Thermosensitive properties of poly(amidoamine) dendrimers with peripheral phenylalanine residues
Thermosensitive properties of poly(amidoamine) dendrimers with peripheral phenylalanine residues
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DOI：
10.1021/la060066t
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发表时间：
2006-05-23
期刊：
影响因子：
3.9
通讯作者：
Kono, Kenji
中科院分区：
文献类型：
--
作者：
Tono, Yohei;Kojima, Chie;Kono, Kenji
树枝状大分子是一种球状、结构清晰的独特聚合物。我们以前制备了聚酰胺胺(PAMAM)树枝状大分子，其每一链末端都含有苯丙氨酸(Phe)残基作为有效的基因载体。在本研究中，我们发现Phe衍生的PAMAM树状大分子的水溶性随温度的变化而变化。树枝状大分子在低温下可溶于水溶液，但在高于特定阈值时变得不溶于水，这被称为较低的临界溶液温度(LCST)。虽然Phe修饰的树枝状大分子的LCST随着树枝状大分子生成量的增加而降低，但这些树枝状大分子在生理条件下表现出20-30℃的LCST。此外，通过在树枝状大分子的链端引入与Phe残基不同比例的异亮氨酸(Ile)残基来控制树枝状大分子的LCST。众所周知，PAMAM树枝状大分子可以包裹各种药物分子。由于这些原因，温度敏感型树枝状大分子可能是有效的药物载体，具有可控的大小和温度响应特性。
Dendrimers are unique polymers with globular shapes and well-defined structures. We previously prepared poly(amidoamine) (PAMAM) dendrimers having phenylalanine (Phe) residues at every chain end of the dendrimer as efficient gene carriers. In this study, we found that Phe-derivatized PAMAM dendrimers change their water solubility depending on temperature. The dendrimers were soluble in aqueous solutions at low temperatures, but they became water-insoluble at temperatures above a specific threshold, which is termed the lower critical solution temperature (LCST). Although the LCST of Phe-modified dendrimers decreased with increasing dendrimer generation, these dendrimers exhibited an LCST of 20-30 degrees C under physiological conditions. In addition, the LCST of the dendrimers was controlled by introducing isoleucine (Ile) residues at chain ends of dendrimers at varying ratios with respect to Phe residues. The PAMAM dendrimers are known to encapsulate various drug molecules. For these reasons, temperature-sensitive dendrimers might be useful as efficient drug carriers with controlled size and temperature-responsive properties.