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目的:制备全反式维A酸(all-trans retinoic acid,ATRA)醇质体并对其稳定性及体外经皮渗透等进行考察。方法:采用注入法制备ATRA醇质体,通过正交设计优化制备工艺;同时测定其Zeta电位及粒径;以改进的Franz扩散池法,进行体外小鼠经皮渗透实验,测定药物累积渗透量及透皮速率。结果:优选处方组成为20%乙醇(w/w),4%磷脂(w/w),磷脂∶胆固醇(w/w)2∶1,磷脂∶维A酸(w/w)10∶1,检测平均粒径为237.3 nm,Zeta电位为-36.31 mV;ATRA醇质体放置1,10,20 d后,7 h累积透皮量分别为(210.6±1.7),(196.2±3.8)和(181.1±4.2)μg.cm-2,而水醇混合物累积透皮量仅为(120.4±5.4)μg.cm-2。结论:ATRA醇质体制备工艺简单可行,所得传递体粒径较小且均匀,室温放置较稳定,透皮效果较好并可以促进维A酸经皮转运。
OBJECTIVE: To prepare all-trans retinoic acid (ATRA) and investigate its stability and transdermal penetration in vitro. Methods: The ATRA ethosomes were prepared by injection method. The orthogonal design was used to optimize the preparation process. The Zeta potential and particle size were determined simultaneously. The percutaneous penetration of mice was evaluated by the improved Franz diffusion cell method. And transdermal rate. Results: A preferred formulation consisted of 20% ethanol (w / w), 4% phospholipid (w / w), phospholipid: cholesterol 2: 1, phospholipid: tretinoin 10: 1, The average particle size was 237.3 nm and the Zeta potential was -36.31 mV. The cumulative transdermal volume at 7 h was (210.6 ± 1.7), (196.2 ± 3.8) and (181.1 ± 4.2) μg.cm-2, while the cumulative transdermal volume of hydroalcoholic mixture was only (120.4 ± 5.4) μg.cm-2. CONCLUSION: The preparation process of ATRA is simple and feasible. The size and diameter of the obtained transfer medium are small and uniform, and it is stable at room temperature. The transdermal effect is good and transdermal delivery of retinoic acid can be promoted.