Cutaneous Absorption and Urinary Excretion of 6-&lt;sup&gt;1&lt;/sup&gt;&lt;sup&gt;4&lt;/sup&gt;C-5-Fluorouracil Ointment Applicated in an Ointment to Healthy and Diseased Human Skin

Erlanger, M; Martz, G; Ott, F. G.; Storck, H; Rieder, Josef

doi:10.1159/000252588

Cited by 34 publications

(7 citation statements)

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“…Shani et al (1985), who measured the penetration of electrolytes through the skin of healthy and psoriatic patients who had bathed in the Dead Sea, found significant increases in the levels of serum Br, Rb, Ca, Zn only in the psoriatic group. Erlanger et al (1970) observed a 15-to 20-fold-increased penetration of 5-fluorouracil ointment on psoriatic patient skin compared with healthy skin. Anigbogu et al (1996), in an in vitro study, found a greater than 2-fold increase in the equilibrium uptake of 8-methoxypsoralen in psoriatic skin compared with normal skin.…”

Section: Psoriasismentioning

confidence: 84%

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Percutaneous absorption in diseased skin: an overview

Chiang¹,

Tudela²,

Maibach³

2012

J of Applied Toxicology

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The stratum corneum's (SC) functions include protection from external hazardous environments, prevention of water loss and regulation of body temperature. While intact skin absorption studies are abundant, studies on compromised skin permeability are less common, although products are often used to treat affected skin. We reviewed literature on percutaneous absorption through abnormal skin models. Tape stripping is used to disrupt water barrier function. Studies demonstrated that physicochemical properties influence the stripping effect: water-soluble drugs are more affected. Abrasion did not affect absorption as much. Freezing is commonly used to preserve skin. It does not seem to modify water absorption, but still increases the penetration of compounds. Comparatively, heating the skin consistently increased percutaneous absorption. Removing SC lipids may increase percutaneous absorption of drugs. Many organic solvents are employed to delipidize. Delipidization with chloroform-methanol increased hydrophilic compound permeability, but not lipophilic. Acetone pre-treatment enhanced hydrophilic compound penetration. More data is needed to determine influence on highly lipophilic compound penetration. Sodium lauryl sulfate (SLS) induces irritant dermatitis and is frequently used as a model. Studies revealed that SLS increases hydrophilic compound absorption, but not lipophilic. However, skin irritation with other chemicals increases lipophilic penetration as much as hydrophilic. Animal studies show that UV exposure increases percutaneous absorption whereas human studies do not. Human studies show increased penetration in psoriatic and atopic dermatitis skin. The data summarized here begin to characterize flux alteration associated with damaged skin. Understanding the degree of alteration requires interpretation of involved conditions and the enlarging of our database to a more complete physicochemical spectrum.

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Section: Psoriasismentioning

confidence: 84%

“…Erlanger et al . () observed a 15‐ to 20‐fold‐increased penetration of 5‐fluorouracil ointment on psoriatic patient skin compared with healthy skin. Anigbogu et al .…”

Section: Diseased Skinmentioning

confidence: 99%

Percutaneous absorption in diseased skin: an overview

Chiang¹,

Tudela²,

Maibach³

2012

J of Applied Toxicology

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“…Indeed, several compounds permeate in higher amounts across (experimental) diseased skin as compared to normal skin [17][18][19][20][21][22][23]. A clinical microdialysis study showed that ALA penetrates faster and in higher amounts through BCCs in patients than through normal skin from healthy volunteers [23].…”

Section: Introductionmentioning

confidence: 99%

Chronic UVB exposure enhances in vitro percutaneous penetration of 5‐aminulevulinic acid in hairless mouse skin

et al. 2004

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“…A study comparing the 0.5 and 5% creams revealed lower levels of systemic absorption in the 0.5% arm compared to the 5% arm [6]. While studies testing its systemic absorption after application to mucosal surfaces are lacking, its absorption has been demonstrated to be increased 15-75 times when applied to diseased or ulcerated skin [7], which may more closely estimate its absorption through mucocutaneous surfaces.…”

Section: Topical 5-fluorouracilmentioning

confidence: 99%

Topical Antineoplastic Agents in the Treatment of Mucocutaneous Diseases

Grossberg

Gaspari

2011

Topical Applications and the Mucosa

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Topical antineoplastic agents have a well-established role in the treatment of several dermatological conditions. Their use in the treatment of mucosal skin disease also has gained increasing recognition. Topical 5-fluorouracil (5-FU), an antimetabolite, and imiquimod, an immunomodulatory agent with antitumor properties, are the two principal topical antineoplastic agents used in the treatment of mucocutaneous diseases. Although the vast majority of their mucosal uses are currently not approved by the Federal Drug Administration, there are numerous case series, open-label studies and randomized controlled trials supporting their uses in the treatment of mucocutaneous diseases. Both topical 5-FU and imiquimod have been successfully utilized in the treatment of a wide range of mucosal diseases, including actinic cheilitis, Bowen's disease of the anal and vulvar mucosa, and genital and perianal condyloma. Reports of their uses in the treatment of mucocutaneous diseases indicate that these agents can be safely administered, though adverse effects such as local inflammation may be augmented when these agents are applied to mucosal surfaces. Additionally, locally acting intralesional chemotherapeutic agents, such as bleomycin and interferon, have well-defined applications in the treatment of mucosal skin diseases such as condyloma acuminata. As further studies are conducted, these topical and intralesional neoplastic agents, in addition to emerging agents that are in various stages of development, such as Toll-like receptor 9 agonists and ingenol mebutate, may play an increasingly important role in the future treatment of mucocutaneous diseases.

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Cutaneous Absorption and Urinary Excretion of 6-<sup>1</sup><sup>4</sup>C-5-Fluorouracil Ointment Applicated in an Ointment to Healthy and Diseased Human Skin

Cited by 34 publications

References 1 publication

Percutaneous absorption in diseased skin: an overview

Percutaneous absorption in diseased skin: an overview

Chronic UVB exposure enhances in vitro percutaneous penetration of 5‐aminulevulinic acid in hairless mouse skin

Topical Antineoplastic Agents in the Treatment of Mucocutaneous Diseases

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