聚酰胺胺树枝状聚合物微凝胶：将树枝状聚合物分层排列成微米域，具有扩展的结构特征，用于可编程药物输送和释放,Macromolecules

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聚酰胺胺树枝状聚合物微凝胶：将树枝状聚合物分层排列成微米域，具有扩展的结构特征，用于可编程药物输送和释放
Macromolecules ( IF 5.1 ) Pub Date : 2018-08-03 00:00:00 , DOI: 10.1021/acs.macromol.8b01006
Juan Wang ₁ , Remy C Cooper ₂ , Hongliang He ₁ , Boxuan Li ₁ , Hu Yang _{1,

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Affiliation

我们报告了使用油包水（w/o）反相微乳液方法和高效的氮杂迈克尔加成法制备微米尺寸的树枝状聚合物水凝胶（μDHs）。将 EDA 核心聚酰胺胺 (PAMAM) 树枝状聚合物 G5 (10 wt%) 和聚乙二醇二丙烯酸酯 (PEG-DA, M _n = 575 g/mol)（胺/丙烯酸酯的摩尔比 = 1/1）溶解在在表面活性剂span 80/tween 80（5/1，w/w）存在下将水相加入到己烷中（己烷与表面活性剂的体积比：70:1）形成w/o微乳液，其中PAMAM G5交叉-通过氮杂迈克尔加成反应与 PEG-DA 连接。所得微凝胶的尺寸在 3-5 μm 范围内，且尺寸分布相对较窄。μDH 具有 pH 响应性可降解。它们表现出良好的细胞相容性并且在体内不会引起急性毒性。此外，它们可以实现疏水性药物CPT的高负载并以颗粒形式进入细胞。CPT和CPT/树枝状聚合物复合物可以按照零级释放动力学缓慢释放。总而言之，在微米域中具有分层有序树枝状大分子的μDH代表了一类新型微粒，其具有扩展的结构特征，可用于可编程药物输送和释放。

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Polyamidoamine Dendrimer Microgels: Hierarchical Arrangement of Dendrimers into Micrometer Domains with Expanded Structural Features for Programmable Drug Delivery and Release

We report on the fabrication of micrometer-sized dendrimer hydrogels (μDHs) using the water-in-oil (w/o) inverse microemulsion method coupled with the highly efficient aza-Michael addition. EDA core polyamidoamine (PAMAM) dendrimer G5 (10 wt %) and poly(ethylene glycol) diacrylate (PEG-DA, M_n = 575 g/mol) (the molar ratio of amine/acrylate = 1/1) were dissolved in the water phase and added to hexane in the presence of surfactants span 80/tween 80 (5/1, w/w) (volume ratio of hexane to surfactants: 70:1) to form w/o microemulsions, in which PAMAM G5 cross-links with PEG-DA via the aza-Michael addition reaction. The resulting microgels are within 3–5 μm with relatively narrow size distribution. μDHs are pH-responsive degradable. They show good cytocompatibility and do not cause acute toxicity in vivo. Furthermore, they can realize a high loading of the hydrophobic drug CPT and enter the cells in the form of particles. The CPT and CPT/dendrimer complex can be slowly released following the zero-order release kinetics. Taken together, μDHs possessing hierarchically ordered dendrimers in micrometer domains represent a new class of microparticles with expanded structural features for programmable drug delivery and release.

更新日期：2018-08-03

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