Vehicle Effects on the In Vitro Penetration of Testosterone through Equine Skin

Mills, Paul C.

doi:10.1007/s11259-006-3446-6

Cited by 11 publications

(10 citation statements)

References 27 publications

(27 reference statements)

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“…Although there are many reports demonstrating that alcohols may act as skin permeability enhancers as solubilizing agents with delipidisation potential [17-20], in the present study no enhancing effect was observed for EtOH or IPA supplementation on transdermal permeation of lidocaine. Permeation of lidocaine, on the contrary, was diminished to alcohol supplementation to the vehicle compared to pure PBS which served as control.…”

Section: Discussioncontrasting

confidence: 82%

“…Permeation of lidocaine, on the contrary, was diminished to alcohol supplementation to the vehicle compared to pure PBS which served as control. There are also various reports about permeation enhancements of sulfoxides like DMSO [19,21,22], which can increase lipid fluidity and promote drug partition [23,24] or polyols like PG [17,25,26], which are described to solvate α-keratin and occupy hydrogen bonding sites [27,28]. IPM exhibits a direct action on the stratum corneum , permeates into liposome bilayers and increases fluidity of membranes [19,29], but even this aliphatic fatty acid esters diminished lidocaine permeation through equine skin (53,54) comparable to PG.…”

Section: Discussionmentioning

confidence: 99%

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The effects of chemical and physical penetration enhancers on the percutaneous permeation of lidocaine through equine skin

Stahl

Kietzmann

2014

BMC Vet Res

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BackgroundThe effect of physical and chemical permeation enhancers on in vitro transdermal permeation of lidocaine was investigated in the horse.Therefore, the effect of six vehicles (phosphate-buffered saline (PBS), 50% ethanol, 50% propylene glycol, 50% isopropylalcohol, 50% isopropylalcohol/isopropylmyristate and 50% dimethylsulfoxide) was examined as well as the effect of microneedle pretreatment with different needle lengths on transdermal drug delivery of lidocaine.The skin was obtained from the thorax of six Warmblood horses and was stored up to two weeks at - 20°C. Franz-type diffusion cells were used to study the transdermal permeation through split skin (600 μm thickness). The amount of lidocaine in the receptor fluid was determined by UV–VIS high-performance liquid chromatography.ResultsAll investigated vehicle supplementations diminished the transdermal flux of lidocaine through equine skin in comparison to pure PBS except dimethylsulfoxide, which resulted in comparable permeation rates to PBS. The maximum flux (Jmax) was 1.6-1.8 fold lower for lidocaine applied in 50% ethanol, propylene glycol, isopropylalcohol and isopropylalcohol/isopropylmyristate. A significant higher Jmax of lidocaine was observed when lidocaine was applied in PBS onto microneedle pretreated skin with similar permeation rates in both needle lengths. After 6 hours, 1.7 fold higher recovery rates were observed in the microneedle pretreated skin samples than in the untreated control samples. The lagtimes were reduced to 20–50% in the microneedle pretreated skin samples.ConclusionMicroneedles represent a promising tool for transdermal lidocaine application in the horse with a rapid systemic bioavailability.

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Section: Discussioncontrasting

confidence: 82%

Section: Discussionmentioning

confidence: 99%

The effects of chemical and physical penetration enhancers on the percutaneous permeation of lidocaine through equine skin

Stahl

Kietzmann

2014

BMC Vet Res

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“…Nevertheless, many in vitro studies for characterizing the percutaneous absorption of different drugs in several animal species have been performed (Yazdaniana, 1994; Mills et al. , 2003; Mills & Cross, 2006a,b, 2007; Mills, 2007; Ahsltrom et al. , 2007, 2009).…”

Section: Discussionmentioning

confidence: 99%

“…As in human pharmacology (Williams, 2006), the progress in veterinary pharmacology has mainly been hampered by a lack of direct in vitro-in vivo comparisons to support the acceptance of the in vitro approach for determining systemic availability of topically applied drugs in large animals kept under field conditions. Nevertheless, many in vitro studies for characterizing the percutaneous absorption of different drugs in several animal species have been performed (Yazdaniana, 1994;Mills et al, 2003;Mills & Cross, 2006a,b, 2007Mills, 2007;Ahsltrom et al, 2007Ahsltrom et al, , 2009. In vitro drug absorption through full thickness skin may potentially differ from that achieved in vivo due to a lack of microcirculation within the upper dermis.…”

Section: Discussionmentioning

confidence: 99%

Comparative in vitro characterization of moxidectin and doramectin percutaneous absorption through bovine skin

Sallovitz

Nejamkin

Lifschitz

et al. 2011

Vet Pharm & Therapeutics

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Topical formulations have achieved worldwide acceptance in veterinary medicine because their administration is an easy, less labor-intensive and nonstressing form. Any chemical compound that comes in contact with the skin has the potential to be locally and/or systemically absorbed. However, many factors related to the features of animal skin, composition of the topical formulation and to the drug itself can determine marked differences in the percutaneous absorption process. The aim of the current work was to characterize the pattern of in vitro percutaneous absorption for moxidectin (MXD) and doramectin (DRM), two of the most worldwide used topical macrocyclic lactone antiparasitic compounds in cattle. The work included the development of a simple and inexpensive in vitro assay useful to predict in vivo drug percutaneous absorption in cattle. Both drugs were administered as the commercial formulations intended for their topical administration to cattle. The in vitro studies were carried out using modified Franz-type vertical diffusion cells. Cattle skin slices of 500 μm thickness were prepared using a dermatome to separate the stratum corneum and upper epidermis from dermis and subcutaneous tissue. The receptor medium was sampled up to 72 h postadministration and drug concentrations were measured by HPLC. The parameters used to estimate the comparative in vitro skin permeation showed marked differences between DRM and MXD. A 5.29-fold longer lag time (T(lag)) was observed for DRM. Similarly, the flux (J) (2.93-fold) and the permeation coefficients (K(p) ) (2.95-fold) in cattle skin were significantly higher (P < 0.05) for DRM compared to those obtained for MXD. Additionally, the data obtained from the in vitro permeation studies was correlated with the plasma concentrations of both compounds achieved in vivo in cattle treated with the same topical formulations. Correlation coefficients between percentage of drug permeated in vitro vs. percentage of drug absorbed in vivo (up to 48 h post-treatment) were 0.856-0.887 (MXD) and 0.976-0.990 (DRM). However, the highest in vitro-in vivo correlations for both molecules were observed up to 24 h post-treatment A rapid screening method for testing different topical formulations can be achieved with the simple in vitro cattle skin permeation technique described here, which has been successfully adapted to test the comparative percutaneous absorption of MXD and DRM.

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“…DMSO can increase the lipid fluidity and promote drug partition [17,18,19,20,21]. PG [22,23,24] is known to solubilize α-keratin in the corneocytes, which is related to the intercellular penetration of drugs [25,26]. IPM directly acts on the stratum corneum, permeates into the lipid bilayer, and increases the fluidity of membranes [14,27].…”

Section: Introductionmentioning

confidence: 99%

Combined Use of N-Palmitoyl-Glycine-Histidine Gel and Several Penetration Enhancers on the Skin Permeation and Concentration of Metronidazole

et al. 2018

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N-Palmitoyl-Glycine-Histidine (Pal-GH) is a novel low molecular weight gelator. In our previous report, ivermectin, a lipophilic drug, was effectively delivered to skin tissue after topical application with Pal-GH as a spray gel formulation, and a much higher skin concentration was confirmed than with the administration of a conventional oral formulation. The objective of this study was to increase the skin permeation of metronidazole (MTZ), a hydrophilic drug, after the topical application of Pal-GH gel. An evaluation of the combined effect of chemical penetration enhancers (CPEs), such as isopropyl myristate (IPM), propylene glycol (PG), ethanol, diethylene glycol monoethyl ether, and dimethyl sulfoxide (DMSO), on skin permeation was also conducted. We found that a 5% Pal-GH gel containing 1% MTZ (F5MTZ) exhibited a 2.7-fold higher MTZ permeation through excised hairless rat skin than its solution. Furthermore, F5PG-MTZ and F5IPM-MTZ further increased the skin permeation of MTZ when compared to F5MTZ. Interestingly, F5PG-MTZ enhanced the skin penetration of MTZ, although no enhancement effect was observed for an MTZ solution containing PG. Thus, a Pal-GH formulation containing PG and IPM may enhance the skin permeation of MTZ.

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Vehicle Effects on the In Vitro Penetration of Testosterone through Equine Skin

Cited by 11 publications

References 27 publications

The effects of chemical and physical penetration enhancers on the percutaneous permeation of lidocaine through equine skin

The effects of chemical and physical penetration enhancers on the percutaneous permeation of lidocaine through equine skin

Comparative in vitro characterization of moxidectin and doramectin percutaneous absorption through bovine skin

Combined Use of N-Palmitoyl-Glycine-Histidine Gel and Several Penetration Enhancers on the Skin Permeation and Concentration of Metronidazole

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