A new class of terpene and vanilloid anti-inflammatory agents, conjugated to a polyamine backbone, has proven to be highly effective in suppression of chemically-induced inflammation by topical application. While amides of spermidine and spermine are stable under physiological conditions, carbamates of these polyamines proved capable of slowly releasing pharmacologically active phenols conjugated through carbamate linkages. Choice of pH, media polarity, temperature, and structure of the linked pharmaceutical, controlled the rate of appearance of the free drug. Phorbol acetate, chloroethyl ethyl sulfide, and sulfur mustard have been used as the irritants in a rodent model and &gt;85% suppression of erythema/edema has been achieved in an ointment prepared from these polyamine conjugates.

Controlled-release mechanism for sulfur mustard anti-inflammatory drugs based on polyamine platform

249th National Meeting (2015)

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