Vehicle effect on topical drug delivery. III. Effect of Azone on the cutaneous permeation of metronidazole and propylene glycol

Wotton, Paul K.; Möllgaard, Birgitte; Hadgraft, Jonathan; Hoelgaard, Annie

doi:10.1016/0378-5173(85)90141-3

Cited by 108 publications

(18 citation statements)

References 4 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…This is surprising as previous work has shown that formulation components clearly influence drug permeation [1][2][3] . Previously, we have investigated the influence of binary and ternary systems of hydrophilic solvents [water, ethanol and propylene glycol (PG)] on ibuprofen transport in silicone membranes and in skin [4,5] .…”

Section: Introductioncontrasting

confidence: 39%

Optimisation of Cosolvent Concentration for Topical Drug Delivery III – Influence of Lipophilic Vehicles on Ibuprofen Permeation

Watkinson¹,

Guy²,

Oliveira³

et al. 2010

Skin Pharmacol Physiol

View full text Add to dashboard Cite

Previously, we have reported the effects of water, ethanol, propylene glycol and various binary and ternary mixtures of these solvents on the permeation of ibuprofen in model membranes and in skin. The present study investigates the influence of lipophilic vehicles on the transport of ibuprofen in silicone membrane and in human skin. The permeation of ibuprofen was measured from mineral oil (MO), Miglyol® 812 (MG) and binary mixtures of MO and MG. The solubility of ibuprofen was 5-fold higher in MG than in MO, however, the permeation of ibuprofen from the pure vehicles and combinations of both was comparable in silicone membrane. Additionally, there were no significant differences in skin permeation for MO and MG vehicles. When the permeation of various hydrophilic and lipophilic vehicles is considered, a trend between flux values for the model membrane and skin is evident (r² = 0.71). The findings suggest that silicone membrane may provide information on qualitative trends in skin permeation for vehicles of diverse solubility and partition characteristics.

show abstract

Section: Introductioncontrasting

confidence: 39%

Optimisation of Cosolvent Concentration for Topical Drug Delivery III – Influence of Lipophilic Vehicles on Ibuprofen Permeation

Watkinson¹,

Guy²,

Oliveira³

et al. 2010

Skin Pharmacol Physiol

View full text Add to dashboard Cite

show abstract

“…The retardation of DEET in presence of laurocapram-PEG 400 was presumably due to the fact that laurocapram-PEG 400 prevented the partitioning of DEET into the skin resulting in reduced permeation. Wotton et al made a similar observation, a test solution of 1% laurocapram and 18% PEG 400 decreased the permeation of metronidazole across the SC (50).…”

Section: Dscmentioning

confidence: 67%

Percutaneous Penetration Modifiers and Formulation Effects: Thermal and Spectral Analyses

Kaushik

Michniak‐Kohn

2010

AAPS PharmSciTech

View full text Add to dashboard Cite

Abstract. The study investigated the formulation effects of laurocapram and iminosulfurane derived penetration modifiers on human stratum corneum using thermal and spectral analyses. Firstly, formulations of penetration modifiers were assessed as enhancers/retardants using the model permeant, diethyl-m-toluamide followed by investigation of their mechanisms of action using differential scanning calorimetry (DSC) and attenuated total reflectance Fourier-transform infra-red spectroscopy. The penetration modifiers investigated were laurocapram, 3-dodecanoyloxazolidin-2-one (N-0915), S,Sdimethyl-N-(4-bromobenzoyl) iminosulfurane (DMBIS), S,S-dimethyl-N-(2-methoxycarbonylbenzenesulfonyl) iminosulfurane (DMMCBI) and tert-butyl 1-dodecyl-2-oxoazepan-3-yl-carbamate (TBDOC) that were formulated in either water, propylene glycol (PG), ethanol or polyethylene glycol 400 (PEG 400). The results explain the mechanism for the first time why an enhancer can become a retardant or vice versa depending upon the vehicle in which it is applied to the skin. DSC indicated that penetration modifier formulations enhanced permeation of active mainly by disruption and fluidization of the stratum corneum lipid bilayers while IR data indicated characteristic blue shifts with decreases in peak intensity. On the other hand, DSC of penetration modifier formulations showing retardation depicted elevated T m2 with a strengthening of lipid-protein complex while IR results indicated formation of multiple peaks around 1,738 cm −1 transition in stratum corneum spectra suggesting retardation may be caused by organization of SC lipids by increased H-bonding.

show abstract

“…The two classes of penetration enhancers, solvent type and lipid fluidizer type, can be combined to reach synergistic effects [6]. In complex formulations, each component can act in different ways.…”

Section: Discussionmentioning

confidence: 99%

Penetration Enhancers Assessed by Corneoxenometry

Goffin¹,

Henry²,

Piérard-Franchimont³

et al. 2000

Skin Pharmacol Physiol

View full text Add to dashboard Cite

Chemical enhancers abating the barrier function of the stratum corneum act in a number of ways. Their relative effects in mixtures are notoriously difficult to determine. Corneoxenometry is a bioassay where xenobiotic interactions with corneocytes are assessed using reflectance colorimetry. It was used to evaluate comparatively the effects of ethanol and laurocapram at various dilutions. In addition, a 10% propylene-glycol-based gel supplemented with N-acetyl-L-cysteine, urea and salicylic acid in various concentrations was tested. The relative index or irritancy (RII) was calculated for each formulation. RII is a surrogate marker of lipid removal and disorganization, and of protein denaturation in the stratum corneum. It is likely a good predictor for barrier function alterations and represents a cheap and rapid alternative to animal testing.

show abstract

Vehicle effect on topical drug delivery. III. Effect of Azone on the cutaneous permeation of metronidazole and propylene glycol

Cited by 108 publications

References 4 publications

Optimisation of Cosolvent Concentration for Topical Drug Delivery III – Influence of Lipophilic Vehicles on Ibuprofen Permeation

Optimisation of Cosolvent Concentration for Topical Drug Delivery III – Influence of Lipophilic Vehicles on Ibuprofen Permeation

Percutaneous Penetration Modifiers and Formulation Effects: Thermal and Spectral Analyses

Penetration Enhancers Assessed by Corneoxenometry

Contact Info

Product

Resources

About