In vivo assessment of enhanced topical delivery of terbinafine to human stratum corneum.

@article{Alberti2001InVA,
  title={In vivo assessment of enhanced topical delivery of terbinafine to human stratum corneum.},
  author={Ingo Alberti and Yogeshvar N. Kalia and Aarti Naik and J. D. Bonny and Richard H. Guy},
  journal={Journal of controlled release : official journal of the Controlled Release Society},
  year={2001},
  volume={71 3},
  pages={
          319-27
        }
}
  • I. Alberti, Y. Kalia, +2 authors R. Guy
  • Published 28 April 2001
  • Chemistry, Medicine
  • Journal of controlled release : official journal of the Controlled Release Society
PURPOSE The objective of this study was to evaluate, using attenuated total reflectance Fourier transform infrared spectroscopy, the stratum corneum (SC) bioavailability of terbinafine (TBF) following topical treatment with four different formulations. METHODS Four skin sites on the ventral forearms of five healthy volunteers were treated for 2 h using one of four formulations based on a vehicle consisting of 50% ethanol and 50% isopropyl myristate. Three of these formulations included a… 
Noninvasive Characterization of Regional Variation in Drug Transport into Human Stratum Corneum in Vivo
TLDR
Investigation of the mechanisms underlying the regional variations in drug transport into human stratum corneum of two model compounds of different lipophilicity and molecular size by non-invasive, quantitative attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy found regional variation in permeability coefficients was mainly influenced by its intrinsic diffusivity across the SC.
Dermatopharmacokinetic prediction of topical drug bioavailability in vivo.
TLDR
Prediction and experiment agreed satisfactorily suggesting that objective and quantitative information, with which to characterize topical drug bioavailability, can be obtained from this approach.
Transdermal iontophoretic delivery of terbinafine hydrochloride: quantitation of drug levels in stratum corneum and underlying skin.
TLDR
Iontophoresis enhanced the delivery of terbinafine hydrochloride into the skin layers and, therefore, may be used to improve the treatment of skin fungal infections.
Evaluation of liposomal and conventional formulations of octyl methoxycinnamate on human percutaneous absorption using the stripping method.
TLDR
The result of this study indicates that an MLV prepared by the fusion method could be a better vehicle for OMC as a sunscreen since it has a slightly better SPF compared to a conventional formulation and more remains in the stratum corneum, reducing its penetration to the deeper layers.
Dermatopharmacokinetics: Factors Influencing Drug Clearance from the Stratum Corneum
TLDR
The important role of formulation excipients in topical delivery is demonstrated, and the local disposition of cosolvents within the SC may impact significantly on drug dermatopharmacokinetics and local bioavailability.
Novel Imaging Method to Quantify Stratum Corneum in Dermatopharmacokinetic Studies: Proof-of-Concept with Acyclovir Formulations
TLDR
The new imaging approach offers a sensitive, reproducible, precise, and rapid technique to quantify the relative SC amount removed on tape-strips, and facilitates the acquisition of DPK data.
FT-IR investigation of Terbinafine interaction with stratum Corneum constituents.
TLDR
Interaction of Tbf with the SC induced substantial β-sheet formation in the keratin, an effect which was partially reversed both by ethanol washing and by exposure to high relative humidity, suggesting the presence of a Tbf reservoir.
Assessment of Topical Bioequivalence Using Dermal Microdialysis and Tape Stripping Methods
TLDR
The test was found to be bioequivalent to reference according to the dermatopharmacokinetic evaluation by tape stripping, and no significant correlations were found between microdialysis and tape stripping methods as regarding the topical bioequivalence of oxytetracycline HCl formulations.
Effect of propylene glycol on ibuprofen absorption into human skin in vivo.
TLDR
Tape-stripping experiments can reveal details of a drug's bioavailability in the skin following topical application and may be used to probe the mechanism(s) by which certain excipients influence local drug delivery.
Dermatopharmocokinetics: An approach to evaluate topical drug bioavailability
TLDR
In this preliminary study, betamethasone valerate was formulated into simple adhesive patches, the removal of which should unambiguously avoid any potential artefacts, but patch adhesion in vitro; and in limited in vivo experiments, was substantial such that a significant fraction of SC was removed with the patch.
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 14 REFERENCES
Mechanism of oleic acid-induced skin penetration enhancement in vivo in humans
Abstract The outermost layer of mammalian skin, the stratum corneum (SC), by virtue of its unique architecture, presents a significant barrier to the transdermal delivery of drugs. Penetration
Drug and vehicle deposition from topical applications: localization of minoxidil within skin strata of the hairless mouse.
TLDR
Questions are raised about the use of in vitro tissue dispositions for bioavailability assessment and bioequivalence demonstration after the cutaneous bioavailability of topical 2% minoxidil solution was verified in live hairless mice.
Characterization of the permeability barrier of human skin in vivo.
TLDR
The technology lends itself both to the prediction of transdermal drug delivery, and the feasibility of this route of administration, and to the assessment of risk after dermal contact with toxic chemicals.
Homogeneous transport in a heterogeneous membrane: water diffusion across human stratum corneum in vivo.
TLDR
Skin impedance (low frequency) was correlated with the relative concentration of water within the SC, thus providing an in vivo probe for skin hydration, and the SC permeability coefficient to water, as a function of SC thickness, was calculated and correlation with the corresponding values of skin admittance derived from IS.
Estimation of a concentration profile of acyclovir in the skin after topical administration
Abstract The Laplace transformed equations for the time courses of drug concentration in the skin and net absorption were derived from Fick's diffusion law assuming a two-layer skin model. Based on
Penetration enhancers for human skin: mode of action of 2-pyrrolidone and dimethylformamide on partition and diffusion of model compounds water, n-alcohols, and caffeine.
TLDR
It is concluded that for polar methanol, nonpolar octanol, and an intermediate compound, caffeine, the markedly increased absorption caused by dimethylformamide is associated with damage to the membrane and 2-pyrrolidone enhances permeation through the polar route of the skin by increasing the diffusivity and partitioning.
Availability of isoconazole in human skin after dermal application as free base and as nitrate in vitro.
  • U. Täuber
  • Chemistry, Medicine
    Arzneimittel-Forschung
  • 1987
TLDR
A 10-fold increase in the concentration of antimycotic has been observed in the viable epidermis and dermis after the application of isoconazole free base in ethanol/propylene glycol.
The enhancement index concept applied to terpene penetration enhancers for human skin and model lipophilic (oestradiol) and hydrophilic (5-fluorouracil) drugs
A series of cyclic monoterpenes has been assessed as skin penetration enhancers towards a model lipophilic drug, oestradiol. In vitro permeation experiments on human epidermal membranes showed that
Terbinafine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in superficial mycoses.
TLDR
Although further research is required to establish the efficacy of terbinafine in comparison with other available therapies, as well as to fully clarify its tolerability profile, the early results obtained with terbINAfine in superficial fungal infections are very encouraging.
Comparison of permeability data from traditional diffusion cells and ATR-FTIR spectroscopy. Part II. Determination of diffusional pathlengths in synthetic membranes and human stratum corneum
Abstract In this study, the morphological structure of the inner and outer regions of human stratum corneum (SC) were investigated using Attenuated Total Reflectance Fourier Transform Infra-Red
...
1
2
...