The invention provides methods of delivering pharmacologic agents linked to an internalization peptide, in which an inflammatory response inducible by the internalization peptide is inhibited by co-administration of an anti-inflammatory or by linking the internalization peptide to biotin or similar molecule. Such methods are premised in part on the results described in the examples whereby administration of a pharmacological agent linked to tat at high dosages is closely followed 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.本発明は、内在化ペプチド連結薬理学的薬剤を送達させる方法であって、内在化ペプチド誘導性の炎症反応を抗炎症剤の同時投与、又は内在化ペプチドにビオチン又は類似分子を連結することによって阻害する、方法を提供する。このような方法は、実施例で記載される結果を部分的に前提とし、その実施例では、tatに連結された薬理学的薬剤の高用量での投与に続いて直ぐにマスト細胞脱顆粒、ヒスタミン放出、及びヒスタミン放出の典型的な後遺症（発赤、熱、腫脹、及び低血圧）を含む炎症反応が起きる。
