Stability, cutaneous delivery, and antioxidant potential of a lipoic acid and α-tocopherol codrug incorporated in microemulsions.
Stability, cutaneous delivery, and antioxidant potential of a lipoic acid and α-tocopherol codrug incorporated in microemulsions.
复制标题
DOI：
10.1002/jps.24053
复制
发表时间：
2014-08
影响因子：
3.8
通讯作者：
Lopes, Luciana B.
中科院分区：
文献类型：
--
作者：
Thomas, Siji;Vieira, Camila S.;Hass, Martha A.;Lopes, Luciana B.
关键词：
本研究的目的是评估α-生育酚-硫辛酸联合药物的皮肤渗透性、稳定性和抗氧化作用。为了增强渗透，我们评价了三种水含量和油相组成不同的微乳液（肉豆蔻酸异丙酯与单辛酸甘油酯或油酸）。联合药物以1%（w/w）掺入。微乳液中的共药物水解随着时间（长达48小时）和制剂含水量（10- 30%，w/w）的增加而增加。24 h后，与对照制剂（肉豆蔻酸异丙酯中的20%单辛酸甘油酯）相比，微乳使共药物向猪耳皮肤活层中的递送增加了2.9-7.8倍。渗透增强作用受油相影响，含单辛酸甘油酯的制剂显示出最显著的效果。使用硫代巴比妥酸反应物质（TBARS）测定法在皮肤生物等效物中评估的抗氧化活性表明，与未负载制剂相比，用含联合药物的微乳处理后，TBARS水平降低了39%。除联合用药外，在活的生物等效组织中检测到生育酚（8.2 ± 0.6 μg/cm 2），表明联合用药在12 h后部分水解。总之，这些结果支持含有生育酚-硫辛酸联合药物的纳米分散制剂改善皮肤抗氧化活性的潜力。
The aim of this study was to assess the skin penetration, stability and antioxidant effects of a α-tocopherol-lipoic acid co-drug. To enhance penetration, we evaluated three microemulsions varying in water content and composition of the oil phase (isopropyl myristate with either monocaprylin or oleic acid). The co-drug was incorporated at 1% (w/w). Co-drug hydrolysis in the microemulsion increased with increases in time (up to 48 h) and formulation water content (10–30%, w/w). Microemulsions increased the co-drug delivery into viable layers of porcine ear skin by 2.9–7.8–fold compared to a control formulation (20% monocaprylin in isopropyl myristate) after 24 h. Penetration enhancement was influenced by the oil phase, with the formulation containing monocaprylin displaying the most pronounced effect. Antioxidant activity, assessed in skin bioequivalents using the thiobarbituric acid-reactive substances (TBARS) assay, demonstrated that TBARS levels decreased by 39% after treatment with the co-drug-containing microemulsion compared to the unloaded formulation. In addition to the co-drug, tocopherol (8.2 ± 0.6 μg/cm2) was detected in the viable bioequivalent tissues, suggesting that the co-drug was partly hydrolyzed after 12 h. Taken together, these results support the potential of nanodispersed formulations containing a tocopherol-lipoic acid co-drug to improve skin antioxidant activity.
登录
查看更多内容
影响因子：
3.4
作者：
McClements, David Julian
通讯作者：
McClements, David Julian
影响因子：
3.3
作者：
Hosmer, Jaclyn;Reed, Rachel;Lopes, Luciana B.
通讯作者：
Lopes, Luciana B.
DOI：
10.1016/s0939-6411(01)00160-6
发表时间：
2001-09-01
影响因子：
4.9
作者：
Lehmann, L;Keipert, S;Gloor, M
通讯作者：
Gloor, M
影响因子：
3.9
作者：
Malheiro, Arthur R.;Varanda, Laudemir C.;Villullas, H. Mercedes
通讯作者：
Villullas, H. Mercedes
影响因子：
5.8
作者：
Herwadkar, Anushree;Sachdeva, Vishal;Banga, Ajay K.
通讯作者：
Banga, Ajay K.