title: In vitro and in vivo evaluations of topically applied capsaicin and nonivamide from hydrogels.
abstract: The purpose of this study was designed to investigate the in vitro and in vivo skin absorption of capsaicin and nonivamide from hydrogels. Various commercialized creams of capsaicin were also compared with hydrogels. Both skin stripping technique and Mexameter were applied to evaluate the level of capsaicin and nonivamide retained in stratum corneum (SC) and skin erythema in vivo. The partition of drug between skin and the hydrogel matrix was considered to play an important role in the permeation process. The in vitro permeation of capsaicin from hydrogels depends on the physicochemical nature and the concentration of the polymer used. The incorporation of nonionic Pluronic F-127 polymer into hydrogels resulted in a retarded release of capsaicin. On the other hand, the in vitro capsaicin permeation showed higher levels in cationic chitosan and anionic carboxymethyl cellulose (CMC) hydrogels than cream bases. The permeation of nonivamide was retarded at the late stage of in vitro application. The inter-subject variation was more significant in the in vivo study than in vitro skin permeation experiments. The cream induced in vivo skin erythema depending on the drug concentration, however, the dose-dependence was not observed in hydrogels. Nonivamide-treated skin showed stronger erythema than capsaicin-treated skin. The present study indicates that there is a moderate correlation between in vitro skin permeation and in vivo erythema responses of topically applied capsaicin and nonivamide. The correlation between drug amount in SC and skin erythema test in vivo was also observed.
authors.affiliation: Graduate Institute of Pharmaceutical Sciences, Taipei Medical University, 250 Wu-Hsing Street, Taipei, Taiwan, ROC.
authors.forename: Y Y
authors.initials: YY
authors.lastname: Wang
authors.forename: C T
authors.initials: CT
authors.lastname: Hong
authors.forename: W T
authors.initials: WT
authors.lastname: Chiu
authors.forename: J Y
authors.initials: JY
authors.lastname: Fang
mesh_terms: D000287:Administration, Topical; D000818:Animals; D002211:Capsaicin / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000493:pharmacokinetics*; D004791:Enzyme Inhibitors / Q000493:pharmacokinetics; D004817:Epidermis / Q000378:metabolism; D004890:Erythema / Q000139:chemically induced; D006801:Humans; D020100:Hydrogels / Q000737:chemistry* / Q000493:pharmacokinetics; D051379:Mice; D008819:Mice, Nude; D009824:Ointments; D012869:Skin Absorption; D013997:Time Factors; D014783:Viscosity
chemical_list: D004791:Enzyme Inhibitors; D020100:Hydrogels; D009824:Ointments; D002211:Capsaicin; C040937:nonivamide