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分别按照Touitou法和Cevc法制备5-氟尿嘧啶(1)乙醇脂质体和变形脂质体,并进行体外透瘢痕试验。建立了高效液相色谱法分析测定两者透过瘢痕组织的1累积含量及1在瘢痕组织中的滞留量。采用C18色谱柱,流动相为甲醇-水(5:95),检测波长265 nm。结果表明:透瘢痕试验24 h后,1乙醇脂质体、1变形脂质体及1 PBS溶液透过瘢痕组织的1累积透过量(μg.ml-1.cm-2)和在瘢痕组织的1滞留量(g/cm2)分别为:14.12±0.1和10.74±1.17、12.35±1.21和17.48±0.82、3.08±0.57和3.21±0.19。可见纳米级乙醇脂质体和变形脂质体均能有效促进1进入并透过瘢痕组织。相比之下,乙醇脂质体具有更好的透瘢痕作用,而变形脂质体能使5-FU在瘢痕组织内具有较高的滞留量。
The 5-Fluorouracil (1) liposomes and liposomes were prepared according to the Touitou method and the Cevc method, respectively. The in vitro scar test was also performed. A high performance liquid chromatography (HPLC) assay was established for the determination of 1 accumulation in scar tissue and 1 retention in scar tissue. The mobile phase was methanol-water (5:95) using a C18 column with a detection wavelength of 265 nm. The results showed that after 1 hour of scar test, the cumulative permeation amount of 1 ethanol liposome, 1 liposome and 1 PBS solution through scar tissue (μg.ml-1.cm-2) and in scar tissue 1 retention (g / cm2) were: 14.12 ± 0.1 and 10.74 ± 1.17, 12.35 ± 1.21 and 17.48 ± 0.82, 3.08 ± 0.57 and 3.21 ± 0.19, respectively. Visible nano-ethanol liposomes and liposomes can effectively promote the 1 into and through the scar tissue. In contrast, ethanol liposomes have a better scarring effect, whereas the deformable liposomes give 5-FU a higher retention in scar tissue.