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姜黄素与透明质酸结合可提高其水溶解度和稳定性。

Conjugation of curcumin onto hyaluronic acid enhances its aqueous solubility and stability.

机构信息

Laboratory for Polymer Analysis, Biomedical Technology Wing, Sree Chitra Tirunal Institute for Medical Sciences & Technology, Poojapura, Trivandrum 695 012, India.

出版信息

J Colloid Interface Sci. 2011 Jul 1;359(1):318-25. doi: 10.1016/j.jcis.2011.03.071. Epub 2011 Apr 13.


DOI:10.1016/j.jcis.2011.03.071
PMID:21492865
Abstract

Polymer-drug conjugates have gained much attention largely to circumvent lower drug solubility and to enhance drug stability. Curcumin is widely known for its medicinal properties including its anticancer efficacy. One of the serious drawbacks of curcumin is its poor water solubility which leads to reduced bioavailability. With a view to address these issues, we synthesized hyaluronic acid-curcumin (HA-Cur) conjugate. The drug conjugate was characterized using FT-IR, NMR, Dynamic light scattering and TEM techniques. The conjugates, interestingly found to assembles as micelles in aqueous phase. The formation of micelles seems to improve the stability of the drug in physiological pH. We also assessed cytotoxicity of the conjugate using L929 fibroblast cells and quantified by MTT assay.

摘要

聚合物-药物偶联物受到了广泛关注,主要是为了克服药物溶解度低和增强药物稳定性。姜黄素以其药用特性而广为人知,包括其抗癌功效。姜黄素的一个严重缺点是其水溶性差,导致生物利用度降低。为了解决这些问题,我们合成了透明质酸-姜黄素(HA-Cur)偶联物。使用傅里叶变换红外光谱(FT-IR)、核磁共振(NMR)、动态光散射和透射电子显微镜(TEM)技术对药物偶联物进行了表征。有趣的是,偶联物在水相中被发现组装成胶束。胶束的形成似乎提高了药物在生理 pH 值下的稳定性。我们还使用 L929 成纤维细胞通过 MTT 测定法评估了偶联物的细胞毒性。

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