Sohn Jeong Sun, Yoon Doo-Soo, Sohn Jun Youn, Park Jeong-Sook, Choi Jin-Seok
Division of Undeclared Majors, Chosun University, Gwangju 501-759, South Korea.
Department of Bioenvironmental & Chemical Engineering, Chosun College of Science & Technology, Gwangju 501-744, South Korea.
Mater Sci Eng C Mater Biol Appl. 2017 Mar 1;72:228-237. doi: 10.1016/j.msec.2016.11.065. Epub 2016 Nov 18.
To overcome the toxicity of excipient or blank nanoparticles for drug delivery nano-system, the surface modified paclitaxel nanocrystals (PTX-NC) have been developed. PTX-NCs were prepared by nano-precipitation method. The surface of PTX-NCs were modified by grafting with apo-transferrin (Tf) or hyaluronic acid (HA). The physical properties of PTX-NCs were evaluated by field emission scanning electron microscope (FE-SEM), zeta-sizer, zeta-potential, differential scanning calorimetry (DSC) and Fourier transform infrared (FT-IR) spectrometry. In vitro drug release study was performed in phosphate buffered saline (PBS) with or without 0.5% (w/v) Tween 80 for 24h. Cellular uptake was studied at time intervals of 0.5, 1, and 2h in MCF-7 cells, and cell growth inhibition study was performed for 24h using MCF-7 cells (cancer cells), and HaCaT cells (normal cells). Three different types of PTX-NCs with a mean size of 236.0±100.6nm (PTX-NC), 302.0±152.0nm (Tf-PTX-NC) and 339±180.6nm (HA-PTX-NC) were successfully prepared. The drug release profiles showed 29.1%/6.9% (PTX (pure)), 40.7%/23.9% (PTX-NC), 50.5%/25.1% (Tf-PTX-NC) and 46.8/24.8% (HA-PTX-NC) in PBS with/without 0.5% (w/v) Tween 80 for 24h, respectively. As per the results, the drug release of PTX-NCs showed the faster release as compared to that of PTX (pure). Surface modified PTX-NCs exhibited higher values for cell permeability than unmodified PTX-NC in the cellular uptake study. Surface modified PTX-NCs inhibited the cell growth approximately to 60% in MCF-7 cells, however effect of surface modified PTX-NCs on normal cell line was lower than the PTX-NC and PTX (pure). In conclusion, biological macromolecules (Tf or HA) surface modified PTX-NC enhanced the cellular uptake and the cell growth inhibition.
为克服辅料或空白纳米颗粒对药物递送纳米系统的毒性，已研发出表面修饰的紫杉醇纳米晶体（PTX-NC）。PTX-NC通过纳米沉淀法制备。通过接枝脱铁转铁蛋白（Tf）或透明质酸（HA）对PTX-NC的表面进行修饰。通过场发射扫描电子显微镜（FE-SEM）、zeta粒度分析仪、zeta电位仪、差示扫描量热法（DSC）和傅里叶变换红外（FT-IR）光谱仪对PTX-NC的物理性质进行评估。在含或不含0.5%（w/v）吐温80的磷酸盐缓冲盐水（PBS）中进行24小时的体外药物释放研究。在MCF-7细胞中于0.5、1和2小时的时间间隔研究细胞摄取情况，并使用MCF-7细胞（癌细胞）和HaCaT细胞（正常细胞）进行24小时的细胞生长抑制研究。成功制备了三种平均粒径分别为236.0±100.6nm（PTX-NC）、302.0±152.0nm（Tf-PTX-NC）和339±180.6nm（HA-PTX-NC）的不同类型的PTX-NC。药物释放曲线显示，在含/不含0.5%（w/v）吐温80的PBS中24小时时，释放率分别为29.1%/6.9%（PTX（纯品））、40.7%/23.9%（PTX-NC）、50.5%/25.1%（Tf-PTX-NC）和46.8/24.8%（HA-PTX-NC）。根据结果，与PTX（纯品）相比，PTX-NC的药物释放更快。在细胞摄取研究中，表面修饰的PTX-NC比未修饰的PTX-NC表现出更高的细胞通透性值。表面修饰的PTX-NC在MCF-7细胞中使细胞生长抑制约达60%，然而表面修饰的PTX-NC对正常细胞系的作用低于PTX-NC和PTX（纯品）。总之，生物大分子（Tf或HA）表面修饰的PTX-NC增强了细胞摄取和细胞生长抑制作用。
