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Skin Permeation and Disposition of Therapeutic and Cosmeceutical Compounds pp 205–224Cite as

Related Topic: Prodrug Approach

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Abstract

The concept of a “prodrug” (Fig. 17.1) was introduced by Albert in 1958 [1]. A prodrug is defined as a derivative from the parent drug that (1) has no or little pharmacological effect, (2) is enzymatically or chemically converted to the parent drug in body, and (3) improves absorption and/or distribution properties of the parent drug and increases the therapeutic effect. A prodrug is designed through the introduction of a moiety to a drug molecule where the moiety is effectively eliminated from the body after performing a role in recovering the shortcomings of the parent drug or increasing the effect of the parent drug. Three kinds of prodrug properties are found: (1) improvement in stability and increase in aqueous solubility or lipophilicity, (2) improvement of absorption properties and/or residence time in the systemic circulation and target tissues, and (3) modification of a bio-reaction (decrease in side effects, improvement of bad taste and smell, and evasion of the first-pass effect).

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Authors and Affiliations

  1. Josai International University, Togane, Chiba, Japan

    Kenji Sugibayashi (President, Professor)

  2. Graduate School of Pharmaceutical Sciences and Faculty of Pharmacy and Pharmaceutical Sciences, Josai University, Sakado, Saitama, Japan

    Kenji Sugibayashi (President, Professor)

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  1. Kenji Sugibayashi
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Correspondence to Kenji Sugibayashi .

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  1. President, Josai International University, Togane, Chiba, Japan

    Kenji Sugibayashi

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Sugibayashi, K. (2017). Related Topic: Prodrug Approach. In: Sugibayashi, K. (eds) Skin Permeation and Disposition of Therapeutic and Cosmeceutical Compounds. Springer, Tokyo. https://doi.org/10.1007/978-4-431-56526-0_17

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