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A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles
Published on: December 23, 2016
Novel pH-sensitive micelles generated by star-shape copolymers containing zwitterionic sulfobetaine for efficient
Jun Cao1, Shuying Zhai, Chenlong Li
1College of Polymer Science and Engineering of Sichuan University, Sichuan University, Chengdu 610065, China.
Journal of Biomedical Nanotechnology
|September 25, 2013
Summary
Novel pH-sensitive star-shaped copolymers form micelles for targeted cancer drug delivery. These micelles efficiently deliver doxorubicin into Hela cells, showing promise for anti-cancer therapies.
Area of Science:
- Biomaterials Science
- Polymer Chemistry
- Nanotechnology
Background:
- pH-sensitive micelles are promising for tumor-targeted drug delivery.
- Traditional hydrophilic blocks like polyethylene glycol (PEG) are often replaced in novel drug carrier designs.
Purpose of the Study:
- To design and synthesize novel pH-sensitive star-shaped copolymers for drug delivery.
- To evaluate the potential of these copolymers as carriers for anti-cancer drugs, specifically doxorubicin.
Main Methods:
- Synthesis of amphiphilic star-shaped copolymers (4sPCLDEAS) using ring-opening polymerization (ROP) and atom transfer radical polymerization (ATRP).
- Characterization of copolymer structure using proton nuclear magnetic resonance (1HNMR).
- Formation and characterization of polymeric micelles, including critical micelle concentration (CMC), size distribution, and pH responsiveness. Encapsulation and in vitro release studies of doxorubicin (DOX). Cytotoxicity and intracellular uptake studies in Hela cells.
Main Results:
- Successfully synthesized novel pH-sensitive star-shaped copolymers (4sPCLDEAS) with a unique hydrophilic segment.
- Formed spherical polymeric micelles with narrow size distribution and low CMC (1 x 10(-3) mg mL(-1)).
- Achieved efficient doxorubicin (DOX) encapsulation with pH-dependent drug release. The DOX-loaded micelles demonstrated good biocompatibility and superior intracellular delivery compared to hydrophilic DOX x HCl in Hela cells.
Conclusions:
- The synthesized pH-sensitive star-shaped copolymers effectively form micelles suitable for drug delivery.
- These micelles show potential as efficient and non-toxic carriers for targeted anti-cancer drug delivery, particularly doxorubicin.
- The replacement of PEG with a novel hydrophilic segment offers a promising alternative for developing advanced drug delivery systems.
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