Sebastiani P, Nicoli S, Santi P
Dipartimento Farmaceutico, University of Parma, Parco Area delle Scienze, 43100 Parma, Italy.
Int J Pharm. 2005 Mar 23;292(1-2):119-26. doi: 10.1016/j.ijpharm.2004.11.038.
The aim of this paper was to explore the efficacy of lactic acid as permeation enhancer for drug molecules across the skin. Three model permeants were chosen: acetaminophen (non-ionized), buspirone hydrochloride (cationic drug) and ibuprofen lysine (anionic drug). We also explored the association of lactic acid and iontophoresis as a means of enhancing drug delivery. Permeation experiments were performed in vitro, using rabbit ear skin as barrier. The results obtained indicate that lactic acid has some effects on model drug permeation across the skin. The effect was more evident with the anionic drug ibuprofen. Cathodal intophoresis increased ibuprofen transport, but when lactic acid was associated with cathodal iontophoresis, a concentration-dependent reduction of ibuprofen iontophoretic flux was observed, probably for the competition by the co-ion. The application of electric current (anodal iontophoresis) to a solution of acetaminophen produced an increase in its transport, due to the presence of an electroosmotic contribution; however, the effect of the association of anodal iontophoresis and lactic acid produced no further enhancement.
本文旨在探讨乳酸作为药物分子经皮渗透促进剂的功效。选择了三种模型渗透物：对乙酰氨基酚（非离子化）、盐酸丁螺环酮（阳离子药物）和赖氨酸布洛芬（阴离子药物）。我们还研究了乳酸与离子电渗疗法联合使用作为增强药物递送的一种手段。使用兔耳皮肤作为屏障进行体外渗透实验。所得结果表明，乳酸对模型药物经皮渗透有一定影响。对于阴离子药物布洛芬，这种影响更为明显。阴极离子电渗疗法增加了布洛芬的转运，但当乳酸与阴极离子电渗疗法联合使用时，观察到布洛芬离子电渗通量呈浓度依赖性降低，这可能是由于共离子的竞争。对乙酰氨基酚溶液施加电流（阳极离子电渗疗法）会使其转运增加，这是由于存在电渗作用；然而，阳极离子电渗疗法与乳酸联合使用并未产生进一步的增强作用。
