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Nat Med. 2000 Nov;6(11):1253-7.

Conjugation of arginine oligomers to cyclosporin A facilitates topical delivery and inhibition of inflammation.

Author information

1
CellGate, Sunnyvale, California 94086, USA. Khavari@cmgm.stanford.edu

Abstract

Many systemically effective drugs such as cyclosporin A are ineffective topically because of their poor penetration into skin. To surmount this problem, we conjugated a heptamer of arginine to cyclosporin A through a pH-sensitive linker to produce R7-CsA. In contrast to unmodified cyclosporin A, which fails to penetrate skin, topically applied R7-CsA was efficiently transported into cells in mouse and human skin. R7-CsA reached dermal T lymphocytes and inhibited cutaneous inflammation. These data establish a general strategy for enhancing delivery of poorly absorbed drugs across tissue barriers and provide a new topical approach to the treatment of inflammatory skin disorders.

PMID:
11062537
DOI:
10.1038/81359
[Indexed for MEDLINE]
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