Amphiphilic Interpenetrating Networks for the Delivery of Hydrophobic, Low Molecular Weight Therapeutic Agents.
Amphiphilic Interpenetrating Networks for the Delivery of Hydrophobic, Low Molecular Weight Therapeutic Agents.
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DOI：
10.1021/ie201593h
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发表时间：
2011-11-16
影响因子：
4.2
通讯作者：
Peppas, Nicholas A.
中科院分区：
文献类型：
--
作者：
Schoener, Cody A.;Hutson, Heather N.;Fletcher, Grace K.;Peppas, Nicholas A.
为了研究疏水性治疗剂的递送，合成了一类新型的互穿网络（IPN），其由两个网络组成：甲基丙烯酸接枝聚（乙二醇）系链，P（MAA-g-EG）和聚（丙烯酸正丁酯）（PBA）。亲水性P（MAA-g-EG）网络是pH响应性水凝胶，当包封的治疗剂（例如低分子量药物或蛋白质）从胃（低pH）传递到小肠上部（中性pH）时，其能够触发释放包封的治疗剂。PBA是一种疏水性均聚物，其可以影响IPN溶胀行为、IPN中的治疗剂负载效率和来自IPN的溶质释放曲线。在动态溶胀条件下，IPN的溶胀率大于P（MAA-g-EG），而在平衡溶胀条件下，IPN的溶胀率随PBA含量的增加而降低。模型治疗剂荧光素的负载效率范围为21 - 44%。从纯P（MAA-g-EG）和随后的IPN的释放研究表明，从低pH（2.0）到中性pH（7.0）的转变触发荧光素释放。最大荧光素释放取决于在这些研究中使用的载体的结构和亲水性。
To investigate the delivery of hydrophobic therapeutic agents, a novel class of interpenetrating networks (IPNs) were synthesized and composed of two networks: methacrylic acid grafted with poly(ethylene glycol) tethers, P(MAA-g-EG), and poly(n-butyl acrylate) (PBA). The hydrophilic P(MAA-g-EG) networks are pH-responsive hydrogels capable of triggered release of an encapsulated therapeutic agent, such as a low molecular weight drug or a protein, when it passes from the stomach (low pH) to upper small intestine (neutral pH). PBA is a hydrophobic homopolymer that can affect the IPN swelling behavior, the therapeutic agent loading efficiencies in IPNs, and solute release profiles from IPNs. In dynamic swelling conditions, IPNs had greater swelling ratios than P(MAA-g-EG), but in equilibrium swelling conditions the IPN swelling ratio decreased with increasing PBA content. Loading efficiencies of the model therapeutic agent fluorescein ranged from 21 – 44%. Release studies from neat P(MAA-g-EG) and the ensuing IPNs indicated that the transition from low pH (2.0) to neutral pH (7.0) triggered fluorescein release. Maximum fluorescein release depended on the structure and hydrophilicity of the carriers used in these studies.
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