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目的:优化白芷香豆素脂质体的处方工艺并考察其释药性能。方法:采用薄膜-超声法制备白芷香豆素脂质体,在单因素试验基础上,以包封率、载药量为综合评价指标,利用Box-Behnken响应面试验考察脂胆比、脂药比和超声时间对处方工艺的影响,利用紫外分光光度法测定白芷香豆素含量,透射电镜观察脂质体的粒径形态及大小。结果:白芷香豆素脂质体最佳处方工艺为脂胆比(6∶1);脂药比(5∶1),超声时间34 min;制备的脂质体粒径均匀,呈球形小囊泡,分散性好,粒径(112.08±1.21)nm,包封率(94.02±1.56)%,载药量(5.42±0.35)%;游离白芷香豆素3 h的累积释放率达100%,空白脂质体与白芷香豆素的混合溶液12 h累积释放率95.3%,白芷香豆素脂质体12 h累积释放率45.6%。结论:该处方工艺稳定可行,制备的白芷香豆素脂质体包封率较高,形态和粒径较均匀,具有明显的缓释效果。
Objective: To optimize the formulation of coumarin liposomes and study their drug release properties. Methods: The radix Angelicae sinensis liposomes were prepared by the membrane-ultrasonic method. Based on the single-factor test, the encapsulation efficiency and drug loading were taken as the comprehensive evaluation indexes. Ratio and ultrasonic time on the prescription process, the use of UV spectrophotometry coumarin content, transmission electron microscopy liposome size and shape. Results: The optimal formulation of coumarin liposomes was the ratio of cholesterol to cholesterol (6:1), the ratio of lipid to drug (5:1), the time of ultrasound was 34 min. The prepared liposomes were uniform in size and spherical in shape (112.08 ± 1.21) nm, encapsulation efficiency (94.02 ± 1.56)% and drug loading (5.42 ± 0.35)% respectively. The cumulative release rate of coumarin from free Radix Angelicae dahurica for 3 h was 100% The cumulative release rate of the mixed solution of the blank liposomes and the angelica coumarin was 95.3% after 12 h, and the cumulative release rate of coumarin liposomes at 12 h was 45.6%. Conclusion: The prescription process is stable and feasible. The prepared encapsulation rate of Angelic-coumarin liposomes is high, the morphology and particle size are uniform, and the sustained-release effect is obvious.