Developments of Transdermal Transport System during Skin Iontophoresis and Electroporation

Nishimura, Tomonori; Akimoto, Makio; Miyazaki, Masaru; Nomoto, Mayumi; Miyakawa, Michio

doi:10.2529/piers100117000608

Cited by 4 publications

(3 citation statements)

References 6 publications

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“…Transdermal drug penetration into the joint cavity is mostly limited by the low permeability of the stratum corneum of the skin, the thickness of the surrounding tissue layer, and the special physicochemical barrier function of the synovial membrane, which is commonly referred to as the “blood–joint barrier.” 27 However, EP is capable of opening transitory pores on complex structures, such as the multilamellar lipid bilayer of the stratum corneum and the synovial membrane. 28 , 29 Macromolecules of up to 40 kDa can thus be transported through and/or into the skin. 11 , 15 …”

Section: Discussionmentioning

confidence: 99%

Electroporation-enhanced transdermal diclofenac sodium delivery into the knee joint in a rat model of acute arthritis

Hartmann¹,

Butt²,

Fehér³

et al. 2018

DDDT

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PurposeSince electroporation (EP) can increase the permeability of biological membranes, we hypothesized that it offers an opportunity to enhance the transdermal delivery of drugs for intra-articular indications. Our aim was to compare the anti-inflammatory and analgesic efficacy of EP-combined topical administration of diclofenac sodium hydrogel (50 mg mL−1 in 230 µL volume) with that of an equivalent dose of oral (75 mg kg−1) and simple topical administration.MethodsArthritis was induced with the injection of 2% λ-carrageenan and 4% kaolin into the right knee joints of male Sprague Dawley rats. EP was applied for 8 min with 900 V high-voltage pulses for 5 ms followed by a 20 ms break. Drug penetration into the synovial fluid and plasma was detected by high-performance liquid chromatography. Leukocyte–endothelial interactions were visualized by intravital videomicroscopy on the internal surface of the synovium. Inflammation-induced thermal and mechanical hyperalgesia reactions, knee joint edema, and inflammatory enzyme activities were assessed at 24 and 48 h after arthritis induction.ResultsEP significantly increased the plasma level of diclofenac as compared with the topical controls 10 min after the 2% λ-carrageenan and 4% kaolin injection. Increased leukocyte–endothelial interactions were accompanied by joint inflammation, which was significantly reduced by oral and EP diclofenac (by 45% and by 30%, respectively) and only slightly ameliorated by simple topical diclofenac treatment (by 18%). The arthritis-related secondary hyperalgesic reactions were significantly ameliorated by oral and EP-enhanced topical diclofenac treatments. The knee cross-section area (which increased by 35%) was also reduced with both approaches. However, simple topical application did not influence the development of joint edema and secondary hyperalgesia.ConclusionThe study provides evidence for the first time of the potent anti-inflammatory and analgesic effects of EP-enhanced topical diclofenac during arthritis. The therapeutic benefit provided by EP is comparable with that of oral diclofenac; EP is a useful alternative to conventional routes of administration.

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Section: Discussionmentioning

confidence: 99%

Electroporation-enhanced transdermal diclofenac sodium delivery into the knee joint in a rat model of acute arthritis

Hartmann¹,

Butt²,

Fehér³

et al. 2018

DDDT

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show abstract

“…Recently, other techniques such as ultrasound, electroporation, and chemical enhancers have been combined with iontophoresis [22] . The combination system seems to be more effective for transdermal delivery compared with the iontophoresis system alone.…”

mentioning

confidence: 99%

Effect of Ethanol on Iontophoretic Transdermal Delivery of 5-Aminolevulinic Acid through Yucatan Micropig Full-thickness Skin

Asai¹,

Ochiai²,

Kawashima³

et al. 2019

pharmaceutical-sciences

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Asai et al.: Effect of Ethanol on Iontophoresis of ALAThe effect of ethanol was investigated on iontophoretic transdermal delivery of 5-aminolevulinic acid through Yucatan micropig full-thickness skin. When 20 % ethanol was added into an aqueous 5-aminolevulinic acid solution, the iontophoretic permeation of 5-aminolevulinic acid through Yucatan micropig full-thickness skin was enhanced. The addition of ethanol also enlarged the partition of 5-aminolevulinic acid into Yucatan micropig full-thickness skin, which gave rise to enhancement of 5-aminolevulinic acid permeation. This result suggested that the combination system of iontophoretic delivery and 20 % ethanol could be a promising approach for the promotion of 5-aminolevulinic acid skin permeation.

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“…Transdermal drug penetration into the joint cavity is mostly limited by the low permeability of the stratum corneum of the skin, the thickness of the surrounding tissue layer and the special physico-chemical barrier function of the synovial membrane, which is commonly referred to as the "blood-joint barrier" [119]. However, EP is capable of opening transitory pores on complex structures, such as the multilamellar lipid bilayer of the stratum corneum and the synovial membrane [120,121]. Macromolecules of up to 40 kDa can thus be transported through and/or into the skin [122,123].…”

Section: Beneficial Effects Of Ep Delivery Of Diclofenac Into the Knee Jointmentioning

confidence: 99%

Pathomechanism and therapeutic possibilities of arthritis

Butt¹

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Purpose: Since electroporation (EP) can increase the permeability of biological membranes, we hypothesized that it offers an opportunity to enhance the transdermal delivery of drugs for intra-articular indications. Our aim was to compare the anti-inflammatory and analgesic efficacy of EP-combined topical administration of diclofenac sodium hydrogel (50 mg mL -1 in 230 µL volume) with that of an equivalent dose of oral (75 mg kg -1 ) and simple topical administration. Methods: Arthritis was induced with the injection of 2% λ-carrageenan and 4% kaolin into the right knee joints of male Sprague Dawley rats. EP was applied for 8 min with 900 V highvoltage pulses for 5 ms followed by a 20 ms break. Drug penetration into the synovial fluid and plasma was detected by high-performance liquid chromatography. Leukocyte-endothelial interactions were visualized by intravital videomicroscopy on the internal surface of the synovium. Inflammation-induced thermal and mechanical hyperalgesia reactions, knee joint edema, and inflammatory enzyme activities were assessed at 24 and 48 h after arthritis induction. Results: EP significantly increased the plasma level of diclofenac as compared with the topical controls 10 min after the 2% λ-carrageenan and 4% kaolin injection. Increased leukocyteendothelial interactions were accompanied by joint inflammation, which was significantly reduced by oral and EP diclofenac (by 45% and by 30%, respectively) and only slightly ameliorated by simple topical diclofenac treatment (by 18%). The arthritis-related secondary hyperalgesic reactions were significantly ameliorated by oral and EP-enhanced topical diclofenac treatments. The knee crosssection area (which increased by 35%) was also reduced with both approaches. However, simple topical application did not influence the development of joint edema and secondary hyperalgesia. Conclusion:The study provides evidence for the first time of the potent anti-inflammatory and analgesic effects of EP-enhanced topical diclofenac during arthritis. The therapeutic benefit provided by EP is comparable with that of oral diclofenac; EP is a useful alternative to conventional routes of administration.

show abstract

Developments of Transdermal Transport System during Skin Iontophoresis and Electroporation

Cited by 4 publications

References 6 publications

Electroporation-enhanced transdermal diclofenac sodium delivery into the knee joint in a rat model of acute arthritis

Electroporation-enhanced transdermal diclofenac sodium delivery into the knee joint in a rat model of acute arthritis

Effect of Ethanol on Iontophoretic Transdermal Delivery of 5-Aminolevulinic Acid through Yucatan Micropig Full-thickness Skin

Pathomechanism and therapeutic possibilities of arthritis

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