Topical Delivery of 3-O-ethyl l-ascorbic Acid from Complex Solvent Systems
Topical Delivery of 3-O-ethyl l-ascorbic Acid from Complex Solvent Systems
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DOI：
10.3390/scipharm88020019
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发表时间：
2020-01-01
影响因子：
2.5
通讯作者：
Lane, Majella E.
中科院分区：
文献类型：
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作者：
Iliopoulos, Fotis;Al Hossain, A. S. M. Monjur;Lane, Majella E.
3-O-乙基l-抗坏血酸（EA）是维生素C的醚衍生物，广泛用于护肤制剂中。以前，我们报道了纯溶剂对EA经皮吸收的影响，并观察到0.6-7.5%的应用EA在24小时内通过皮肤递送。在这项工作中，我们设计了复杂的配方，使用的溶剂组合，可能会发挥协同作用，并检查其对EA渗透在猪皮肤在体外有限剂量条件下的影响。丙二醇（PG）和丙二醇单月桂酸酯（PGML）的二元组合与单独的溶剂相比，能有效地促进EA的皮肤渗透（p < 0.05）。与纯溶剂相比，PGML与1，2-己二醇（HEX）的组合没有导致显著更高的EA渗透（p > 0.05）。此外，挥发性溶剂异丙醇（IPA）PG解决方案也没有改善EA的皮肤交付相比，纯PG。三元溶剂系统含有PG：PGML随后通过添加亲脂性溶剂，无论是肉豆蔻酸异丙酯（IPM），中链甘油三酯（MCT）或异硬脂酸异硬脂酯（ISIS）制备。PG：PGML：IPM为最佳载体，促进EA经皮释放达70.9%。PG：PGML：ISIS媒介物也促进EA穿过皮肤的渗透，但程度显著低于含IPM的媒介物。PG：PGML：MCT混合物未观察到EA递送增强。这些结果将为将来EA的靶向制剂的开发提供信息。
3-O-ethyl l-ascorbic acid (EA), an ether derivative of Vitamin C, is widely used in skincare formulations. Previously, we reported the effects of neat solvents on EA percutaneous absorption and observed that 0.6-7.5% of the applied EA was delivered through the skin over 24 h. In this work, we designed complex formulations using combinations of solvents that may act synergistically and examined their impact on EA permeation in porcine skin in vitro under finite dose conditions. Binary combinations of propylene glycol (PG) with propylene glycol monolaurate (PGML) were effective in enhancing skin permeation of EA compared with individual solvents (p < 0.05). Combining PGML with 1,2-hexanediol (HEX) did not result in significantly higher EA permeation compared with the neat solvents (p > 0.05). Addition of the volatile solvent isopropyl alcohol (IPA) to PG solutions also did not improve EA skin delivery compared with neat PG. Ternary solvent systems containing PG:PGML were subsequently prepared by the addition of a lipophilic solvent, either isopropyl myristate (IPM), medium-chain triglycerides (MCT) or isostearyl isostearate (ISIS). The optimum vehicle, PG:PGML:IPM, promoted up to 70.9% skin delivery of EA. The PG:PGML:ISIS vehicles also promoted EA permeation across the skin, but to a significantly lesser extent than the IPM-containing vehicles. No enhancement of EA delivery was noted for the PG:PGML:MCT mixtures. These results will inform the development of targeted formulations for EA in the future.