Dermal Pharmacokinetics of Terpinen-4-ol Following Topical Administration of Zingiber cassumunar (plai) Oil

Abstract The purpose of this study was to investigate dermal pharmacokinetics of terpinen-4-ol in rats following topical administration of plai oil derived from the rhizomes of Zingiber cassumunar Roxb. Unbound terpinen-4-ol concentrations in dermal tissue were measured by microdialysis. The dermal pharmacokinetic study of terpinen-4-ol was performed under non-occlusive conditions. The oil was topically applied at a dose of 2, 4, and 8 mg/cm2 plai oil corresponding to the amount of 1.0, 1.9, and 3.8 mg/cm2 terpinen-4-ol, respectively. Following topical application of the oil, terpinen-4-ol rapidly distributed into the dermis and demonstrated linear pharmacokinetics with no changes in the dose-normalized area under the concentration-time curves across the investigated dosage range. The mean percentages of free terpinen-4-ol distributed in the dermis per amount of administered were 0.39 ± 0.06 %, 0.41 ± 0.08 %, and 0.30 ± 0.03 % for 2, 4, and 8 mg/cm2 doses, respectively. The dermal pharmacokinetics of terpinen-4-ol could provide information for its further formulation development and therapy schedules.

[1]  P. Rugthaworn,et al.  Chemical Composition and Physical Properties of Oil from Plai (Zingiber cassumunar Roxb.) Obtained by Hydro Distillation and Hexane Extraction , 2009 .

[2]  S. Haas,et al.  Microdialysis as a tool to determine free kidney levels of voriconazole in rodents: a model to study the technique feasibility for a moderately lipophilic drug. , 2008, Journal of pharmaceutical and biomedical analysis.

[3]  M. Roberts,et al.  Human skin penetration of the major components of Australian tea tree oil applied in its pure form and as a 20% solution in vitro. , 2008, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[4]  U. Fuhr,et al.  Plasma and Tissue Pharmacokinetics of Epirubicin and Paclitaxel in Patients Receiving Neoadjuvant Chemotherapy for Locally Advanced Primary Breast Cancer , 2007, Clinical pharmacology and therapeutics.

[5]  M. Zeitlinger,et al.  Development of a high-performance liquid chromatography method for the determination of caspofungin with amperometric detection and its application to in vitro microdialysis experiments. , 2006, Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.

[6]  J. Reichling,et al.  In vitro studies on release and human skin permeation of Australian tea tree oil (TTO) from topical formulations. , 2006, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[7]  K. Cal,et al.  Stratum corneum absorption and retention of linalool and terpinen-4-ol applied as gel or oily solution in humans. , 2006, Journal of dermatological science.

[8]  K. Cal,et al.  Effect of physicochemical properties of cyclic terpenes on their ex vivo skin absorption and elimination kinetics. , 2006, Journal of dermatological science.

[9]  K. Cal.  Skin Penetration of Terpenes from Essential Oils and Topical Vehicles , 2006, Planta medica.

[10]  F. Nielsen,et al.  Topical use of tea tree oil reduces the dermal absorption of benzoic acid and methiocarb , 2006, Archives of Dermatological Research.

[11]  A. Ahuja,et al.  A validated HPTLC method for determination of tea tree oil from cosmeceutical formulations. , 2005, Journal of pharmaceutical and biomedical analysis.

[12]  K. Cal.  How does the type of vehicle influence the in vitro skin absorption and elimination kinetics of terpenes? , 2005, Archives of Dermatological Research.

[13]  K. Ward,et al.  Enhancement of in vitro and in vivo microdialysis recovery of SB‐265123 using Intralipid® and Encapsin® as perfusates , 2003, Biopharmaceutics & drug disposition.

[14]  T. Tomson,et al.  Microdialysis sampling of carbamazepine, phenytoin and phenobarbital in subcutaneous extracellular fluid and subdural cerebrospinal fluid in humans: an in vitro and in vivo study of adsorption to the sampling device. , 2002, Pharmacology & toxicology.

[15]  Kwang-Hyeon Liu,et al.  Dermal Pharmacokinetics of Furathiocarb in Rats , 2000 .

[16]  E. Benfeldt.  In vivo microdialysis for the investigation of drug levels in the dermis and the effect of barrier perturbation on cutaneous drug penetration. Studies in hairless rats and human subjects. , 1999, Acta dermato-venereologica. Supplementum.

[17]  A. Jørgensen,et al.  In vitro microdialysis of hydrophilic and lipophilic compounds , 1997 .

[18]  L. Groth.  Cutaneous microdialysis. Methodology and validation. , 1996, Acta dermato-venereologica. Supplementum.

[19]  G. S. Hawkins,et al.  Percutaneous penetration and skin retention of topically applied compounds: an in vitro-in vivo study. , 1991, Journal of pharmaceutical sciences.

[20]  U. Ungerstedt,et al.  A comparison between three methods for estimation of extracellular concentrations of exogenous and endogenous compounds by microdialysis. , 1991, Journal of pharmacological methods.

[21]  C. Anderson,et al.  Ethanol absorption across human skin measured by in vivo microdialysis technique. , 1991, Acta dermato-venereologica.

[22]  B. Kemppainen,et al.  Methods for Skin Absorption , 1990 .