Formulation, characterization and clinical evaluation of propranolol hydrochloride gel for transdermal treatment of superficial infantile hemangioma

The objective of the present study is to formulate and characterize propranolol hydrochloride (PPL center dot HCl) gel, and to evaluate the efficacy of this formulation in transdermal treatment for superficial infantile hemangioma (IH). The transdermal PPL center dot HCl gel was prepared by a direct swelling method, which chose hydroxypropyl methylcellulose (HPMC) as the matrix and used terpenes plus alcohols as permeation enhancer. Permeation studies of PPL center dot HCl were carried out with modified Franz diffusion cells through piglet skin. Our results pointed to that among all studied permeation enhancers, farnesol plus isopropanol was the most effective combination (Q(24), 6027.4 +/- 563.1 mu g/cm(2), ER, 6.8), which was significantly higher than that of control gel (p < 0.05). High percutaneous penetration with related lower plasma drug level of PPL center dot HCl gel was confirmed by microdialysis technique in rats using the homemade PPL center dot HCl oral solution as a control. Clinical studies also confirmed the excellent therapeutic response and few side effects of the PPL center dot HCl gel. These results suggest that transdermal application of the PPL center dot HCl gel is an effective and safe formulation in treating superficial IH.