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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。
Quercetin (1) mediator was prepared by injection method and high pressure homogenization method. The modified Franz diffusion cell method was used to investigate the effects of different surfactants (Tween-80, sodium cholate, sodium caprate and sodium oleate), sodium chloride and phospholipids on the cumulative permeation of 1 and the retention of skin influences. Among them, the cumulative transmission of 24 h after transfection with egg lecithin and Tween-80, sodium cholate, sodium caprate or sodium oleate was (9.37 ± 2.59), (8.73 ± 1.34), (6.79 ± 1.83) and (3.46 ± 0.66) mg / cm ~ 2 respectively. The retention of skin was 0.97 ~ 1.34 mg / cm ~ 2. Transdermal permeabilization 1 and transdermal delivery of 1 in the vehicle group were significantly increased (P <0.01), compared with those in the 1-suspension group [cumulative 24-hour permeation was 0 and skin retention was (0.11 ± 0.06) mg / 0.05). Compared with sodium oleate group, there was significant difference between Tween-80 group and sodium cholate group (P <0.05). After 24 h incubation, the cumulative permeation of 1 increased to (13.03 ± 4.15) or (10.58 ± 6.98) mg / cm ~ 2, respectively, after adding sodium chloride or replacing the yolk lecithin with soybean lecithin No significant difference (P> 0.05). The results showed that the z potential of 1-transferrin prepared without sodium chloride was (-38.0 ± 1.5) mV with Tween-80 and soybean lecithin, and the permeability and retention of 1 were significantly increased.