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为提高豆豉纤溶酶口服生物利用度,建立了豆豉纤溶酶载纳米脂质体系统,并对其表征进行评价。采用硫酸铵梯度法制备的豆豉纤溶酶纳米脂质体的包封率为(52.74±4.24)%,粒径(72.04±31.2)nm,平均Zeta电位-44.2 mV,PdI 0.237。试验结果表明:豆豉纤溶酶纳米脂质体在体外稳定性好,在人工肠液中的释放符合一级动力学释放规律,豆豉纤溶酶在12 h后释放接近完全,无突释现象。豆豉纤溶酶及载酶纳米脂质体肠吸收液酶活性测定结果表明:豆豉纤溶酶及其载酶纳米脂质体在小肠均有吸收,吸收后仍具有纤溶活性。纳米脂质体可有效促进豆豉纤溶酶的吸收。
In order to improve oral bioavailability of bean curd fibrinolytic enzyme, a nano-liposome system was established and its characterization was evaluated. The entrapment efficiency of nanometer liposomes prepared by ammonium sulfate gradient method was (52.74 ± 4.24)%, the diameter was (72.04 ± 31.2) nm, the average Zeta potential was -44.2 mV and PdI was 0.237. The experimental results showed that the nano-liposome of fibrolactam was stable in vitro and the release in artificial intestinal juice was in accordance with the first-order kinetic release rule. The release of fibrinolytic enzyme was nearly complete after 12 h without any burst release. The results showed that the enzyme activity of the intestinal absorption of bean curd fibrinolytic enzyme and enzyme-loaded nano-liposomes were both absorbed in the small intestine and still had fibrinolytic activity. Nano-liposomes can effectively promote the absorption of bean curd plasmin.