Unit for Drug Research and Development, North-West University, Potchefstroom Campus, Potchefstroom, South Africa.
Skin Pharmacol Physiol. 2010;23(5):273-82. doi: 10.1159/000314702. Epub 2010 May 18.
This study investigated the effect of emulsifiers and their liquid crystalline structures on the dermal and transdermal delivery of hydroquinone (HQ), salicylic acid (SA) and octadecenedioic acid (DIOIC). Emulsions containing liquid crystalline phases were compared with an emulsion without liquid crystals. Skin permeation experiments were performed using Franz-type diffusion cells and human abdominal skin dermatomed to a thickness of 400 mum. The results indicate that emulsifiers arranging in liquid crystalline structures in the water phase of the emulsion enhanced the skin penetration of the active ingredients with the exception of SA. SA showed a different pattern of percutaneous absorption, and no difference in dermal and transdermal delivery was observed between the emulsions with and without liquid crystalline phases. The increase in skin penetration of HQ and DIOIC could be attributed to an increased partitioning of the actives into the skin. It was hypothesized that the interaction between the different emulsifiers and active ingredients in the formulations varied and, therefore, the solubilization capacities of the various emulsifiers and their association structures.
本研究考察了乳化剂及其液晶结构对氢醌(HQ)、水杨酸(SA)和十八烯二酸(DIOIC)经皮和透皮传递的影响。将含有液晶相的乳液与不含液晶的乳液进行了比较。使用 Franz 型扩散池和厚度为 400 微米的人腹部皮肤进行皮肤渗透实验。结果表明,乳化剂在乳液水相中排列成液晶结构,除了 SA 之外,还增强了活性成分的皮肤穿透性。SA 表现出不同的经皮吸收模式,在具有和不具有液晶相的乳液之间,未见透皮和经皮传递的差异。HQ 和 DIOIC 皮肤穿透性的增加可归因于活性物质向皮肤中的分配增加。据推测,配方中不同乳化剂和活性成分之间的相互作用不同,因此各种乳化剂的增溶能力及其缔合结构也不同。