Otto A, du Plessis J, Wiechers J W
Unit for Drug Research and Development, North-West University, Potchefstroom Campus, Potchefstroom, South Africa.
Int J Cosmet Sci. 2009 Feb;31(1):1-19. doi: 10.1111/j.1468-2494.2008.00467.x.
It has been recognized that the vehicle in which a permeant is applied to the skin has a distinctive effect on the dermal and transdermal delivery of active ingredients. The cutaneous and percutaneous absorptions can be enhanced, e.g. by an increase in thermodynamic activity, supersaturation and penetration modifiers. Furthermore, dermal and transdermal delivery can be influenced by the interactions that may occur between the vehicle and the skin on the one hand, and interactions between the active ingredient and the skin on the other hand. Emulsions are widely used as cosmetic and pharmaceutical formulations because of their excellent solubilizing capacities for lipophilic and hydrophilic active ingredients and application acceptability. This review focuses, in particular, on the effect of emulsions on the dermal and transdermal delivery of active ingredients. It is shown that the type of emulsion (w/o vs. o/w emulsion), the droplet size, the emollient, the emulsifier as well as the surfactant organization (micelles, lyotropic liquid crystals) in the emulsion may affect the cutaneous and percutaneous absorption. Examples substantiate the fact that emulsion constituents such as emollients and emulsifiers should be selected carefully for optimal efficiency of the formulation. Moreover, to understand the influence of emulsion on dermal and transdermal delivery, the physicochemical properties of the formulation after application are considered.
人们已经认识到,将渗透剂应用于皮肤的载体对活性成分的真皮和透皮递送具有独特的影响。皮肤和经皮吸收可以通过例如热力学活性的增加、过饱和和渗透促进剂来增强。此外,真皮和透皮递送可能受到一方面载体与皮肤之间以及另一方面活性成分与皮肤之间可能发生的相互作用的影响。乳液因其对亲脂性和亲水性活性成分具有出色的增溶能力以及应用可接受性而被广泛用作化妆品和药物制剂。本综述特别关注乳液对活性成分真皮和透皮递送的影响。结果表明,乳液的类型(油包水型乳液与水包油型乳液)、液滴大小、润肤剂、乳化剂以及乳液中的表面活性剂组织(胶束、溶致液晶)可能会影响皮肤和经皮吸收。实例证实了这样一个事实,即应仔细选择乳液成分,如润肤剂和乳化剂,以实现制剂的最佳效果。此外,为了理解乳液对真皮和透皮递送的影响,还考虑了应用后制剂的物理化学性质。
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