Copolymers of N-isopropylacrylamide, HEMA-lactate and acrylic acid with time-dependent lower critical solution temperature as a bioresorbable carrier

Copolymers of N-isopropylacrylamide, HEMA-lactate and acrylic acid with time-dependent lower critical solution temperature as a bioresorbable carrier
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DOI:
10.1002/pi.1709
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发表时间:
2005-02-01
影响因子:
3.2
通讯作者:
Vernon, B
Vernon, B
中科院分区:
化学3区
文献类型:
--
作者:
Lee, BH;Vernon, B

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以N-异丙基丙烯酰胺(NIPAAm)、甲基丙烯酸2-羟乙酯乳酸酯(HEMA-lactate)和丙烯酸(AAc)为单体,通过改变单体的摩尔比,制备了具有时间依赖性的低临界溶解温度(LCST)的可生物吸收原位凝胶材料。用核磁共振、凝胶渗透色谱和差示扫描量热法对合成的共聚物进行了表征。在pH 7.4的0.1 M磷酸盐缓冲盐水溶液中,这些共聚物具有低于体温的LCST。随着共聚物中HEMA-乳酸酯含量的增加,LCST降低。此外,在这些条件下,由于HEMA-乳酸酯的水解,共聚物的LCST表现出时间依赖性。随着HEMA-乳酸盐水解,共聚物变得更加亲水,从而导致LCST增加。这种亲水性导致约6摩尔%的AAc的共聚物在水解后表现出高于体温的LCST。在中性溶液中,具有不同摩尔%的AAc的共聚物在一到十天内看到它们的LCST升高到37 ℃以上,这取决于HEMA-乳酸盐/NIPAAm的比率,这是由于HEMA-乳酸盐的完全水解。上述性质表明,这些共聚物可用于药物递送,因为它们的可变LCST使它们具有生物可吸收性。(C)2004化学工业协会。
Copolymers of N-isopropylacrylamide (NIPAAm), 2-hydroxyethyl methacryl lactate (HEMA-lactate) and acrylic acid (AAc) were prepared, with varying mole ratios of monomers, to develop a bioresorbable in-situ-gelling material with a time-dependent lower critical solution temperature (LCST). The synthesized copolymers were characterized by nuclear magnetic resonance, gel permeation chromatography and differential scanning calorimetry. In 0.1 M phosphate-buffered saline solution of pH 7.4, these copolymers had an LCST below body temperature. The LCST decreased as the HEMA-lactate content of the copolymers was increased. Furthermore, in these conditions, the LCST of the copolymers exhibited time-dependent properties, due to hydrolysis of the HEMA-lactate. As the HEMA-lactate hydrolyzed, the copolymers became more hydrophilic, thereby leading to an increase in LCST. This hydrophilicity caused copolymers of approximately 6 mol% of AAc to exhibit an LCST above body temperature after hydrolysis. In neutral solution, copolymers with varying mol% of AAc saw their LCST rise above 37degreesC within one to ten days, depending upon the HEMA-lactate/NIPAAm ratio, due to the complete hydrolysis of the HEMA-lactate. The above properties indicate that these copolymers would be useful for drug delivery because their variable LCST makes them bioresorbable. (C) 2004 Society of Chemical Industry.