Benzoyl peroxide: Percutaneous penetration and metabolic disposition

https://doi.org/10.1016/S0190-9622(81)70004-5Get rights and content

The transepidermal penetration and metabolic disposition of 14C-benzoyl peroxide were assessed in vitro (excised human skin) and in vivo (rhesus monkey). In vitro, the benzoyl peroxide penetrated into the skin, through the stratum corneum or the follicular openings, or both, and was recovered on the dermal side as benzoic acid. In vivo, benzoic acid was recovered from urine in amounts equivalent to 45% and 98% of the radiolabel following, respectively, topical and intramuscular administration of small amounts of 14C-benzoyl peroxide. We conclude that benzoyl peroxide penetrates as such into the skin layers and is converted therein to benzoic acid, which, in turn is absorbed into the systemic circulation. Renal clearance of the metabolite is sufficiently rapid as to preclude its hepatic conjugation with glycine, since following topical administration to rhesus monkeys, no hippuric acid was found in the urine, as could have been expected had a significant amount of benzoic acid passed through the liver.

References (11)

There are more references available in the full text version of this article.

Cited by (84)

  • Topical Therapeutics

    2022, A Comprehensive Guide to Hidradenitis Suppurativa
  • Management of dermatological conditions in pregnancy

    2021, Clinical Pharmacology During Pregnancy
  • An update on formulation strategies of benzoyl peroxide in efficient acne therapy with special focus on minimizing undesired effects

    2020, International Journal of Pharmaceutics
    Citation Excerpt :

    This side effect is inextricably linked to its chemical structure and its antibacterial mechanism of action: the formation of reactive oxygen species (Cove and Holland, 1983). After penetration into the stratum corneum, benzoyl peroxide is rapidly degraded to benzoic acid (Seubert et al., 1984) so that no side effects occur in deeper skin layers (Nacht et al., 1981). Symptomatic local irritations are itching, redness and (rarely) swelling as well as increased peeling and dryness of the skin.

  • Topical Antibacterial Agents

    2020, Comprehensive Dermatologic Drug Therapy, Fourth Edition
  • Safety of dermatologic medications in pregnancy and lactation: Part I. Pregnancy

    2014, Journal of the American Academy of Dermatology
    Citation Excerpt :

    It is highly bound to plasma protein (>99%) and maternal plasma concentrations are low, so placental transfer is unlikely. Healthy infants were delivered in several cases of inadvertent exposure.41,100,101 Isotretinoin is absolutely contraindicated in pregnancy because of increased first-trimester pregnancy loss and increased birth defects, such as cleft palate, hydrocephalus, cardiac outflow tract defects, microtia, and external ear canal stenosis.102

View all citing articles on Scopus
View full text