Tapfumaneyi Pronalis, Phan Khanh, Huang Yicheng, Sodsri Kewaree, Namjoshi Sarika, Maibach Howard, Mohammed Yousuf
Faculty of Pharmacy, Rhodes University, Grahamstown, Makhanda 6139, South Africa.
Frazer Institute, Faculty of Health, Medicine and Behavioural Sciences, The University of Queensland, Brisbane, QLD 4102, Australia.
Pharmaceutics. 2025 Jun 10;17(6):764. doi: 10.3390/pharmaceutics17060764.
Human skin provides an effective route of delivery for selected drugs. Topical penetration of molecules is largely attributed to passive diffusion, and the degree of penetration can be represented by in silico, in vitro, and ex vivo models. Percutaneous absorption of pharmaceutical ingredients is a delicate balance between the molecular properties of the drug, the skin properties of the patients, and the formulation properties. Understanding this interplay can aid in the development of products applied to the skin. The kinetics of percutaneous absorption and an understanding of the rate-limiting steps involved can facilitate the optimization of these systems and enhance the degree to which skin drug delivery can be achieved. Solute-vehicle, vehicle-skin, and solute-skin interactions contribute notably to product release as well as the rate of absorption and diffusion across skin layers. These interactions alter the degree of permeation by interfering with the skin barrier or solubility and thermodynamic activity of the active pharmaceutical ingredient. This article aims to provide a concise understanding of some of the factors involved in the skin absorption of topical products, i.e., the pharmacokinetics of percutaneous absorption as well as the solute-vehicle-skin interactions that determine the rate of release of products and the degree of drug diffusion across the skin.
人体皮肤为某些药物提供了一条有效的给药途径。分子的局部渗透主要归因于被动扩散,其渗透程度可以通过计算机模拟、体外和离体模型来表示。药物成分的经皮吸收是药物分子特性、患者皮肤特性和制剂特性之间的微妙平衡。了解这种相互作用有助于开发应用于皮肤的产品。经皮吸收的动力学以及对所涉及的限速步骤的理解可以促进这些系统的优化,并提高实现皮肤给药的程度。溶质 - 载体、载体 - 皮肤和溶质 - 皮肤相互作用对产品释放以及跨皮肤层的吸收和扩散速率有显著贡献。这些相互作用通过干扰皮肤屏障或活性药物成分的溶解度和热力学活性来改变渗透程度。本文旨在简要介绍局部产品皮肤吸收所涉及的一些因素,即经皮吸收的药代动力学以及决定产品释放速率和药物跨皮肤扩散程度的溶质 - 载体 - 皮肤相互作用。