Effect of Penetration Enhancers and Iontophoresis on the Ultrastructure and Cholecystokinin-8 Permeability through Porcine Skin

Bhatia, Kuljit S.; Gao, Shen; Freeman, Thomas; Singh, Jagdish

doi:10.1021/js970023k

Cited by 51 publications

(18 citation statements)

References 36 publications

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“…Our study demonstrates that all the formulations shifted the spectral bands to higher wavenumbers which result in a blue shift of CH stretching. This may be due to the increase in the degree of disorder of the lipid acyl chains, resulting in the increased fluidity of SC (33).…”

Section: Discussionmentioning

confidence: 99%

Enhanced Topical Delivery of Finasteride Using Glyceryl Monooleate-Based Liquid Crystalline Nanoparticles Stabilized by Cremophor Surfactants

et al. 2013

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Abstract. The aim of this study was to investigate the capability of two surfactants, Cremophor RH 40 (RH) and Cremophor EL (EL), to prepare liquid crystalline nanoparticles (LCN) and to study its influence on the topical delivery of finasteride (FNS). FNS-loaded LCN was formulated with the two surfactants and characterized for size distribution, morphology, entrapment efficiency, in vitro drug release, and skin permeation/retention. Influence of FNS-loaded LCN on the conformational changes on porcine skin was also studied using attenuated total reflectance Fourier-transform infrared spectroscopy. Transmission electron microscopical image confirmed the formation of LCN. The average particle size of formulations was in the range of 165.1-208.6 and 153.7-243.0 nm, respectively. The formulations prepared with higher surfactant concentrations showed faster release and significantly increased skin permeation. Specifically, LCN prepared with RH 2.5% presented higher permeation flux (0.100± 0.005 μgcm −2 h −1 ) compared with lower concentration (0.029±0.007 μgcm −2 h −1 ). Typical spectral bands of lipid matrix of porcine skin were shifted to higher wavenumber, indicating increased degree of disorder of the lipid acyl chains which might cause fluidity increase of stratum corneum. Taken together, Cremophor surfactants exhibited a promising potential to stabilize the LCN and significantly augmented the skin permeation of FNS.

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Section: Discussionmentioning

confidence: 99%

Enhanced Topical Delivery of Finasteride Using Glyceryl Monooleate-Based Liquid Crystalline Nanoparticles Stabilized by Cremophor Surfactants

et al. 2013

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“…These results suggested that the enhanced transdermal absorption of SA iontophoretically by the presence of ethanol in a drug solution is not due to the increased current density in vivo, but probably due to the direct action of ethanol on the stratum corneum. It is reported that pretreatment of skin surface with absolute ethanol caused a loss of structural components in the superficial stratum corneum cell layers [8]. Also, burns are sometimes caused by iontophoresis [14].…”

Section: Resultsmentioning

confidence: 99%

“…The pretreatment effect of ethanol on the skin surface has been reported by several investigators, in which the ethanol pretreatment prior to iontophoresis dramatically increased the transdermal absorption of insulin, leutinizing hormone releasing hormone and cholecystokinin-8 [6][7][8]. Regarding the direct effect of ethanol in a drug solution in iontophoresis, however, there is no report available, except our previous reports [9,10].…”

Section: Introductionmentioning

confidence: 88%

Iontophoretic Transdermal Delivery of Salicylic Acid Dissolved in Ethanol-Water Mixture in Rats

Murakami

Ihara²,

Kiyonaka³

et al. 1999

Skin Pharmacol Physiol

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The usefulness of iontophoresis is restricted to highly water-soluble compounds, since drugs are generally applied as an aqueous solution in a drug electrode. In the present study, salicylic acid (SA) dissolved in ethanol-water mixture was loaded in a drug electrode, and the effect of ethanol on the iontophoretic transdermal delivery of SA was evaluated. Ethanol at a concentration of 10 or 30% showed no significant effect on the iontophoretic transdermal delivery of SA compared to that in the absence of ethanol, but 40 or 70% ethanol increased it significantly. The current density passing through in vivo during iontophoretic treatment decreased with increase in ethanol concentrations. These results suggested that the enhanced transdermal absorption of SA iontophoretically by the presence of ethanol in a drug solution is not due to the increased current density in vivo, but probably due to the direct action of ethanol on the stratum corneum. In conclusion, addition of ethanol to a drug solution at an appropriate concentration was proved to enhance the iontophoretic transdermal delivery of SA. A mixture of ethanol and water can dissolve many poorly water-soluble drugs, and therefore it would be able to expand the application of iontophoresis to include many drugs that are poorly soluble in water.

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“…Because high-molecular-weight drugs cannot be delivered using a single method, some combination systems -iontophoresis as a physical method plus chemical penetration enhancer as a chemical method -have been suggested to solve this problem [4][5][6][7]. However, the mechanism of their synergistic effect has not been reported from in vivo studies.…”

Section: Discussionmentioning

confidence: 99%

“…A problem with the iontophoretic drug delivery system is how to overcome the resistance of the SC, the main permeability barrier, for more effective penetration with less side effects. Some researches in in vitro skin studies have shown that pretreatment with a chemical penetration enhancer before iontophoresis increases the penetration of high-molecular-weight drugs [4][5][6][7].…”

Section: Introductionmentioning

confidence: 99%

The Pretreatment Effect of Chemical Skin Penetration Enhancers in Transdermal Drug Delivery Using Iontophoresis

Choi

Lee

Ahn

et al. 1999

Skin Pharmacol Physiol

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The transdermal drug delivery (TDD) system has largely been divided into physical, biochemical and chemical methods. Recently, combinations of these methods were introduced for more effective delivery with less side effects. We performed this study to identify the effectiveness and mechanism of TDD using the physical method, ‘iontophoresis’, plus the chemical method, ‘pretreatment with chemical enhancer’. The action sites of chemical enhancers in the stratum corneum (SC) were observed by electron microscope. We also studied whether this combined method synergistically impaired the skin barrier. To confirm the synergistic effect on skin penetration by this combined method, we measured the blood glucose level after insulin iontophoresis following a chemical enhancer pretreatment in rabbits. The results were that (1) dilatation of the intercellular lipid layers of the SC and lacunae was prominent in pretreatment with chemical enhancers inducing high transepidermal water loss (TEWL); (2) the skin barrier impairment, with repeated treatments showing an increased TEWL and also epidermal proliferation, was increased with the chemical enhancers that showed a high TEWL immediately after treatment; (3) the combination of chemical enhancer pretreatment and iontophoresis showed no synergistic impairment of the skin barrier, and (4) the chemical enhancer pretreatment with greater impairment of the skin barrier could increase the delivery of insulin by iontophoresis. The results showed that a combination of chemical enhancer pretreatment and iontophoresis could deliver drugs more effectively than iontophoresis alone. Our proposed theory is that iontophoretic drug delivery may be easier through the dilated intercellular spaces of the SC which have a lower electrical impedance following the chemical enhancer pretreatment. Because the effect and the side effects in the combination are decided by the chemical enhancer rather than iontophoresis, the development of proper chemical enhancers is important in future plans.

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Effect of Penetration Enhancers and Iontophoresis on the Ultrastructure and Cholecystokinin-8 Permeability through Porcine Skin

Cited by 51 publications

References 36 publications

Enhanced Topical Delivery of Finasteride Using Glyceryl Monooleate-Based Liquid Crystalline Nanoparticles Stabilized by Cremophor Surfactants

Enhanced Topical Delivery of Finasteride Using Glyceryl Monooleate-Based Liquid Crystalline Nanoparticles Stabilized by Cremophor Surfactants

Iontophoretic Transdermal Delivery of Salicylic Acid Dissolved in Ethanol-Water Mixture in Rats

The Pretreatment Effect of Chemical Skin Penetration Enhancers in Transdermal Drug Delivery Using Iontophoresis

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