Intradermal Concentration of Hydroquinone after Application of Hydroquinone Ointments Is Higher than Its Cytotoxic Concentration

Ointments of the skin depigmentation agent hydroquinone (HQ) have been prepared by extemporaneous nonsterile compounding in our hospital. The HQ ointments were highly effective in the treatment of various types of skin pigmentations; however, various problems have emerged including chromatic aberrat...

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Bibliographic Details
Published in:Biological & Pharmaceutical Bulletin 2003, Vol.26(9), pp.1365-1367
Main Authors: Matsubayashi, Teruhisa, Sakaeda, Toshiyuki, Kita, Tomoko, Kurimoto, Yoshie, Nakamura, Tsutomu, Nishiguchi, Kohshi, Fujita, Takuya, Kamiyama, Fumio, Yamamoto, Akira, Okumura, Katsuhiko
Format: Article
Language:English
Subjects:
Animals
Antioxidants - pharmacology
Ascorbic Acid - pharmacology
Biological and medical sciences
Cell Survival - drug effects
Cells, Cultured
Colorimetry
cytotoxicity
Diffusion
Drug toxicity and drugs side effects treatment
Fibroblasts
hydroquinone
Hydroquinones - administration & dosage
Hydroquinones - pharmacokinetics
Hydroquinones - toxicity
intradermal concentration
Male
Medical sciences
ointment
Ointments
Pharmacology. Drug treatments
Rats
Rats, Wistar
Skin - cytology
Skin - metabolism
Skin Absorption
Sulfates - pharmacology
Toxicity: skin, dermoskeleton
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Summary:Ointments of the skin depigmentation agent hydroquinone (HQ) have been prepared by extemporaneous nonsterile compounding in our hospital. The HQ ointments were highly effective in the treatment of various types of skin pigmentations; however, various problems have emerged including chromatic aberration of the ointments, a relatively large variability of efficacy, and mild topical side effects including irritation. In this paper, the cytotoxicity of HQ was assessed in vitro using rat skin fibroblasts as the concentration with 50% survival after 24 h exposure to be 16.5 μM. The intradermal concentrations at 2 h after application of the HQ ointments was also estimated to be 358 mM and 51.7 mM in stratum corneum and viable tissue (viable epidermis+dermis), respectively, by an in vitro rat skin permeation study with rat full-thickness abdominal skin and Franz-type diffusion cells. It was demonstrated that the intradermal concentration of HQ was much higher than that eliciting cytotoxicity, suggesting that the topical side effects after application of HQ ointment were due to the cytotoxicity of HQ.
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.26.1365