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

Fang, Jia‐You; Hung, Chi‐Feng; Fang, Yi‐Ping; Chan, Te-Fu

doi:10.1016/j.ijpharm.2003.10.025

Cited by 49 publications

(33 citation statements)

References 20 publications

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“…With progressive removal of the stratum corneum, the ionised and neutral forms of phenobarbital permeated through the less-resistant skin barrier at much higher rates. Similar behaviour has been seen for 5-fluorouracil (Fang et al, 2004), with removal of the stratum corneum leading to an increase in passive diffusion from <0.03 mol cm −2 in 6 h to approximately 17 mol cm −2 a difference of more than 550-fold. Fig.…”

Section: Permeation Across Compromised Skinsupporting

confidence: 74%

Passive and iontophoretic transdermal delivery of phenobarbital: Implications in paediatric therapy

Djabri¹,

Guy²,

Delgado‐Charro³

2012

International Journal of Pharmaceutics

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Section: Permeation Across Compromised Skinsupporting

confidence: 74%

Passive and iontophoretic transdermal delivery of phenobarbital: Implications in paediatric therapy

Djabri¹,

Guy²,

Delgado‐Charro³

2012

International Journal of Pharmaceutics

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“…In contrast, the anodal polarity may also have created transient aqueous pathways. But this would have had no effect on the electrophoretic transport of a negatively charged drug [13,14] . The results indicate that the contribution of electrophoretic movement was not important for (+)-catechin.…”

Section: Transdermal Delivery Of (+)-Catechin By Electroporationmentioning

confidence: 99%

Transdermal Delivery of Tea Catechins by Electrically Assisted Methods

Fang¹,

Hung²,

Hwang³

et al. 2005

Skin Pharmacol Physiol

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Tea polyphenols, including (+)-catechin, (–)-epicatechin, and (–)-epigallocatechin-3-gallate (EGCG), have been shown to possess potent antioxidant and chemopreventive activities. The aim of this study was to assess the effects of electroporation, iontophoresis, and their combination on the transdermal delivery of tea catechins across porcine skin. The permeation characteristics were investigated using various analogues of catechins, pH values, and modes of electroporation and iontophoresis. The mechanisms by which these catechins were transported via the skin were elucidated by examining the electric conductivity, transepidermal water loss (TEWL), and fusion of stratum corneum lipid liposomes (SCLL). The isomers, (+)-catechin and (–)-epicatechin, showed different behaviors of skin permeation and local skin deposition with the electrically assisted methods. The results suggest evidence of selective skin absorption of (–)-epicatechin over (+)-catechin. A synergistic effect was detected for (+)-catechin but not for (–)-epicatechin after application of electroporation followed by iontophoresis. The presence of a gallic acid ester in the structure of EGCG significantly increased the skin uptake of catechins. However, a negligible amount of or no EGCG molecules permeated across the skin. The mechanisms involved in the enhancement of electroporation may be the skin reservoir effect and an increase in skin permeability. The TEWL profiles suggest that in addition to the force of electrorepulsion, the skin hydration effect and structural alterations may also have contributed to the enhancement by iontophoresis. Electroporation did not influence the skin barrier function, although the skin permeability increased according to the SCLL fusion study.

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“…To meet the criteria for reliable and reproducible skin-mediated drug delivery, a range of approaches and enhancement techniques, primarily aimed at disrupting the formidable barrier effect of the (epi)dermal layer, have been proposed, and these are typically physical or chemical in origin (Howard & Kenneth, 1996;Benson, 2005;Ritesh & Anil, 2007;Tiwary et al, 2007;Wang et al, 2007;Nikhil et al, 2008;Dhamecha et al, 2009;Pathan & Setty, 2009;Kumar et al, 2010;Madishetti et al, 2010;Sharma et al, 2011). The physical techniques primarily include iontophoresis, sonophoresis and laser-based treatments, all of which are laborious, require specialized equipment and there are also cases of irreversible skin damage being attributed to such approaches (Meidan et al, 1999;Fang et al, 2004;Brahma & Shyam, 2008;Clara et al, 2008).…”

Section: Introductionmentioning

confidence: 99%

Enhancement in deposition and permeation of 5-fluorouracil through human epidermis assisted by peptide dendrimers

et al. 2013

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Enhancing the deposition and permeation of 5-fluorouracil across human epidermis assisted by appropriately charged and well-defined peptide dendrimers was investigated. Peptide dendrimers with arginine as the terminal amino acid and having a range of terminal positive charges (4þ and 16 þ ) were synthesized by solid phase peptide synthesis. Various parameters including effect of peptide dendrimers on the solubility and partition coefficient of 5-FU, degradation of drug in skin as well as deposition and permeation of 5-FU in/through skin were studied. All the tested dendrimers increased the aqueous solubility and partition coefficient of 5-FU with each also significantly (p50.05) enhancing the deposition and permeation of 5-FU in/across human epidermis in a concentration-dependent manner. Of the three peptide dendrimers examined, R8 dendrimer (bearing 8 þ charge derived from four terminal arginines and MW of &1000 Da) showed greatest values for flux, Q 48 (cumulative amount of drug permeated at the end of 48 h) and amount of drug retained in human skin. Furthermore, this study also scrutinized and reports on the likely mechanisms by which peptide dendrimers act as transdermal permeation enhancers.

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

Cited by 49 publications

References 20 publications

Passive and iontophoretic transdermal delivery of phenobarbital: Implications in paediatric therapy

Passive and iontophoretic transdermal delivery of phenobarbital: Implications in paediatric therapy

Transdermal Delivery of Tea Catechins by Electrically Assisted Methods

Enhancement in deposition and permeation of 5-fluorouracil through human epidermis assisted by peptide dendrimers

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