Facile Synthesis of Polyester Dendrimers as Drug Delivery Carriers

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• 作者：Xinpeng Ma ; Zhuxian Zhou ; Erlei Jin ; Qihang Sun ; Bo Zhang ; Jianbin Tang ; Youqing Shen
• 刊名：Macromolecules
• 出版年：2013
• 出版时间：January 8, 2013
• 年：2013
• 卷：46
• 期：1
• 页码：37-42
• 全文大小：339K
• 年卷期：v.46,no.1(January 8, 2013)
• ISSN：1520-5835

文摘

Aliphatic polyester dendrimers are attractive carriers for in vivo delivery of bioactive molecules due to their biocompatibility and biodegradability, but efficient precision synthesis of these dendrimers without tedious purifications remains challenging. Herein, we report an efficient synthesis approach to polyester dendrimers from two AB₂-type monomers via combining a click reaction of thiol/acrylate Michael addition with esterification. The reaction solution of each generation contains only the targeted dendrimer macromolecules; thus, the only required separation is simple precipitation. The resulting hydroxyl-terminated fifth-generation dendrimer is thermoresponsive with a LCST of 41 掳C. The dendrimer could be further pegylated to obtain a water-soluble biocompatible dendrimer capable of encapsulation and controlled release of a hydrophobic anticancer drug, doxorubicin.