The invention provides methods of delivering pharmacologic agents linked toan internalization peptide, in which an inflammatory response inducible bythe internalization peptide is inhibited by co-administration of an anti-inflammatoryor by linking the internalization peptide to biotin or similar molecule. Suchmethods are premised in part on the results described in the examples wherebyadministration of a pharmacological agent linked to tat at high dosages is closelyfollowed by an inflammatory response, which includes mast cell degranulation,histamine release and the typical sequelae of histamine release, such as redness,heat, swelling, and hypotension.