title: Formulation, characterization and clinical evaluation of propranolol hydrochloride gel for transdermal treatment of superficial infantile hemangioma.
abstract: The objective of the present study is to formulate and characterize propranolol hydrochloride (PPL · HCl) gel, and to evaluate the efficacy of this formulation in transdermal treatment for superficial infantile hemangioma (IH). The transdermal PPL · 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 · 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 (Q24, 6027.4 ± 563.1 μg/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 · HCl gel was confirmed by microdialysis technique in rats using the homemade PPL · HCl oral solution as a control. Clinical studies also confirmed the excellent therapeutic response and few side effects of the PPL · HCl gel. These results suggest that transdermal application of the PPL · HCl gel is an effective and safe formulation in treating superficial IH.
authors.affiliation: Department of Pharmaceutics, School of Pharmaceutical Sciences, Central South University , Changsha, Hunan Province , China .
authors.forename: Wenhu
authors.initials: W
authors.lastname: Zhou
authors.forename: Shiying
authors.initials: S
authors.lastname: He
authors.forename: Yijun
authors.initials: Y
authors.lastname: Yang
authors.forename: Dan
authors.initials: D
authors.lastname: Jian
authors.forename: Xiang
authors.initials: X
authors.lastname: Chen
authors.forename: Jinsong
authors.initials: J
authors.lastname: Ding
mesh_terms: D000279:Administration, Cutaneous; D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D000818:Animals; D002626:Chemistry, Pharmaceutical; D002675:Child, Preschool; D004311:Double-Blind Method; D005079:Excipients / Q000737:chemistry; D005260:Female; D006391:Hemangioma / Q000188:drug therapy*; D006801:Humans; D065347:Hypromellose Derivatives / Q000737:chemistry; D007223:Infant; D008297:Male; D010539:Permeability; D011433:Propranolol / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D013552:Swine; D013729:Terpenes / Q000737:chemistry
chemical_list: D000319:Adrenergic beta-Antagonists; D005079:Excipients; D013729:Terpenes; D065347:Hypromellose Derivatives; D011433:Propranolol
keywords: Clinical evaluation; microdialysis; percutaneous permeation; propranolol hydrochloride gel; superficial infantile hemangioma