Xie Jingwei, Marijnissen Jan C M, Wang Chi-Hwa
Department of Chemical and Biomolecular Engineering, National University of Singapore, 4 Engineering Drive 4, Singapore 117576, Singapore.
Biomaterials. 2006 Jun;27(17):3321-32. doi: 10.1016/j.biomaterials.2006.01.034. Epub 2006 Feb 21.
This study aims to fabricate biodegradable polymeric particles by electrohydrodynamic atomization (EHDA) for applications in sustained delivery of anticancer drug-paclitaxel to treat C6 glioma in vitro. Controllable morphologies such as spheres, doughnut shapes and corrugated shapes with sizes from several tens of microns to hundred nanometers of particles were observed by scanning electron microscopy (SEM) and field emission electron microscope (FSEM). The differential scanning calorimetry (DSC) study indicated that paclitaxel could be either in an amorphous or disordered-crystalline phase of a molecular dispersion or a solid solution state in the polymer matrix after fabrication. The X-ray photoelectron spectroscopy (XPS) result suggested that some amount of paclitaxel could exist on the surface layer of the microparticles. The encapsulation efficiency was around 80% and more than 30 days in vitro sustained release profile could be achieved. Cell cycling results suggested that paclitaxel after encapsulation by EHDA could keep its biological function and inhibit C6 glioma cells in G2/M phase. The cytotoxicity of paclitaxel-loaded biodegradable microparticles to C6 glioma cells could be higher than Taxol in the long-term in vitro tests evaluated by MTS assay. The drug delivery devices developed by EHDA in this study could be promising for the local drug delivery to treat malignant glioma.
本研究旨在通过电液动力雾化（EHDA）制备可生物降解的聚合物颗粒，用于体外持续递送抗癌药物紫杉醇以治疗C6胶质瘤。通过扫描电子显微镜（SEM）和场发射电子显微镜（FSEM）观察到了尺寸从几十微米到几百纳米的可控形态，如球形、甜甜圈形和波纹形颗粒。差示扫描量热法（DSC）研究表明，制备后紫杉醇在聚合物基质中可能处于分子分散或固溶体状态的非晶态或无序结晶相。X射线光电子能谱（XPS）结果表明，微粒表面层可能存在一定量的紫杉醇。包封率约为80%，体外可持续释放30多天。细胞周期结果表明，经EHDA包封后的紫杉醇能保持其生物学功能，并在G2/M期抑制C6胶质瘤细胞。在通过MTS法评估的长期体外试验中，负载紫杉醇的可生物降解微粒对C6胶质瘤细胞的细胞毒性可能高于紫杉醇。本研究中通过EHDA开发的药物递送装置有望用于局部药物递送以治疗恶性胶质瘤。
