Lian Ting, Peng Mingli, Vermorken Alphons J M, Jin Yanyan, Luo Zhiyi, Van de Ven Wim J M, Wan Yinsheng, Hou Peng, Cui Yali
J Nanosci Nanotechnol. 2016 Jun;16(6):6258-64. doi: 10.1166/jnn.2016.11370.
Curcumin, a polyphenol extracted from turmeric (Curcuma longa), has emerged as a potent multimodal cancer-preventing agent. It may attenuate the spread of cancer and render chemotherapy more effective. However, curcumin is neither well absorbed nor well retained in the blood, resulting in low efficacy. In an attempt to enhance the potency and to improve the bioavailability of curcumin, new delivery agents, hydroxypropyl-beta-cyclodextrin (HP-β-CD)-modified GoldMag nanoparticles (CD-GMNs) were designed and synthesized to incorporate curcumin. The CD-GMNs were characterized by Fourier Transform Infrared Spectroscopy (FT-IR), Thermo-gravimetric Analysis (TGA), X-ray Diffraction (XRD), Dynamic Light Scattering measurements (DLS), Transmission Electron Microscopy (TEM) and Vibrating Sample Magnetometer (VSM) analyses. For the magnetic carrier of CD-GMNs, the content of HP-β-CD was 26.9 wt%. CD-GMNs have a saturation magnetization of 22.7 emu/g with an average hydrodynamic diameter of 80 nm. The curcumin loading, encapsulation efficiency and releasing properties in vitro were also investigated. The results showed that the drug encapsulation ratio was 88% and the maximum curcumin loading capacity of CD-GMNs was 660 μg/5 mg. In vitro drug release studies showed a controlled and pH-sensitive curcumin release over a period of one week. Collectively, our data suggest that HP-β-CD-modified GoldMag nanoparticles can be considered to form a promising delivery system for curcumin to tumor sites. Targeting can be achieved by the combined effects of the application of an external magnetic field and the effect on drug release of lower pH values often found in the tumor microenvironment.
姜黄素是从姜黄(Curcuma longa)中提取的一种多酚,已成为一种有效的多模式癌症预防剂。它可能会减弱癌症的扩散并使化疗更有效。然而,姜黄素在血液中的吸收和保留都不好,导致疗效较低。为了提高姜黄素的效力并改善其生物利用度,设计并合成了新型递送剂——羟丙基-β-环糊精(HP-β-CD)修饰的金磁纳米颗粒(CD-GMNs)来包裹姜黄素。通过傅里叶变换红外光谱(FT-IR)、热重分析(TGA)、X射线衍射(XRD)、动态光散射测量(DLS)、透射电子显微镜(TEM)和振动样品磁强计(VSM)分析对CD-GMNs进行了表征。对于CD-GMNs的磁性载体,HP-β-CD的含量为26.9 wt%。CD-GMNs的饱和磁化强度为22.7 emu/g,平均流体动力学直径为80 nm。还研究了姜黄素的负载量、包封效率和体外释放特性。结果表明,药物包封率为88%,CD-GMNs的最大姜黄素负载量为660 μg/5 mg。体外药物释放研究表明,姜黄素在一周内呈可控的pH敏感释放。总体而言,我们的数据表明,HP-β-CD修饰的金磁纳米颗粒可被视为一种有前景的将姜黄素递送至肿瘤部位的递送系统。通过施加外部磁场的联合作用以及肿瘤微环境中常见的较低pH值对药物释放的影响,可以实现靶向递送。