeric micelles may be a strong and effective drug delivery system for DTX therapy and uptake of the drug into tumor cells, and overcome the disadvantages and side effects of conventional DTX.


2011 ◽  
Vol 65 (4) ◽  
Author(s):  
Guo-Quan Zhu ◽  
Qiao-Chun Gao ◽  
Fa-Gang Wang ◽  
Guo-Chang Li ◽  
Ping Wang

AbstractPoly(ethylene glycol)-block-poly(γ-benzyl l-glutamate)-graft-poly(ethylene glycol) (PEG-b-PBLG-g-PEG) copolymer was synthesised by the ester exchange reaction of PEG-block-PBLG copolymer with mPEG. The self-association behaviour of PEG-b-PBLG-g-PEG in mixtures of ethanol, chloroform, and trifluoroacetic acid as denaturing acid was investigated by transmission electron microscopy, nuclear magnetic resonance spectroscopy, FT-IR spectroscopy, dynamic light scattering, and viscometry. It was revealed that the increase in denaturing acid content in the mixed system not only promoted the critical micelle concentration but also changed the morphology of the polymeric micelles from elliptical to spherical.


2010 ◽  
Vol 64 (5) ◽  
Author(s):  
Guo-Quan Zhu ◽  
Fa-Gang Wang ◽  
Yu-Ying Liu ◽  
Qiao-Chun Gao

AbstractPoly(γ-benzyl l-glutamate)-graft-poly(ethylene glycol) (PBLG-graft-PEG) copolymer was synthesized by the ester exchange reaction of PBLG homopolymer with mPEG. Aggregation behavior of the PBLG-graft-PEG copolymer in mixtures of ethanol and chloroform was investigated by transmission electron microscopy (TEM), dynamic light scattering (DLS), and viscometry. Effects of the polymer solution concentration, grafting degree, test temperature, and chloroform content on the morphology, average particle diameter, and critical micelle concentration (CMC) of the micelles formed by the PBLG-graft-PEG copolymer in the mixed solvents were mainly studied. It was revealed that the PBLG-graft-PEG copolymer can self-assemble into polymeric micelles with a core-shell structure in various shapes depending on the preparation conditions.


RSC Advances ◽  
2016 ◽  
Vol 6 (63) ◽  
pp. 58160-58172 ◽  
Author(s):  
Y. Chen ◽  
Y. X. Zhang ◽  
Z. F. Wu ◽  
X. Y. Peng ◽  
T. Su ◽  
...  

The self-assembly and drug release of the three PEG–PCL copolymers with different topologies but identical molar ratio between PEG to PCL.


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