title: Evaluation of a 13-hexyl-berberine hydrochloride topical gel formulation.
abstract: 13-hexyl-berberine hydrochloride (HB-13) is a derivative from berberine which finds widespread applications in the treatment of infectious pathogens including fungi, bacteria, parasites and viruses. As our continuing efforts for treatment of herpes simplex virus (HSV), we studied the topical delivery and safety of HB-13 in a gel formulation (0.5%) in a pig model. Our studies demonstrated the maximal HB-13 concentration was 2.51 µg/mL, which was more than the half maximal inhibitory concentration (IC50) as we previously reported. In addition, there was no sign of irritation or histological aberrance for stripped skin continuously applied with 0.5% HB-13 gel for 21 days. In conclusion, 0.5% HB-13 gel can achieve effective anti-HSV concentration in the dermis and it is safe to use.
authors.affiliation: Institute of Dermatology, Peking Union Medical College, Chinese Academy of Medical Science, Nanjing, People's Republic of China. huilin.wei@gmail.com
authors.forename: Hui Lin
authors.initials: HL
authors.lastname: Wei
authors.forename: Shuqi
authors.initials: S
authors.lastname: Wang
authors.forename: Feng
authors.initials: F
authors.lastname: Xu
authors.forename: Lan Fang
authors.initials: LF
authors.lastname: Xu
authors.forename: Jia Run
authors.initials: JR
authors.lastname: Zheng
authors.forename: Yun
authors.initials: Y
authors.lastname: Chen
mesh_terms: D000287:Administration, Topical; D000818:Animals; D000998:Antiviral Agents / Q000737:chemistry / Q000493:pharmacokinetics* / Q000633:toxicity; D001599:Berberine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D002851:Chromatography, High Pressure Liquid; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D005782:Gels / Q000008:administration & dosage; D006561:Herpes Simplex / Q000188:drug therapy*; D018258:Herpesvirus 2, Human / Q000187:drug effects; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption; D013552:Swine; D014018:Tissue Distribution
chemical_list: C583326:13-hexylberberine; D000998:Antiviral Agents; D005782:Gels; D001599:Berberine