Percutaneous absorption of ibuprofen: Vehicle effects on transport through rat skin

Irwin, W. J.; Sanderson, Francis D.; Po, A. Li Wan

doi:10.1016/0378-5173(90)90399-o

Cited by 26 publications

(7 citation statements)

References 15 publications

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“…Example of penetration modifiers which act via altering the solubility of the permeant in the skin are diethylene glycol monoethyl ether (Transcutol ® : Gattefossé, Saint‐Priest, France) and propylene glycol. Conversely, oleic acid and laurocapram (Azone ® : Nelson Research Inc., Irvine, CA, USA) are known examples of penetration modifiers that migrate into intercellular lipid bilayers and alter the order of the lipid packing [27–29].…”

Section: The Effect Of the Vehicle On Dermal And Transdermal Deliverymentioning

confidence: 99%

Formulation effects of topical emulsions on transdermal and dermal delivery

Otto

Plessis

Wiechers³

2009

Intern J of Cosmetic Sci

189

109

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SynopsisIt has been recognized that the vehicle in which a permeant is applied to the skin has a distinctive effect on the dermal and transdermal delivery of active ingredients. The cutaneous and percutaneous absorptions can be enhanced, e.g. by an increase in thermodynamic activity, supersaturation and penetration modifiers. Furthermore, dermal and transdermal delivery can be influenced by the interactions that may occur between the vehicle and the skin on the one hand, and interactions between the active ingredient and the skin on the other hand. Emulsions are widely used as cosmetic and pharmaceutical formulations because of their excellent solubilizing capacities for lipophilic and hydrophilic active ingredients and application acceptability. This review focuses, in particular, on the effect of emulsions on the dermal and transdermal delivery of active ingredients. It is shown that the type of emulsion (w/o vs. o/w emulsion), the droplet size, the emollient, the emulsifier as well as the surfactant organization (micelles, lyotropic liquid crystals) in the emulsion may affect the cutaneous and percutaneous absorption. Examples substantiate the fact that emulsion constituents such as emollients and emulsifiers should be selected carefully for optimal efficiency of the formulation. Moreover, to understand the influence of emulsion on dermal and transdermal delivery, the physicochemical properties of the formulation after application are considered. Ré suméOn sait que le véhicule dans lequel un perméat est appliqué sur la peau a un effet spécifique sur la libération dermique et transdermique des ingrédients actifs. Les absorptions cutanées et percutanées peuvent être augmentées, par exemple par une augmentation de l'activité thermodynamique, une super saturation ou la présence de modificateurs de pénétration. Ainsi, la libération dermique et transdermique peut être influencée par les interactions susceptibles de s'établir d'un côté entre le véhicule et la peau et de l'autre entre l'ingrédient actif et la peau. Les émulsions sont largement utilisées dans les formulations cosmétiques et pharmaceutiques du fait de leurs excellentes capacités de solubilisation des ingrédients actifs lipophiles et hydrophiles, et du fait de leur bonne tolérance. Cette revue traite, en particulier, des effets des émulsions sur la libération dermique et trans-dermique d'ingrédients actifs. On montre que le type d'émulsion (E/H par rapport à H/E), la granulomé-trie, l'émollient, les émulsifiants, autant que l'organisation des tensioactifs (micelles, cristaux liquides lyotropes) peuvent influencer l'absorption cutanée et percutanée. Des exemples justifient le fait qu'un choix soigné des constituants de l'émulsion comme les émollients et les émulsifiants peut optimiser l'efficacité de la formulation. En complément, pour comprendre l'influence de l'émulsion sur la libéra-tion dermique et transdermique, les propriétés physico-chimiques de la formulation après application sont étudiées.The effect of the vehicle on dermal and transdermal deli...

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Section: The Effect Of the Vehicle On Dermal And Transdermal Deliverymentioning

confidence: 99%

Formulation effects of topical emulsions on transdermal and dermal delivery

Otto

Plessis

Wiechers³

2009

Intern J of Cosmetic Sci

189

109

View full text Add to dashboard Cite

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“…Device‐free transdermal drug delivery technologies have been developed with a goal to improve the utility of this mode of drug delivery to a broader class of drugs. These chemical enhancer technologies including vesicular‐based approaches including liposomes, niosomes, transferosomes, and the creation of nanoparticles from conventional formulation components have had some success …”

Section: Introductionmentioning

confidence: 99%

“…These chemical enhancer technologies including vesicular-based approaches including liposomes, niosomes, transferosomes, and the creation of nanoparticles from conventional formulation components have had some success. [5][6][7][8][9][10][11][12][13][14][15][16] Other approaches for enhanced transdermal drug delivery have used combinations of dermal penetration enhancers (PEs) including fatty acids or solvents to improve the diffusion coefficient, 2,4,17,18 as well as other substances including vasomodulators as possible enhancers of transdermal drug delivery to modulate blood flow in the localized skin tissue. [19][20][21] Those studies, focused on the effect of a vasodilator on iontophoretic delivery of lidocaine, concluded that the coadministration of a vasodilator facilitated the clearing of the drug from the skin tissue, presumably into the bloodstream.…”

Section: Introductionmentioning

confidence: 99%

Vasomodulation Influences on the Transdermal Delivery of Ibuprofen

Carter

Zhu

Váradi

et al. 2013

Journal of Pharmaceutical Sciences

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“…Co-solvents have been widely used both as the vehicle as well as the penetration enhancer in the formulation of vehicles for topical drugs (Chiang et a1 1989;Irwin et al 1990;Liu et a1 1992). In addition to regulating the ionization processes of the drugs, co-solvents may alter the barrier properties which in turn modify the transport profile.…”

mentioning

confidence: 99%

Studies on the In-vitro Percutaneous Penetration of Indomethacin from Gel Systems in Hairless Mice

Liu

Hsieh

et al. 1995

Journal of Pharmacy and Pharmacology

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The influence of co-solvents on the in-vitro percutaneous penetration of indomethacin from gel systems was studied using a simplex lattice experimental design. Gel formulations were prepared by gelling the vehicle mixture of water, either alcohol or isopropanol and either propylene glycol or PEG 400 with 1% w/w Carbomer 940. Hairless mouse skin was employed as the barrier in a Franz-type diffusion cell. The penetration rates at steady state for seven formulations were fitted to a polynomial equation based on this simple lattice method and a three-dimensional plot was constructed. The formulation having the maximal penetration rate was determined to be the vehicle with a solvent ratio of water: alcohol: propylene glycol equal to 15:33:52, and which possessed a solubility parameter of 15 and a drug solubility of around 10 mg mL-1. When the solubility parameter of the vehicle was > 15, the drug solubility increased. However, the penetration rate decreased with an increasing solubility parameter. For those vehicles with a solubility parameter < 15, both the drug solubility and the penetration rate decreased with a decrease in the solubility parameter. There was shown to be an approximately 20-fold increase in the relative enhancement factor when using both alcohol and isopropanol, but only a threefold increase for both propylene glycol and PEG 400, when compared with water.

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Percutaneous absorption of ibuprofen: Vehicle effects on transport through rat skin

Cited by 26 publications

References 15 publications

Formulation effects of topical emulsions on transdermal and dermal delivery

Formulation effects of topical emulsions on transdermal and dermal delivery

Vasomodulation Influences on the Transdermal Delivery of Ibuprofen

Studies on the In-vitro Percutaneous Penetration of Indomethacin from Gel Systems in Hairless Mice

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