Experimental study on phototoxicity and the photosensitization potential of ketoprofen, suprofen, tiaprofenic acid and benzophenone and the photocross‐reactivity in guinea pigs

Sugiura, Mariko; Hayakawa, Ritsuko; Xie, Zhenlin; Sugiura, Katsuaki; Hiramoto, Keiichi; Shamoto, Mikihiro

doi:10.1034/j.1600-0781.2002.180205.x

Cited by 38 publications

(32 citation statements)

References 22 publications

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“…Negative phototoxicity was observed in a guinea pig skin phototoxicity study of ketoprofen (Sugiura et al, 2002). Mice given ketoprofen by single oral dosing and irradiated with UV-A did not demonstrate any change due to the phototoxicity (Ljunggren and Lundberg, 1985).…”

Section: Introductionmentioning

confidence: 99%

Phototoxicity Study of a Ketoprofen Poultice in Guinea Pigs

et al. 2005

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-Ketoprofen has been reported to have such side effects as photosensitive dermatitis in humans (The Ministry of Health, Labour and Welfare, 2001). In the present study, as part of a safety evaluation of Miltax ® , an application drug containing ketoprofen, phototoxicity of Miltax ® was examined in guinea pigs.In the present skin phototoxicity study, Miltax ® was applied for 12 hr. Ultraviolet (UV) rays were irradiated to examine whether or not Miltax ® elicited skin reaction. Two kinds of UV-A plus UV-B dual irradiation and UV-A single irradiation were used for the elicitation. With UV-A plus UV-B dual irradiation on the Miltax ® application site, no skin reaction was observed at UV irradiation side in any animals, in contrast to the case of the positive control article, . Similar results were obtained with UV-A single irradiation.From these results, Miltax ® that contained ketoprofen did not show any skin phototoxicity in the guinea pig.

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Section: Introductionmentioning

confidence: 99%

Phototoxicity Study of a Ketoprofen Poultice in Guinea Pigs

et al. 2005

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“…1 In an experimental study, it was found that benzoyl radical is the key structure that provokes photosensitivity and the photo cross-reactivity of KP, suprofen and tiaprofenic acid. 2 As that radical is common in benzophenone ultraviolet (UV) filters, cross-reactions are familiar with sunscreens containing mainly oxybenzone.…”

Section: Ketoprofen ([Rs]2-[3-benzoylphenyl]-propionic Acid) (Kp) Is mentioning

confidence: 99%

Ketoprofen-loaded polymer carriers in bigel formulation: an approach to enhancing drug photostability in topical application forms

Andonova¹,

Peneva²,

Georgiev³

et al. 2017

IJN

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The purpose of the study was to investigate the stability and biopharmaceutical characteristics of ketoprofen, loaded in polymeric carriers, which were included into a bigel in a semisolid dosage form. The polymer carriers with in situ-included ketoprofen were obtained by emulsifier-free emulsion polymerization of the monomers in aqueous medium or a solution of the polymers used. The morphological characteristics of the carriers, the in vitro release and the photochemical stability of ketoprofen were evaluated. The model with optimal characteristics was included in a bigel formulation. The bigel was characterized in terms of pH, rheological behavior, spreadability, and in vitro drug release. Acute skin toxicity, antinociceptive activity, anti-inflammatory activity, and antihyperalgesic effects of the prepared bigel with ketoprofen-loaded polymer carrier were evaluated. The carriers of ketoprofen were characterized by a high yield and drug loading. The particle size distribution varied widely according to the polymer used, and a sustained release was provided for up to 6 hours. The polymer mixture poly(vinyl acetate) and hydroxypropyl cellulose as a drug carrier, alone or included in the bigel composition, improved the photostability of the drug compared with unprotected ketoprofen. The bigel with ketoprofen-loaded particles provided sustained release of the drug and had optimal rheological parameters. In vivo experiments on the bigel showed no skin inflammation or irritation. Four hours after its application, a well-defined analgesic, anti-inflammatory, and antihyperalgesic effect was registered. The polymer mixture of poly(vinyl acetate) and hydroxypropyl cellulose as a carrier of ketoprofen and the bigel in which it was included provided an enhanced photostability and sustained drug release.

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“…Although the free radical species were speculated to be benzophenone, [9][10][11][12] benzoyl radical, 13) carbonyl radical 14) and superoxide anion, 15) their true identities remain unknown to this day. We elucidated the pathways for the photo-degradation of ketoprofen and the generation of free radicals in our previous study.…”

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confidence: 99%