Biodegradable Hyperbranched Polyglycerol with Ester Linkages for Drug Delivery

Biodegradable hyperbranched polyglycerols (dHPGs) were synthesized through oxyanionic initiating hybrid polymerization of glycerol and glycidyl methacrylate. Due to the introduction of ester linkages into the hyperbranched polyglycerol backbone, dHPGs showed good biodegradability and low cytotoxicit...

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Veröffentlicht in:Biomacromolecules 2012-11, Vol.13 (11), p.3552-3561
Hauptverfasser: Hu, Mei, Chen, Mingsheng, Li, Guolin, Pang, Yan, Wang, Dali, Wu, Jieli, Qiu, Feng, Zhu, Xinyuan, Sun, Jian
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container_end_page 3561
container_issue 11
container_start_page 3552
container_title Biomacromolecules
container_volume 13
creator Hu, Mei
Chen, Mingsheng
Li, Guolin
Pang, Yan
Wang, Dali
Wu, Jieli
Qiu, Feng
Zhu, Xinyuan
Sun, Jian
description Biodegradable hyperbranched polyglycerols (dHPGs) were synthesized through oxyanionic initiating hybrid polymerization of glycerol and glycidyl methacrylate. Due to the introduction of ester linkages into the hyperbranched polyglycerol backbone, dHPGs showed good biodegradability and low cytotoxicity. Benefiting from the existence of terminal hydroxyls and methacryloyl groups, both the anticancer drug methotrexate (MTX) and fluorescent probe Rhodamine-123 could be conjugated onto the surface of dHPGs easily. The resultant MTX-conjugated polymers (dHPG-MTXs) exhibited an amphiphilic character, resulting in the formation of micelles in an aqueous solution. The release of MTX from micelles was significantly faster at mildly acidic pH of 5.0 compared to physiological pH of 7.4. dHPG-MTX micelles could be efficiently internalized by cancer cells. MTT assay against cancer cells showed dHPG-MTXs micelles had high anticancer efficacy. On the basis of their good biodegradability and low cytotoxicity, dHPGs provide an opportunity to design excellent drug delivery systems.
doi_str_mv 10.1021/bm300966d
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Due to the introduction of ester linkages into the hyperbranched polyglycerol backbone, dHPGs showed good biodegradability and low cytotoxicity. Benefiting from the existence of terminal hydroxyls and methacryloyl groups, both the anticancer drug methotrexate (MTX) and fluorescent probe Rhodamine-123 could be conjugated onto the surface of dHPGs easily. The resultant MTX-conjugated polymers (dHPG-MTXs) exhibited an amphiphilic character, resulting in the formation of micelles in an aqueous solution. The release of MTX from micelles was significantly faster at mildly acidic pH of 5.0 compared to physiological pH of 7.4. dHPG-MTX micelles could be efficiently internalized by cancer cells. MTT assay against cancer cells showed dHPG-MTXs micelles had high anticancer efficacy. On the basis of their good biodegradability and low cytotoxicity, dHPGs provide an opportunity to design excellent drug delivery systems.</abstract><cop>Washington, DC</cop><pub>American Chemical Society</pub><pmid>22998016</pmid><doi>10.1021/bm300966d</doi><tpages>10</tpages></addata></record>
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subjects 3T3 Cells
Animals
Applied sciences
Biological and medical sciences
Biological Transport
Cell Line, Tumor
Cell Proliferation - drug effects
Drug Carriers - chemistry
Exact sciences and technology
General pharmacology
Glycerol - chemical synthesis
Glycerol - chemistry
Glycerol - metabolism
HeLa Cells
Humans
Medical sciences
Methotrexate - administration & dosage
Methotrexate - chemistry
Methotrexate - pharmacology
Mice
Micelles
Organic polymers
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Physicochemistry of polymers
Polymers - chemical synthesis
Polymers - chemistry
Polymers - metabolism
Polymers with particular properties
Preparation, kinetics, thermodynamics, mechanism and catalysts
Rhodamine 123 - administration & dosage
Rhodamine 123 - chemistry
Rhodamine 123 - pharmacology
title Biodegradable Hyperbranched Polyglycerol with Ester Linkages for Drug Delivery
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