Department of Pharmaceutics, Shenyang Pharmaceutical University, Liaoning, China.
Int J Pharm. 2011 Jan 17;403(1-2):219-29. doi: 10.1016/j.ijpharm.2010.10.020. Epub 2010 Oct 29.
The evaluation of N-trimethyl chitosan (TMC)-coated liposomes containing Coenzyme Q(10) as potential ophthalmic drug delivery system was carried out. Firstly, transcorneal permeation studies were conducted at 34°C using a side-by-side diffusion apparatus. The transport process of the fluorescent marker, rhodamine B, across the corneal epithelium was visualized with confocal laser scanning microscopy. Secondly, the human lens epithelial cells (HLECs) were cultured without or with Coenzyme Q(10) followed by addition of H(2)O(2). The cell viability and apoptosis were evaluated. The permeability coefficient for rhodamine B with TMC-coated liposomes increased more than two times in comparison with the value obtained for solution as control, from (0.42±0.018)×10(5)cms(-1) to (1.31±0.030)×10(5)cms(-1). Confocal laser scanning microscopy revealed that a TMC coating enhanced the transepithelial transport, dependent on the TMC concentration and contacting time. Coenzyme Q(10) elevated the cell viability and reduced the oxidative damage with the decreased percentage of apoptotic cells in a positive concentration-dependent manner. The ATP content of liposome-treated cells was increased about 2-fold compared with that of H(2)O(2)-treated cells. Together, our findings demonstrate that with the enhanced permeation effect of the TMC coating, Coenzyme Q(10)-loaded TMC-coated liposomes appear to be a promising ophthalmic drug delivery carrier with an efficacy in protecting HLECs against H(2)O(2)-induced oxidative damage.
评价 N-三甲基壳聚糖(TMC)包裹的辅酶 Q(10)脂质体作为潜在的眼部药物传递系统。首先,在 34°C 下使用侧-侧扩散装置进行角膜透过性研究。用共焦激光扫描显微镜可视化荧光标记物罗丹明 B 穿过角膜上皮的传输过程。其次,培养不含或含辅酶 Q(10)的人晶状体上皮细胞 (HLECs),然后加入 H(2)O(2)。评估细胞活力和细胞凋亡。与作为对照的溶液相比,TMC 包裹的脂质体的罗丹明 B 的渗透系数增加了两倍以上,从(0.42±0.018)×10(5)cms(-1)增加到(1.31±0.030)×10(5)cms(-1)。共聚焦激光扫描显微镜显示,TMC 涂层增强了跨上皮转运,这取决于 TMC 浓度和接触时间。辅酶 Q(10)以浓度依赖性方式提高细胞活力并降低氧化损伤,使凋亡细胞的百分比降低。与 H(2)O(2)处理的细胞相比,脂质体处理的细胞中的 ATP 含量增加了约 2 倍。总之,我们的研究结果表明,TMC 涂层具有增强的渗透作用,载有辅酶 Q(10)的 TMC 包裹的脂质体似乎是一种有前途的眼部药物传递载体,可有效保护 HLECs 免受 H(2)O(2)诱导的氧化损伤。
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