新型透明质酸包裹的疏水改性壳聚糖聚电解质复合药物用于阿霉素的递送。
Novel hyaluronic acid coated hydrophobically modified chitosan polyelectrolyte complex for the delivery of doxorubicin.
机构信息
Key Laboratory of Biomaterials of Guangdong Higher Education Institutes, Guangdong Provincial Engineering and Technological Research Center for Drug Carrier Development, Department of Biomedical Engineering, Jinan University, Guangzhou 510632, China; Department of Chemistry, Jinan University, Guangzhou 510632, China.
Key Laboratory of Biomaterials of Guangdong Higher Education Institutes, Guangdong Provincial Engineering and Technological Research Center for Drug Carrier Development, Department of Biomedical Engineering, Jinan University, Guangzhou 510632, China.
出版信息
Int J Biol Macromol. 2019 Apr 1;126:254-261. doi: 10.1016/j.ijbiomac.2018.12.215. Epub 2018 Dec 22.
The aim of this work was to examine the formation and properties of a novel polyelectrolyte complex of drug carrier system for the delivery of doxorubicin (DOX), which consists of hyaluronic acid (HA) coated hydrophobically modified chitosan (CS). Various batches of polyelectrolyte complexes with the molar ratio of deoxycholic acid (DCA) and chitosan (CS) of 0.1, 0.2, 0.3 were prepared, and were termed as CS-DCA, CS-DCA, and CS-DCA respectively. The samples were characterized by Fourier transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD), Transmission electron microscopy (TEM), nuclear magnetic resonance hydrogen spectrum (H NMR) and dynamic light scattering (DLS). Particle sizes of synthesized polyelectrolyte complex nanoparticles (PCNs) were found to be in the range of 280-310 nm, larger than those of uncoated nanoparticles (~150 nm). The PCNs have large zeta potentials (about 26 mV) which make them stable and no sizes' change was determined. DOX could be easily incorporated into the PCNs with encapsulation efficiency (56%) and kept a sustained release manner without burst effect when exposed to PBS (pH 7.4) at 37 °C. Overall, these findings confirmed the potential of these PCNs for drug carrier and prolonged and sustained delivery in the bloodstream.
这项工作的目的是研究一种新型的药物载体系统的聚电解质复合物的形成和性质，该系统由透明质酸（HA）包覆的疏水改性壳聚糖（CS）组成。制备了具有不同摩尔比的脱氧胆酸（DCA）和壳聚糖（CS）的 0.1、0.2、0.3 批聚电解质复合物，并分别命名为 CS-DCA、CS-DCA 和 CS-DCA。通过傅里叶变换红外（FTIR）光谱、X 射线衍射（XRD）、透射电子显微镜（TEM）、氢核磁共振谱（H NMR）和动态光散射（DLS）对样品进行了表征。合成的聚电解质复合物纳米颗粒（PCN）的粒径在 280-310nm 之间，大于未包覆的纳米颗粒（约 150nm）。PCN 具有较大的 zeta 电位（约 26mV），使其稳定，且在 37°C 的 PBS（pH 7.4）中不会发生尺寸变化。DOX 可以很容易地掺入 PCN 中，包封效率（56%），在暴露于 PBS（pH 7.4）时没有突释效应，保持持续释放。总的来说，这些发现证实了这些 PCN 作为药物载体的潜力，以及在血液中延长和持续释放的潜力。
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