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Conjugation of arginine oligomers to cyclosporin A facilitates topical delivery and inhibition of inflammation
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DOI：10.1038/81359.png)
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Abstract
En 中文
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.
Keywords:
EPIDERMAL PERMEABILITY BARRIER
ALLERGIC CONTACT-DERMATITIS
ATOPIC-DERMATITIS
DRUG-DELIVERY
ALOPECIA-AREATA
DOUBLE-BLIND
PSORIASIS
EFFICACY
SKIN
PROTEINS
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