A pH-Sensitive Hydrogel with Hydrophobic Association for Controlled Release of Poorly Water-Soluble Drugs

A pH-Sensitive Hydrogel with Hydrophobic Association for Controlled Release of Poorly Water-Soluble Drugs
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一种具有疏水缔合的 pH 敏感水凝胶,用于控制释放水溶性差的药物

DOI:
10.1080/10601320903004707
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发表时间:
2009-06
影响因子:
2.5
通讯作者:
Yang, Zhiwen
Yang, Zhiwen
中科院分区:
化学4区
文献类型:
--
作者:
Tong, Zhen;Ma, Jing;Liu, Xinxing;Yang, Zhiwen

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通过丙烯酸(AA)和两亲性大分子单体聚乙二醇单月桂基醚单丙烯酸酯(PEGLA)与交联剂乙二醇二甲基丙烯酸酯的紫外线诱导自由基聚合,开发了一种新型pH敏感水凝胶,用于控制释放水溶性较差的模型药物阿昔洛韦。在 I = 0.1 M 的不同 pH 缓冲液以及乙醇/水混合物中研究了溶胀行为。研究发现,PEGLA 中烃链形成的疏水缔合主导着水凝胶的溶胀特性,由于 AA 链段的电离,其 pH 敏感性较低。因此,随着水凝胶中PEGLA含量的增加,阿昔洛韦的载药量得到改善,阿昔洛韦的释放速率减慢。通过Weibull方程拟合释放数据,当水凝胶中PEGLA含量超过20 mol%时,阿昔洛韦释放动力学从Fickian扩散变为反常扩散。
A novel pH-sensitive hydrogel has been developed by UV induced radical polymerization of acrylic acid (AA) and amphiphilic macromonomer polyethylene glycol monolaurylether monoacrylate (PEGLA) with crosslinker ethylene glycol dimethacrylate for controlled release of acyclovir, a poor water-soluble model drug. The swelling behavior was investigated in the buffer of different pH at I = 0.1 M, as well as in the ethanol/water mixture. The hydrophobic association formed by the hydrocarbon chains in PEGLA was found to dominate the swelling properties of the hydrogels with subordinate pH sensitivity due to the ionization of the AA segments. Therefore, the drug loading of acyclovir has been improved and the release rate of acyclovir was slowed down with increasing the PEGLA content in the hydrogels. By fitting the release data with Weibull equation, the acyclovir release kinetics was changed from the Fickian diffusion to an anomalous diffusion when the PEGLA content in the hydrogels was beyond 20 mol%.
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