载铜纳米粒鼻用原位凝胶体外释放度研究

为研究载铜纳米粒鼻用原位凝胶（TETA-Cu-NPs-gel）中三乙烯四胺铜（TETA-Cu）的体外释放规律,本文通过透析法研究TETA-Cu的体外释放度,以0.1 mol?mL-1磷酸盐缓冲液（PBS,pH7.4）为释放介质,并用Origin软件对释药数据进行模型拟合。采用高效液相色谱法检测TETA-Cu在溶出介质中的释放水平,以Swell ChromplusTM C18（4. 6 mm × 150 mm,5 μm）为色谱柱,流动相A为pH3.0磷酸盐缓冲液,流动相B为甲醇（A: B = 90:10）,流速1.0 mL?min-1,检测波长为260 nm。结果表明,TETA-Cu在0.05-1mg?mL-1 范围内线性关系良好,高、中、低三个浓度的回收率在99.9%~101.0%,RSD均小于2%;与TETA-Cu溶液相比,TETA-Cu-NPs-gel释药速率缓慢,符合一级释药动力学方程。可见,本研究所建立的TETA-Cu-NPs-gel体外释放度测定方法准确、简便可行。TETA-Cu-NPs-gel具有缓释的作用。

In vitro release of copper-loaded nanoparticles from nasal insitu gels

In order to study the in vitro release pattern of copper triethylenetetramine (TETA-Cu) from copper-loaded nanoparticles in nasal in situ gels (TETA-Cu-NPs-gel) . Dialysis was used to investigate In vitro release. 0.1 mol?mL-1 phosphate buffer solution (PBS, pH 7.4) was used as the release medium and the model was fitted to the release data using Origin software. HPLC was used to investigate the release level of TETA-Cu in dissolution media. The chromatographic column was Swell ChromplusTM C18 (4.6 mm × 150 mm, 5 μm), mobile phase A was pH 3.0 phosphate buffer, and mobile phase B was methanol (A: B = 90:10). The flow rate was 1.0 mL?min-1, the detection wavelength was 260 nm, Intake quantity 20 μL. The results show that TETA-Cu showed good linearity in the range of 0.05-1mg ?mL-1. The recoveries of the high, medium, and low concentrations are in the range of 99.9%~101.0%, with the RSDs of less than 2%. Compared with the TETA-Cu solution, the rate of drug release of TETA-Cu-NPs-gel is slow, which conformed to the kinetic equation of the first level of drug release. It is concluded that the in vitro release assay of TETA-Cu-NPs-gel established in this study is accurate, simple, and feasible. TETA-Cu-NPs-gel has a slow-release effect.