Poly(ethylene glycol)-b-poly(lysine) copolymer bearing nitroaromatics for hypoxia-sensitive drug delivery

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• 作者：Thavasyappan Thambi^a ; Soyoung Son^b ; Doo Sung Lee^a ; Jae Hyung Park^a ; ^b ; ^{jhpark1@skku.edu" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Hypoxia ; DOX ; Drug delivery ; Block copolymer ; Cancer
• 刊名：Acta Biomaterialia
• 出版年：2016
• 出版时间：1 January 2016
• 年：2016
• 卷：29
• 期：Complete
• 页码：261-270
• 全文大小：1387 K

文摘

Hypoxia occurs in a variety of pathological conditions including stroke, rheumatoid arthritis, atherosclerosis, and tumors. In this study, an amphiphilic block copolymer, composed of poly(ethylene glycol) as the hydrophilic block and poly(ε-(4-nitro)benzyloxycarbonyl-l-lysine) as the hydrophobic block, was prepared for hypoxia-sensitive drug delivery. Owing to its amphiphilic nature, the block copolymer formed micelles and encapsulated doxorubicin (DOX) in an aqueous condition. The DOX-loaded micelles exhibited rapid intracellular release of DOX under the hypoxic condition, implying high potential as a drug carrier for cancer therapy.

Statement of significance

Hypoxia occurs in a variety of pathological conditions including stroke, rheumatoid arthritis, atherosclerosis, and tumors. In this study, we developed a novel type of hypoxia-sensitive polymeric micelles (HS-PMs) that can specifically release the drug under the hypoxic conditions. HS-PMs were prepared using poly(ethylene glycol) as the hydrophilic block and poly(ε-(4-nitro)benzyloxycarbonyl-l-lysine) as the hydrophobic block. Owing to its amphiphilic nature, the block copolymer formed micelles and encapsulated doxorubicin (DOX) in an aqueous condition. The DOX-loaded micelles exhibited rapid intracellular release of DOX under the hypoxic condition. Overall, it is evident that the HS-PMs prepared in this study have the potential to effectively deliver hydrophobic drugs into the hypoxic cells involved in various intractable diseases.