处方组成对槲皮素传递体透皮作用的影响

Effect of Formulation on Transdermal Delivery of Quercetin Transfersomes

采用注入法-高压均质法制备槲皮素(1)传递体。采用改良Franz扩散池法,考察不同表面活性剂(Tween-80、胆酸钠、癸酸钠及油酸钠)、氯化钠及磷脂种类对传递体中1的累积渗透量及皮肤滞留量的影响。其中,采用蛋黄卵磷脂以及Tween-80、胆酸钠、癸酸钠或油酸钠制备的1传递体,24 h累积渗透量分别为(9.37±2.59)、(8.73±1.34)、(6.79±1.83)和(3.46±0.66)mg/cm^2;皮肤滞留量为0.97~1.34mg/cm^2。与1混悬剂组[24 h累积渗透量为0,皮肤滞留量为(0.11±0.06)mg/cm^2]相比,传递体中1的透皮能力和皮肤滞留量显著提高(P<0.05);与油酸钠组相比,Tween-80组和胆酸钠组存在显著差异(P<0.05)。含Tween-80的传递体中加入氯化钠或用大豆磷脂替换蛋黄卵磷脂后,1的24 h累积渗透量增加至(13.03±4.15)或(10.58±6.98)mg/cm^2,但均没有显著差异(P>0.05)。结果显示,以Tween-80及大豆磷脂为材料,不加入氯化钠制备的1传递体z电位为(-38.0±1.5)mV,并显著提高了1的皮肤渗透性及滞留量。

The quercetin（1） transfersomes were prepared by injection and high-pressure homogenization method. The effects of surfactants （Tween-80, sodium cholate, sodium decanoate and sodium oleate）, sodium chloride and phospholipids used in the transfersome formulations on the cumulative permeation amount and skin retention of 1 were evaluated by the modified Franz diffusion cell method. The cumulative permeation amount of 1 transfersomes containing egg-yolk phosphatidylcholine （EPC） and Tween-80, sodium cholate, sodium decanoate or sodium oleate were （9.37±2.59）, （8.73±1.34）, （6.79±1.83） and（3.46±0.66）μg/cm2, respectively. And the retention amounts in skin of the above groups were in the range of 0.97—1.34 μg/cm2. Compared wiht 1 suspension, whose cumulative permeation amountat 24 h and skin retention were 0 and （0.11±0.06）μg/cm2, the permeation ability and skin retention of 1 transfersomes were significantly increased （P〈0.05）. Moreover, the cumulative permeation amounts of the transfersomes containing Tween-80 or sodium cholate were significantly higher than that of the transfersomes containing sodium oleate （P〈0.05）. Adding sodium chloride into the transfersomes containing Tween-80 or using soybean phosphatidylcholine （SPC） instead of EPC, the cumulative permeation amounts were increased to （13.03±4.15） or （10.58±6.98）μg/cm2, but there was no obvious differences were observed （P〉0.05）. The results showed that owing to its low ζ potential, transfersomes prepared by Tween-80 （especially that containing sodium chloride） showed a higher transdermal property and better affinity to the skin, whose pH value of the formulation was close to that of normal people, compared with vesicles prepared by other anionic surfactants （sodium cholate, sodium decanoate or sodium oleate）. In summary, the 1 transfersomes with Tween-80 and SPC and without NaCl led to high ζ potential [（-38.0±1.5）mV] and remarkable enhances of the cumulative permeation and retention amount of 1.