pH-responsive polymeric micelles of poly(ethylene glycol)-b-poly(alkyl(meth)acrylate-co-methacrylic acid): Influence of the copolymer composition on self-assembling properties and release of candesartan cilexetil

2007 ◽  
Vol 65 (3) ◽  
pp. 379-387 ◽  
Author(s):  
Prashant Satturwar ◽  
Mohamad Nasser Eddine ◽  
François Ravenelle ◽  
Jean-Christophe Leroux
2012 ◽  
Vol 77 ◽  
pp. 333-342 ◽  
Author(s):  
Hong Yun Tai ◽  
Craig L. Duvall ◽  
Patrick S. Stayton ◽  
Alan S. Hoffman ◽  
Wen Xin Wang

pH-Responsive polymers have attracted much attention for biotechnology applications as carriers or matrix to facilitate intracellular or extracellular therapeutic drug delivery and release. In this paper, we report the development of new pH-responsive and hyperbranched copolymers with potential for such applications. These pH-responsive hyperbranched copolymers were synthesized via one pot reversible addition-fragmentation chain transfer (RAFT) copolymerization of propylacrylic acid (PAA) and a branching co-monomer poly(ethylene glycol diacrylate) (PEGDA) (Mn=258 Da) at the monomer feed molar ratios [PAA]0/[PEGDA]0 = 99/1, 90/10 and 80/20. The resultant poly(PAA-PEGDA) copolymers were characterized by Proton Nuclear Magnetic Resonance (1H NMR) and Gel Permeation Chromatography (GPC) to obtain the molecular weight, copolymer composition and degree of acrylate functionality. The hydrodynamic dimensions of these copolymers at pH range between 5.0 and 7.4 were studied using Dynamic Light Scattering technique (DLS). Moreover, these hyperbranched copolymers demonstrated composition- and size-dependent membrane disruptive properties by red blood cell hemolysis assay. Poly(PAA-PEGDA) with the copolymer composition [PAA]/[PEGDA]= 68/32, obtained from the copolymerization at the monomer feed molar ratio [PAA]0/[PEGDA]0 = 99/1, demonstrated significant membrane disruptive activity.


2019 ◽  
Vol 7 (2) ◽  
pp. 334-345 ◽  
Author(s):  
Zhaoyuan Guo ◽  
Ke Zhao ◽  
Rong Liu ◽  
Xiaolan Guo ◽  
Bin He ◽  
...  

pH-responsive stereocomplexed micelles based on poly(l-lactic acid)-b-polylysine/poly(d-lactic acid)-b-methoxy poly(ethylene glycol) (PLLA-b-PLys/PDLA-b-mPEG) were fabricated by stereocomplexation between enantiomeric PLA segments.


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.


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