Hydrophobically Modified Keratin Vesicles for GSH-Responsive Intracellular Drug Release

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• 作者：Manuela Curcio ; Barbara Blanco-Fernandez ; Luis Diaz-Gomez ; Angel Concheiro ; Carmen Alvarez-Lorenzo
• 刊名：Bioconjugate Chemistry
• 出版年：2015
• 出版时间：September 16, 2015
• 年：2015
• 卷：26
• 期：9
• 页码：1900-1907
• 全文大小：388K
• ISSN：1520-4812

文摘

Redox-responsive polymersomes were prepared by self-assembly of a hydrophobically modified keratin and employing a water addition/solvent evaporation method. Polyethylene glycol-40 stearate (PEG₄₀ST) was chosen as hydrophobic block to be coupled to keratin via radical grafting. The amphiphilic polymer exhibited low critical aggregation concentration (CAC; 10 渭g/mL), indicating a good thermodynamic stability. The polymeric vesicles loaded both hydrophilic methotrexate and hydrophobic curcumin with high entrapment efficiencies, and showed a GSH-dependent drug release rate. Confocal studies on HeLa cells revealed that the obtained polymersomes were efficiently internalized. Biocompatibility properties of the proposed delivery vehicle were assessed in HET-CAM test and Balb-3T3 mouse fibroblasts. Polymersomes loaded with either methotrexate or curcumin inhibited HeLa and CHO-K1 cancer cells proliferation. Overall, the proposed keratin polymersomes could be efficient nanocarriers for chemotherapeutic agents.