秋水仙碱类脂囊泡的制备及其经皮渗透性考察

Preparation and Percutaneous Permeability of Colchicine Niosomes

采用pH梯度法制备秋水仙碱(1)类脂囊泡,并通过单因素试验以包封率为评价指标筛选非离子表面活性剂组成和胆固醇含量。结果表明,最优处方中Span-60、Tween-80和胆固醇质量比为2∶2∶1。该优化制品平均粒径为(689.0±3.7)nm,ζ电位为(–14.11±0.45)mV,包封率为(78.82±0.64)%。初步稳定性试验表明,该制品于4℃贮存90 d的包封率无明显变化,泄漏率<10%。采用改良Franz扩散池试验,比较1水溶液及其类脂囊泡的体外透皮性能。结果显示,1类脂囊泡的体外累积透过量、稳态渗透速率和皮肤滞留量分别为水溶液组的2.08、1.74和1.69倍。大鼠经皮吸收试验表明,1-NS较1水溶液能显著增强1的透皮性能,且具有一定的缓释作用。

The colchicine niosomes(1-NS)were prepared by pH gradient method and the formulation parameters,namely the composition of non-ionic surfactants and amount of cholesterol,were optimized by single factor experiment with encapsulation efficiency(EE)as the indicator.The mean particle size,ζpotential and EE of the optimal 1-NS with the carrier consisted of Span-60,Tween-80 and cholesterol at a mass ratio of 2∶2∶1 were(689.0±3.7)nm,(–14.11±0.45)mV and(78.82±0.64)%,respectively.Preliminary stability test showed that the EE of the optimal 1-NS had no obvious changes during the storage at 4℃for 90 d,and the leakage rate was lower than 10%.A modified Franz diffusion cell test was carried out to compare the transdermal performances of 1 aqueous solution and 1-NS in vitro.The results showed that the cumulative amount,steady-state permeation rate and skin retention of 1-NS in vitro were 2.08,1.74 and 1.69 times as high as those of the aqueous solution.The results of percutaneous absorption in rats showed that 1-NS could significantly enhance the transdermal property of 1 and had a certain sustained-release effect compared with 1 aqueous solution.