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Biodegradable poly(terephthalate-co-phosphate)s: synthesis, characterization and drug-release properties
Hai-Quan Mao1, Irina Shipanova-Kadiyala, Zhong Zhao
1Department of Biomedical Engineering, Johns Hopkins University School of Medicine, 726 Ross Building, 720 Rutland Avenue, Baltimore, MD 21205, USA.
Journal of Biomaterials Science. Polymer Edition
|March 30, 2005
Summary
Researchers developed new biodegradable poly(terephthalate-co-phosphate)s with tunable properties for biomedical uses. These phosphate-containing polymers offer improved solubility, degradability, and biocompatibility, showing promise for drug delivery applications.
Area of Science:
- Polymer Chemistry
- Biomaterials Science
- Materials Engineering
Background:
- Development of biodegradable polymers with tailored physicochemical and biological properties is crucial for advanced biomedical applications.
- Existing polymers often lack the desired balance of degradability, mechanical strength, and biocompatibility.
- Poly(ethylene terephthalate) (PET) is a widely used polymer but lacks biodegradability and favorable drug release characteristics.
Purpose of the Study:
- To synthesize and characterize a novel series of biodegradable poly(terephthalate-co-phosphate)s.
- To investigate the influence of phosphate incorporation on polymer properties, including solubility, degradability, thermal characteristics, and mechanical performance.
- To evaluate the in vitro and in vivo biocompatibility and degradation behavior, as well as drug release profiles for potential biomedical applications.
Main Methods:
- Two-step poly-condensation synthesis involving 1,4-bis(2-hydroxyethyl) terephthalate, ethylphosphorodichloridate (EOP), and terephthaloyl chloride (TC).
- Characterization of physicochemical properties: solubility, glass transition temperature (Tg), crystallinity, hydrophilicity, mechanical testing (elongation, elastic modulus).
- In vitro and in vivo degradation studies, cytotoxicity assays, tissue biocompatibility assessment, and drug release studies (FITC-BSA, cyclosporine-A).
Main Results:
- Incorporation of phosphate into the PET backbone yielded soluble, biodegradable co-polymers with reduced Tg, lower crystallinity, and increased hydrophilicity.
- A specific co-polymer (80:20 EOP/TC ratio) demonstrated excellent film-forming properties, favorable in vitro toxicity, and good in vivo muscle tissue biocompatibility.
- Co-polymers exhibited controlled degradation rates (21% mass loss in vitro in 21 days, 20% in vivo in 4 months) and tunable drug release kinetics for both hydrophilic and hydrophobic drugs.
Conclusions:
- The synthesized poly(terephthalate-co-phosphate)s offer a versatile platform for designing biodegradable biomaterials with tunable properties.
- Structure-property relationships were established, showing increased hydrolytic lability with higher phosphate content and specific side chain modifications.
- These co-polymers hold significant potential for various biomedical applications, including drug delivery systems and tissue engineering scaffolds.