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Dermal and Transdermal Formulations: How They Can Affect the Active Compound

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Percutaneous Penetration Enhancers Chemical Methods in Penetration Enhancement

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Abstract

Topical application of drugs has become very popular in the last decades. However, the outmost skin layer, the stratum corneum, represents an effective barrier against the intrusion of foreign substances and endogenous water loss, which has to be overcome. Besides ideal physicochemical properties of the applied drug, the formulation can promote drug diffusion into and through the different skin layers. Owing to the grade of disease or the localization of the treatment, various formulation types are commercially available, which can be classified into semisolid and liquid formulation types. Dermal therapeutics should deliver the drug in adequate concentrations to the right localization in the skin, where it should remain for a sufficient time period. A transdermal therapeutic, on the other hand, has to enable the drug to pass the skin and reach the blood and lymphatic system in order to act systemically. These processes, based on partition and diffusion of a drug, can be controlled by the formulation. Thus, various formulations with the same amount of the active compound provide different permeation profiles and skin concentrations of the active.

Topically applied formulations (dermal and transdermal formulations) present a complex mixture of various classes of substances, in order to ensure optimized pharmacological and sensory properties, as well as to pose no health risk for the consumer. Considering the physicochemical regularities of the drug diffusion process through the skin (e.g., Fick’s law of diffusion), various parameters like the diffusion or the partition coefficient can be altered to establish the desired permeation profile. However, each additive has to be critically examined, since interactions with the compound or the skin may occur.

As a consequence, each topically applied drug needs a formulation/vehicle precisely adapted to its physicochemical properties in order to provide an optimized diffusion into or through the skin.

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Authors and Affiliations

  1. Department of Pharmacology, Toxicology and Pharmacy, University of Veterinary Medicine Hannover, Foundation, Hannover, Germany

    Jessica Stahl

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  1. Jessica Stahl
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Correspondence to Jessica Stahl .

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  1. Apoteka "Beograd", Belgrade, Serbia

    Nina Dragicevic

  2. San Francisco, California, USA

    Howard I. Maibach

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Stahl, J. (2015). Dermal and Transdermal Formulations: How They Can Affect the Active Compound. In: Dragicevic, N., Maibach, H. (eds) Percutaneous Penetration Enhancers Chemical Methods in Penetration Enhancement. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-662-45013-0_15

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  • DOI: https://doi.org/10.1007/978-3-662-45013-0_15

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