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An attempt to reduce the photosensitizing potential of chlorpromazine with the simultaneous use of β- and dimethyl-β-cyclodextrins in guinea pigs

✍ Scribed by T. Hoshino; K. Ishida; T. Irie; K. Uekama; T. Ono


Publisher
Springer-Verlag
Year
1989
Tongue
English
Weight
541 KB
Volume
281
Category
Article
ISSN
0340-3696

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✦ Synopsis


The effects of topically applied fleyclodextrin (fl-CyD) and heptakis(2,6-di-O-methyl)fl-cyclodextrin (DM-fl-CyD) on photoallergic contact dermatitis due to chiorpromazine hydrochloride (CPZ) were investigated using the photomaximization technique in guinea pigs. From the gross and histological observations, the photosensitizing potential of CPZ with the simultaneous topical use of fl-CyDs was significantly lower than that of CPZ alone. The alleviating efficacy of DM-fl-CyD was greater than that of fl-CyD, fl-CyDs suppressed the penetration of CPZ into the skin through the formation of poorly skin-permeable complexes. In addition, fl-CyDs inhibited (a) the photoinduced free radicals derived from CPZ in the isolated dry skin and (b) the in vitro photochemical binding of CPZ to bovine serum albumin. These observations suggest that fl-CyDs suppress the photochemical reactions between CPZ and biological macromolecules present in the skin, resulting in the failure to form a photoantigen. The present results indicate that DM-fl-CyD is particularly effective in alleviating photoallergic contact dermatitis due to CPZ.