Use of Electroporation to Accelerate the Skin Permeability Enhancing Action of Oleic Acid.

Takeuchi, Yoshikazu; Miyawaki, Kohji; Kamiyabu, Satoshi; Fukushima, Shoji; Yamaoka, Yumiko; Kishimoto, Seiji; Taguchi, Kenji; Masai, Hideki; Kamata, Yuri

doi:10.1248/bpb.23.850

Cited by 6 publications

(5 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Using timeresolved freeze-fracture electron microscopy, we observed the development of local disruption areas of the lipid lamellae in the SC, in the form of vesicle formation (Gallo et al, 1999(Gallo et al, , 2002. Structural disruption was also detected by FTIR as increased SC hydration (Takeuchi et al, 2000), and by small angle x-ray diffraction (SAXD) as increased structural disorder (Jadoul et al, 1998b(Jadoul et al, , 1997. Because SC lipids are involved in structural alteration by the electric pulses, we expect that modifying the SC lipids will have an effect on transdermal transport by electroporation.…”

Section: Introductionmentioning

confidence: 97%

Saturated Anionic Phospholipids Enhance Transdermal Transport by Electroporation

Sen

Zhao

Hui

2002

Biophysical Journal

View full text Add to dashboard Cite

Anionic phospholipids, but not cationic or neutral phospholipids, were found to enhance the transdermal transport of molecules by electroporation. When added as liposomes to the milieus of water-soluble molecules to be delivered through the epidermis of porcine skin by electroporation, these phospholipids enhance, by one to two orders of magnitude, the transdermal flux. Encapsulation of molecules in liposomes is not necessary. Dimyristoylphosphatidylserine (DMPS), phosphatidylserine from bovine brain (brain-PS), dioleoylphosphatidylserine (DOPS), and dioleoylphosphatidylglycerol (DOPG) were used to test factors affecting the potency of anionic lipid transport enhancers. DMPS with saturated acyl chains was found to be a much more potent transport enhancer than those with unsaturated acyl chains (DOPS and DOPG). There was no headgroup preference. Saturated DMPS was also more effective in delaying resistance recovery after pulsing, and with a greater affinity in the epidermis after pulsing. Using fluorescent carboxyl fluorescein and fluorescein isothiocyanate (FITC)-labeled Dextrans as test water-soluble molecules for transport, and rhodamine-labeled phospholipids to track anionic phospholipids, we found, by conventional and confocal fluorescence microscopy, that transport of water-soluble molecules was localized in local transport spots or regions (LTRs) created by the electroporation pulses. Anionic phospholipids, especially DMPS, were located at the center of the LTRs and spanned the entire thickness of the stratum corneum (SC). The degree of saturation of anionic phospholipids made no difference in the densities of LTRs created. We deduce that, after being driven into the epidermis by negative electric pulses, saturated anionic phospholipids mix and are retained better by the SC lipids. Anionic lipids prefer loose layers or vesicular rather than multilamellar forms, thereby prolonging the structural recovery of SC lipids to the native multilamellar form. In the presence of 1 mg/ml DMPS in the transport milieu, the flux of FITC-Dextran-4k was enhanced by 80-fold and reached 175 microg/cm(2)/min. Thus, the use of proper lipid enhancers greatly extends the upper size limit of transportable chemicals. Understanding the mechanism of lipid enhancers enables one to rationally design better enhancers for transdermal drug and vaccine delivery by electroporation.

show abstract

Section: Introductionmentioning

confidence: 97%

Saturated Anionic Phospholipids Enhance Transdermal Transport by Electroporation

Sen

Zhao

Hui

2002

Biophysical Journal

View full text Add to dashboard Cite

show abstract

“…2,3,6) However, a clinically applicable system has not been reported yet. Gallo et al examined the permeability changes of full-thickness porcine skin when two electrodes were attached to the stratum corneum.…”

Section: Discussionmentioning

confidence: 99%

“…However, we subsequently demonstrated that the simultaneous presence of the drug at the time of the electric pulse was not necessary for enhancement of penetration. 6) Therefore, a separate space in which the drug solution is retained is not necessary. The frog-type electrode was designed so that electric pulse could be applied uniformly to the stratum corneum.…”

Section: Discussionmentioning

confidence: 99%

“…[7][8][9][10][11][12][13][14][15][16][17][18][19][20][21] In the second case, the electrodes are set only on the stratum corneum and electroporation is applied on the surface of the stratum corneum. 6,22) The latter system might be more suitable for clinical applications.…”

mentioning

confidence: 99%

“…Using a FT-IR/ATR method, we found 6) that electroporation by the frog-type electrode disordered the lipid and protein structure of the stratum corneum. These structural changes were accelerated by combination with oleic acid.…”

mentioning

confidence: 99%

See 2 more Smart Citations

Transdermal Drug Delivery by Electroporation Applied on the Stratum Corneum of Rat Using Stamp-Type Electrode and Frog-Type Electrode in Vitro.

Fukushima

Kishimoto

Horai

et al. 2001

Biological & Pharmaceutical Bulletin

Self Cite

View full text Add to dashboard Cite

Transdermal enhancement effects of electroporation applied only on the stratum corneum by two electrode types, the stamp-type electrode and the frog-type electrode, were investigated in vitro using excised rat skin. Carboxyfluorescein (CF) was selected as a model compound. The excised skin was set in a Franz type diffusion cell and a square wave electric pulse was applied to the stratum corneum under various electric pulse conditions. We determined the permeability of CF to the receptor compartment under these conditions. Voltage, electric pulse length, and number of electric pulses, were varied from 10 to 1000 V, 50 m ms to 15 ms and 5 to 30 pulses, respectively. Flux rate was enhanced as the electric pulse condition strengthened. However, the maximum value was attained in the flux rate, above which no increase was observed despite strengthening of the electric pulse. Although at low electric pulses, the enhancement effect of the frog-type electrode was superior to that of the stamptype electrode, the maximum flux rates were the same. These results indicate that electroporation on the stratum corneum using the stamp-type electrode or frog-type electrode, is useful for transdermal drug delivery.

show abstract

Transdermal iontophoresis of 5-fluorouracil combined with electroporation and laser treatment

Fang

Hung

Fang

et al. 2004

International Journal of Pharmaceutics

View full text Add to dashboard Cite

Use of Electroporation to Accelerate the Skin Permeability Enhancing Action of Oleic Acid.

Cited by 6 publications

References 0 publications

Saturated Anionic Phospholipids Enhance Transdermal Transport by Electroporation

Saturated Anionic Phospholipids Enhance Transdermal Transport by Electroporation

Transdermal Drug Delivery by Electroporation Applied on the Stratum Corneum of Rat Using Stamp-Type Electrode and Frog-Type Electrode in Vitro.

Transdermal iontophoresis of 5-fluorouracil combined with electroporation and laser treatment

Contact Info

Product

Resources

About