Investigation of Drug Partition Property in Artificial Sebum

    Satyanarayana Valiveti, James A. Wesley, Guang Wei Lu
    From the encyclopedia
    Ketoconazole →

    antifungal with some anti-androgenic benefits, often used as a shampoo

    Minoxidil →

    An essential vasodilator with some anti-androgenic effects

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    Studysummary This study found that the sebum partition coefficient (K(sebum)) for some drugs differs from the stratum corneum partition coefficient (K(sc)), indicating its importance for targeted drug delivery into hair and sebaceous follicles.
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    The study aimed to develop a method for determining the sebum partition coefficient (Ksebum) to predict drug delivery into hair and sebaceous follicles. Researchers measured the partition coefficients of 11 model drugs in artificial sebum/water and human stratum corneum/water at 37°C. They found that Ksebum varied significantly from the stratum corneum/water partition coefficient (Ksc) and the calculated octanol-water partition coefficient (clog P), with some drugs showing higher affinity for sebum. A poor correlation was observed between log Ksebum, log Ksc, and clog P for most compounds, except for a strong linear relationship in the 4-hydroxybenzoate series. Ketoconazole had the highest Ksebum value, suggesting it is more likely to be transported through sebaceous and hair follicles, while minoxidil had a lower value, indicating transport through the stratum corneum. The study concluded that Ksebum is a critical parameter for predicting drug delivery into hair and sebaceous follicles, and it provides more relevant information than traditional partition coefficients. The study involved a small number of samples, with n=6 for Ksebum and n=3 for Ksc.
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