In vivo human skin permeability enhancement by oleic acid: transepidermal water loss and fourier-transform infrared spectroscopy studies

Tanojo, Hanafi; Junginger, Hans E.; Boddé, Harry E.

doi:10.1016/s0168-3659(96)01613-6

Cited by 50 publications

(39 citation statements)

References 30 publications

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“…Many bands in the spectrum can be either related to protein or lipids or both. [12][13][14] In the present study, cetrimide was found to enhance the flux and permeability of HP through SC. The SC was treated with various concentrations of cetrimide and IR spectra were obtained at different time intervals to study the mechanism of these actions.…”

Section: Resultsmentioning

confidence: 75%

Effect of Cetrimide and Ascorbic Acid on in Vitro Human Skin Permeation of Haloperidol.

Vaddi

Wang

et al. 2001

CHEMICAL & PHARMACEUTICAL BULLETIN

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Haloperidol (HP) is given in the treatment of acute psychosis as well as in maintenance therapy to prevent the relapse of the psychosis.1) Long-acting formulations are more meaningful in the maintenance therapy since long-term daily oral dose of 3 to 10 mg of HP 2) may lead to noncompliance. HP decanoate oily injection, the only long acting formulation available at present, has some disadvantages namely; complex dosing schedule while converting from oral therapy to depot therapy, 3) pain at the site of injection, individual to individual variation in the liberation of active drug from the parent drug 4) and marked variations of HP plasma concentration.5) Because of these disadvantages, the development of alternative long-acting formulations could be beneficial.Drug delivery via skin offers many advantages such as sustained drug delivery, improved patient compliance, reduced side effects, elimination of first-pass effect, interruption or termination of treatment when necessary. 6) However, many drugs require some mechanism to enhance their penetration through the excellent skin barrier to achieve therapeutic plasma concentration. One common approach is using chemical enhancers, which act by increasing the solubility of the drug in stratum corneum (SC) or disrupting the lipid matrix of SC or interacting with the intracellular protein.7) HP, which was reported to penetrate only sub-therapeutically through the human skin in vitro, would require penetration enhancers. 8) In this study, cetrimide and ascorbic acid, effect of which were studied in our earlier work on the permeation of HP through the rat skin in vitro, 9) were used at various concentrations 0.1, 0.3 and 0.6% (w/v) on human skin and the mechanism of enhancement by cetrimide was probed with diffusion profile kinetics and Fourier transform infrared (FT-IR) spectroscopy. ExperimentalMaterials HP, droperidol, DL-lactic acid, L-ascorbic acid, antibiotic antimycotic solution (100ϫ) and sodium dihydrogen phosphate monohydrate were purchased from Sigma Chemical Company and cetrimide from Chempure Pte Ltd., Singapore. All other chemical reagents were of at least reagent grade and all materials were used as supplied.Analytical Method Drug concentrations were determined by reversed phase HPLC (C 18 column, Hewlett Packard Pte Ltd., Germany) at 254 nm. Mobile phase consisted of 0.05 M phosphate buffer (pH 3) and acetonitrile in the ratio of 50 : 50. Droperidol was used as an internal standard. Flow rate was 1.3 ml/min and injection volume was 100 ml. Retention times of the internal standard and drug were approximately 4 and 6.5 min. Mean peak area ratios of the drug and internal standard in 0.03% (v/v) lactic acid were linearly related to the drug concentrations for the samples containing 1 to 7 mg/ml (rϭ0.9999). Intraday and interday coefficient of variations for all concentrations varied from 1.29 to 11.64%. Solubility Studies Excess of HP was added to 0.03% (v/v) lactic acid containing antibacterial antimycotic solution (1 in 100 dilution) with and without enhanc...

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Section: Resultsmentioning

confidence: 75%

Effect of Cetrimide and Ascorbic Acid on in Vitro Human Skin Permeation of Haloperidol.

Vaddi

Wang

et al. 2001

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…In the present system, microemulsion was prepared using castor oil (fatty acid), which induces highly permeable pathways in the stratum corneum (18)(19)(20). Tween 80 is a widely accepted nonionic surfactant, used in many pharmaceutical formulations (21)(22)(23).…”

Section: Resultsmentioning

confidence: 99%

Microemulsion System with Improved Loading of Piroxicam: A Study of Microstructure

2009

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Abstract. Formulation of a new oil-in-water (o/w) microemulsion composed of castor oil/Tween 80/ ethanol/phosphate buffer for enhancing the loading capacity of an anti-inflammatory drug piroxicam has been accomplished. The pseudo-ternary phase diagram has been delineated at constant surfactant/ cosurfactant ratio (1:2). The internal structure of so created four-component system was elucidated by means of an analysis of isotropic area magnitudes in the phase diagram. Conductivity (σ), kinematic viscosity (k η ), and surface tension (γ) studies with the variation in Φ w (weight fraction of aqueous phase) show the occurrence of structural changes from water-in-oil (w/o) microemulsion to oil-in-water (o/w). Along with the solubility and partition studies of piroxicam in microemulsion components, the changes in the microstructure of the microemulsion after incorporation of drug have been evaluated using pH, σ, γ, k η , and density studies. Piroxicam, a poorly water-soluble drug displayed high solubility (1.0%) in an optimum microemulsion formulation using ethanol (55.0%), Tween 80 (26.5%), castor oil (7.5%), and phosphate buffer (11.0%). The results have shown that the microemulsion remained stable after the incorporation of piroxicam. Fluorescence spectra analysis taking pyrene as fluorescent probe was performed, and the results showed that pyrene was completely solubilized in the oil phases of the bicontinuous microemulsions. The fluorescence spectrum of the model drug piroxicam was used to probe the intramicellar region of nonionic microemulsion. The results showed that the piroxicam was localized in the interfacial film of microemulsion systems more deeply in the palisade layer with ethanol as the cosurfactant.

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“…In this context, Tanojo et al [15] using ATR-FTIR have reported that the increase in absorbance ratio of 1,710/1,740 cm -1 peak returned to normal values after 3 h as OA diffuses into deeper layers. Unlike the attenuated total reflectance infrared spectroscopy, simple FT-IR (as used in the study) cannot detect the biophysical changes taking place as a function of depth in skin [33].…”

Section: Discussionmentioning

confidence: 98%

“…In this procedure, the epidermis sample serves as its own control, thereby avoiding intersample variation. To estimate the uptake of fatty acid in skin, the ratio of peak area corresponding to the free carboxylic group of exogenous free fatty acid at 1,710 cm -1 and the esterified carboxylic group of the skin lipids at 1,740 cm -1 was calculated as described earlier in the literature [15].…”

Section: Ft-ir Spectroscopic Studiesmentioning

confidence: 99%

Transdermal Iontophoresis of Insulin

Pillai¹,

Panchagnula²

2004

Skin Pharmacol Physiol

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The delivery of large peptides through the skin poses a significant challenge, and various strategies are under active investigation for enhancing the transdermal permeation. For large peptides, it is difficult to achieve significant permeation using iontophoresis alone. Hence a combination of fatty acids with iontophoresis was hypothesized to result in higher enhancement than achieved with either of them alone. Saturated fatty acids and cis unsaturated fatty acids were studied in combination with iontophoresis using excised rat skin. The skin was pretreated for 2 h with an ethanolic (EtOH) solution of 5% w/v or v/v fatty acids, namely lauric acid (LA), oleic acid (OA), linoleic acid (LOA) and linolenic acid (LLA), followed by either passive or iontophoretic permeation (0.5 mA/cm² for 6 h). Fourier transform infrared spectroscopy (FT-IR) was used to investigate the biophysical changes on treatment with fatty acid/EtOH or neat fatty acid, mainly focusing on the infrared region at 2,920, 1,710 and 1,720 cm^–1. Unsaturated fatty acids showed higher enhancement than LA, and the enhancement increased with the number of double bonds. On the other hand, in the presence of iontophoresis, LA/EtOH showed the highest enhancement. Neat LOA did not show any significant difference (p > 0.05) compared to the LOA/EtOH combination. FT-IR studies revealed that fatty acids act by interacting with the skin lipids. All the fatty acids showed synergistic enhancement when combined with iontophoresis. The flux enhancement was highest with LA, which in the presence of iontophoresis showed 20 times enhancement of insulin flux in comparison to passive flux and 9 times enhancement as compared to iontophoresis alone. Flux enhancement of unsaturated fatty acids was in the following decreasing order LOA > OA > LLA.

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In vivo human skin permeability enhancement by oleic acid: transepidermal water loss and fourier-transform infrared spectroscopy studies

Cited by 50 publications

References 30 publications

Effect of Cetrimide and Ascorbic Acid on in Vitro Human Skin Permeation of Haloperidol.

Effect of Cetrimide and Ascorbic Acid on in Vitro Human Skin Permeation of Haloperidol.

Microemulsion System with Improved Loading of Piroxicam: A Study of Microstructure

Transdermal Iontophoresis of Insulin

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