Promethazine hydrochloride (PMZ), an antihistaminic drug, was shown to be cytotoxic in vitroand in vivo at concentrations of 10-4 molar or greaterregardless of pH. A controlled-releasemicroencapsulated formulation was developed thateliminated leukocyte infiltration (irritation) in the nasalepithelium at PMZ concentrations greater than the invitro cytotoxic limit. Alleviation of cytotoxicity couldresult from controlled release and acceleratedabsorption of PMZ.
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