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采用甘草酸二钾为膜软化剂,以逆向蒸发法制备甲氨蝶呤柔性纳米脂质体。并以包封率为评价指标,采用正交设计优化处方。结果表明,优化后的甲氨蝶呤柔性纳米脂质体呈球形,平均粒径(212.7±3.9)nm,电位(-19.7±0.2)mV,平均包封率(25.62±0.18)%。初步稳定性研究显示,制品在4℃放置10 d,外观、平均粒径、电位和包封率无显著改变。采用离体乳猪皮肤为渗透屏障,对比了甲氨蝶呤柔性纳米脂质体凝胶及其普通凝胶的透皮情况。结果表明,两种制剂的24 h累积透过量分别为(4.22±1.74)和(25.38±30.60)g/cm2,皮肤滞留量分别为(301.30±69.87)和(138.89±49.56)g/g。
Dipotassium glycyrrhizinate was used as membrane softener to prepare methotrexate flexible nanoliposome by reverse evaporation method. Taking the entrapment efficiency as the evaluation index, orthogonal design was adopted to optimize the prescription. The results showed that the optimized methotrexate nanospheres were spherical with an average diameter of 212.7 ± 3.9 nm and a potential of -19.7 ± 0.2 mV with an average entrapment efficiency of 25.62 ± 0.18%. Preliminary stability studies showed that the product was placed at 4 ℃ for 10 d, the appearance, average particle size, potential and encapsulation efficiency did not change significantly. The skin of suckling piglets was used as the osmotic barrier, and the transdermal conditions of methotrexate flexible nano-liposome gel and its common gel were compared. The results showed that the accumulated permeation rates of the two preparations for 24 h were (4.22 ± 1.74) and (25.38 ± 30.60) g / cm2, respectively, and the skin retention was (301.30 ± 69.87) and (138.89 ± 49.56) g / g, respectively.