β-Cyclodextrin-curcumin self-assembly enhances curcumin delivery in prostate cancer cells
β-Cyclodextrin-curcumin self-assembly enhances curcumin delivery in prostate cancer cells
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DOI：
10.1016/j.colsurfb.2010.03.039
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发表时间：
2010-08-01
影响因子：
5.8
通讯作者：
Chauhan, Subhash C.
中科院分区：
文献类型：
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作者：
Yallapu, Murali Mohan;Jaggi, Meena;Chauhan, Subhash C.
姜黄素是一种来源于姜黄属植物姜黄根茎的疏水性多酚类化合物，具有广泛的生物学应用，包括癌症治疗。然而，由于次优的药代动力学和肿瘤部位的生物利用度差，其在癌症治疗中的突出应用受到限制。为了改善姜黄素的亲水性和释药特性，我们采用包封技术制备了β-环糊精（β-CD）介导的姜黄素释药系统。姜黄素通过包合物机制包封到CD腔中。通过增加姜黄素与CD的比例来提高姜黄素的包封率。采用傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）、热重分析（TGA）、扫描电镜（SEM）和透射电镜（TEM）对CD-姜黄素复合物的形成进行了表征。评价了优化的CD-姜黄素复合物（CD 30）的细胞内摄取和抗癌活性。细胞增殖和克隆形成试验表明，与游离姜黄素相比，β-环糊精-姜黄素自组装增强了姜黄素的递送，并提高了其在前列腺癌细胞中的治疗功效。(C)2010 Elsevier B. V.保留所有权利。
Curcumin, a hydrophobic polyphenolic compound derived from the rhizome of the herb Curcuma long, possesses a wide range of biological applications including cancer therapy. However, its prominent application in cancer treatment is limited due to sub-optimal pharmacokinetics and poor bioavailability at the tumor site. In order to improve its hydrophilic and drug delivery characteristics, we have developed a beta-cyclodextrin (CD) mediated curcumin drug delivery system via encapsulation technique. Curcumin encapsulation into the CD cavity was achieved by inclusion complex mechanism. Curcumin encapsulation efficiency was improved by increasing the ratio of curcumin to CD. The formations of CD-curcumin complexes were characterized by Fourier transform infrared (FTIR), differential scanning calorimetry (DSC), thermo-gravimetric analysis (TGA), scanning electron microscope (SEM), and transmission electron microscope (TEM) analyses. An optimized CD-curcumin complex (CD30) was evaluated for intracellular uptake and anti-cancer activity. Cell proliferation and clonogenic assays demonstrated that beta-cyclodextrin-curcumin self-assembly enhanced curcumin delivery and improved its therapeutic efficacy in prostate cancer cells compared to free curcumin. (C) 2010 Elsevier B.V. All rights reserved.