Facile synthesis of drug-conjugated PHPMA core-crosslinked star polymers
Facile synthesis of drug-conjugated PHPMA core-crosslinked star polymers
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DOI：
10.1039/c5py00497g
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发表时间：
2015-06
影响因子：
4.6
通讯作者：
B. S. Tucker;Stephen G. Getchell;Megan R. Hill;B. Sumerlin
中科院分区：
文献类型：
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作者：
B. S. Tucker;Stephen G. Getchell;Megan R. Hill;B. Sumerlin
聚（N-（2-羟丙基）甲基丙烯酰胺）（PHPMA）是一种生物相容性和非免疫原性聚合物，用于形成核心交联星形聚合物，用于潜在的药物输送应用。通过改变 PHPMA 单聚体的分子量、[交联剂]:[单聚体]比例和溶剂，研究了 PHPMA 星形的形成条件。然后，在 PHPMA 单聚体的交联反应过程中，通过直接共聚 HPMA 修饰的抗癌药物甲氨蝶呤，使用优化的条件形成载药 PHPMA 星形聚合物。通过1H NMR光谱证实药物的掺入，并使用紫外-可见光谱确定20wt%的载药量。我们最初的药物释放研究表明，添加酯酶会诱导药物释放。
Poly(N-(2-hydroxypropyl)methacrylamide) (PHPMA), a biocompatible and non-immunogenic polymer, was used to form core-crosslinked star polymers for potential drug delivery applications. The conditions for the formation of the PHPMA stars were studied by varying the molecular weight of the PHPMA unimers, [crosslinker]:[unimer] ratios, and solvent. The optimized conditions were then used to form drug-loaded PHPMA star polymers by directly copolymerizing an HPMA-modified anticancer drug, methotrexate, during the crosslinking reaction of PHPMA unimers. The incorporation of the drug was confirmed by 1H NMR spectroscopy, and UV-visible spectroscopy was used to determine a drug loading of 20 wt%. Our initial drug release studies showed that the addition of an esterase induced drug release.