Analysis of hair follicle penetration of lidocaine and fluorescein isothiocyanate-dextran 4 kDa using hair follicle-plugging method

Horita, Daisuke; Yoshimoto, Masato; Todo, Hiroaki; Sugibayashi, Kenji

doi:10.3109/03639045.2012.762653

Cited by 20 publications

(16 citation statements)

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“…3 and 4). These drugs may permeate skin via the aqueous porous pathway (34,35) or via appendages, such as sweat glands and hair follicles (36,37), due to their polarity. The contribution of such pathways should be taken into account in order to estimate the skin concentration of hydrophilic chemicals.…”

Section: Discussionmentioning

confidence: 99%

In Silico Estimation of Skin Concentration Following the Dermal Exposure to Chemicals

et al. 2015

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Section: Discussionmentioning

confidence: 99%

In Silico Estimation of Skin Concentration Following the Dermal Exposure to Chemicals

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“…29) This method revealed that the hair follicle could be the primary permeation pathway for watersoluble compounds such as ionized lidocaine (ionized LC) and fluorescein isothiocyanate-dextran 4 kDa (FD-4).…”

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“…[26][27][28] Therefore, we developed a method for hair follicle infundibulum-plugging with a mixture of silicone grease, cyanoacrylate adhesive and nile red, referred to as the hair follicle-plugging method, to analyze drug permeability through skin appendages. 29) This method revealed that the hair follicle could be the primary permeation pathway for watersoluble compounds such as ionized lidocaine (ionized LC) and fluorescein isothiocyanate-dextran 4 kDa (FD-4).…”

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“…29) The PA-mixture consisted of equal parts of silicone grease (Super Lube ® Silicone Dielectric Grease; Synco Chemical Corp., Bohemia, NY, U.S.A.) and α-cyanoacrylate adhesives (Aron Alpha Jelly; Konishi Co., Ltd., Osaka, Japan) with small amounts of nile red being applied to the hair follicles. Nile red was used to visualize the skin area treated by the PA-mixture.…”

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Analysis of the Pretreatment Effect of Ethanol on the Stratum Corneum- and Hair Follicular-Penetration of Drugs Using the Hair Follicle-Plugging Method

Horita

Todo

Sugibayashi

2014

CHEMICAL & PHARMACEUTICAL BULLETIN

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The hair follicle-plugging method was used to analyze the effects of EtOH on skin permeation pathways. Methods: In vitro permeation experiments were performed on 4 model drugs [isosorbide mononitrate (ISMN), ionized lidocaine (ionized LC), fluorescein (FL), and fluorescein isothiocyanate (FITC)-dextran 4 kDa (FD-4)] using excised pig ear skin. The skin permeations of ionized LC, FL, and FD-4 were decreased by hair follicle-plugging. Hair follicle-plugging prevented the skin permeation of FL and FD-4 in EtOHpretreated skin, but did not prevent that of ISMN. On the other hand, the effect of hair follicle-plugging on the permeation of ionized LC was different among the pretreatment conditions. These results indicate that the EtOH pretreatment greatly affected the aqueous pathway in the stratum corneum and hair follicles.Key words skin permeation; aqueous pathway; hair follicle-plugging; EtOH pretreatment; permeation route; enhancer Drug delivery systems (DDSs) have been investigated extensively to provide drug formulations with sustained release and/or targeting properties. Transdermal therapeutic systems (TTSs) are a typical example of DDSs. Therapeutic medicines in TTSs that have already been marketed include tulobuterol for the treatment of bronchial asthma, 1) clonidine for hypertension,2) nitroglycerin and isosorbide dinitrate for angina pectoris, 3,4) and rivastigmine for Alzheimer's disease. 5) However, the enhancement of skin permeation is sometimes required for drugs. Skin penetration enhancers are one of the methods used to increase the skin permeation of drugs.Skin penetration enhancers include alcohols, 6,7) fatty acids, 8,9) fatty acid esters, 10,11) terpenes, 12,13) pyrrolidones, 14,15) surfactants, 16,17) and Azone. 18,19) Among these enhancers, ethanol (EtOH) is the most commonly used additive in topical formulations. It is applied not only as a skin penetration enhancer, but also a solvent, such as water, for skin disinfection, as well as a solubilizer for poorly-soluble drugs. Estradiol and fentanyl dermal patches are typical examples that contain EtOH to enhance their absorption into the skin. [20][21][22] The mechanisms underlying the penetration-enhancement effect of EtOH on the stratum corneum barrier were previously reported to be lipid extraction, an increase in lipid fluidity, the enhancement of drug solubility in stratum corneum lipids, changes in skin hydration, effects on the putative pore pathway, alterations in keratinized proteins, and effects on solvent drugs. 23,24) Although many studies have already examined skin permeability with the simultaneous application of EtOH and drugs, few have investigated the effects of an EtOH pretreatment on the skin permeation of drugs. EtOH-containing formulations are frequently applied to the skin surface for the purpose of preventing disinfection and other therapeutic treatments. Other topical formulations may also be applied following treatments with EtOH-containing formulations.We previously investigated the effects of an EtOH pretreatment on th...

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“…Consequently, Mg 2+ should only pass through the interfollicular epidermis and its lipid domains and possibly through the sweat glands. Unlike the previous methods of hair follicle plugging with a microdrop of special varnishwax-mixture (Horita et al 2014), we used a combination of acriflavine dye and cyanoacrylate. The resulting polymerization reaction of cyanoacrylate molecules when they contacted acriflavine solution formed a rigid bond around the hair follicles blocking the orifice (Santappa & Sheriff n.d.).…”

Section: Discussionmentioning

confidence: 99%

Effect of topical magnesium application on epidermal integrity and barrier function

Chandrasekaran¹

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Dead Sea therapy is one of the oldest forms of treatment for skin disease and some chronic inflammatory diseases like arthritis and psoriasis. Much of the research to date has attributed the clinical effects of Dead Sea therapy to its mineral composition; mostly to magnesium salts.Magnesium salts, such as magnesium sulphate (Epsom salts), have long been used as a spa product and as a therapeutic to manage clinical conditions. The rationale of this PhD research was to understand the role of topically applied magnesium ions in epidermal integrity of human skin. We compartmentalized this research project into studying physiological, metabolic and proteolytic changes occurring at different layers of the skin. To begin with, we investigated the permeability of magnesium ions through stratum corneum. In Chapter 3, we developed a method to stain skin sections using mag-fura-2, a fluorescent dye that specifically binds to magnesium ions. When magnesium chloride (MgCl 2 ) solution was topically applied on normal and tape stripped skin, we observed that it is possible for magnesium ions to permeate through stratum corneum. We also varied the concentration and time of exposure of MgCl 2 solutions and found that at higher magnesium concentration, permeability is faster and penetration increases with progression of time.To further characterize permeability of the skin to magnesium, we blocked individual hair follicles using a novel method and subsequently treated skin with MgCl 2 solution. We found that hair follicles significantly contribute towards the permeation of magnesium ions. In Chapter 4, the hypothesis tested was that magnesium accelerates barrier recovery. Experiments were conducted on volunteers who did not have any history of skin conditions. We caused stratum corneum disruption on their volar forearm through tape stripping and subsequently treated that defined region with different salt solutions. The parameters we considered for understanding barrier function were transepidermal water loss, skin hydration and skin pH over 96 hours with repeated treatment at 24-hour intervals. We found that treatment with a variety of salt solutions, including magnesium chloride did not aid in lowering the TEWL to levels pre-tape stripping and no changes to skin pH were observed. However, we observed that treating the skin with 1.9 M magnesium solution nearly 2 fold (p < 0.05) increased hydration at 6 hours, relative to baseline at time zero, whereas water treatment increased hydration only 1.2 fold, and the hydration returned to normal levels within 24 hours in both cases. Skin barrier formation is a continuous process and occurs as a result of differentiating epidermal cells subsequently leading to terminal differentiation. In the case of disrupted barrier, the epidermal cells differentiate to replenish the lost layers of stratum corneum.Therefore as an extension to Chapter 4, experiments in Chapter 5 involved understanding the metabolic changes occurring in all three layers of the epidermis -granulosum, spinosum, bas...

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Analysis of hair follicle penetration of lidocaine and fluorescein isothiocyanate-dextran 4 kDa using hair follicle-plugging method

Abstract: The hf pathway must be important for the skin permeation of ionized compounds and hydrophilic high molecular compounds. hf-plugging is also a useful method for assessing the skin permeability of compounds through the hf pathway.

Cited by 20 publications

References 20 publications

In Silico Estimation of Skin Concentration Following the Dermal Exposure to Chemicals

In Silico Estimation of Skin Concentration Following the Dermal Exposure to Chemicals

Analysis of the Pretreatment Effect of Ethanol on the Stratum Corneum- and Hair Follicular-Penetration of Drugs Using the Hair Follicle-Plugging Method

Effect of topical magnesium application on epidermal integrity and barrier function

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