Structure–Activity Relationship for Chemical Skin Permeation Enhancers: Probing the Chemical Microenvironment of the Site of Action

Warner, Kevin S.; Li, S.Kevin; He, Ning; Suhonen, T. Marjukka; Chantasart, Doungdaw; Bolikal, Durgadas; Higuchi, William I.

doi:10.1002/jps.10367

Cited by 46 publications

(89 citation statements)

References 32 publications

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“…H is the hindered transport factor for passive diffusion and is related to the ratio of solute molecular size to the effective pore size of the transport pathway [23]. The parallel pathway model has been used in the evaluation of chemical penetration enhancers and the examination of quantitative structure enhancement relationships of the enhancers in skin permeation studies [24,25,26,27,28,29,30,31,32]. Because the skin is a composite of two layers in series of different barrier properties (stratum corneum and underneath tissues, respectively), the total permeability coefficient of skin (P T ) can be described by [33,34]:…”

Section: Mechanistic Model Of Skin Transportmentioning

confidence: 99%

Passive and Iontophoretic Transport through the Skin Polar Pathway

Peck

2013

Skin Pharmacol Physiol

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The purpose of the present article is to briefly recount the contributions of Prof. William I. Higuchi to the area of skin transport. These contributions include developing fundamental knowledge of the barrier properties of the stratum corneum, mechanisms of skin transport, concentration gradient across skin in topical drug applications that target the viable epidermal layer, and permeation enhancement by chemical and electrical means. The complex and changeable nature of the skin barrier makes it difficult to assess and characterize the critical parameters that influence skin permeation. The systematic and mechanistic approaches taken by Dr. Higuchi in studying these parameters provided fundamental knowledge in this area and had a measured and lasting influence upon this field of study. This article specifically reviews the validation and characterization of the polar permeation pathway, the mechanistic model of skin transport, the influence of the dermis on the target skin concentration concept, and iontophoretic transport across the polar pathway of skin including the effects of electroosmosis and electropermeabilization.

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Section: Mechanistic Model Of Skin Transportmentioning

confidence: 99%

Passive and Iontophoretic Transport through the Skin Polar Pathway

Peck

2013

Skin Pharmacol Physiol

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“…19,20 More specifically, enhancing SC permeability by targeting specific SC lipids has long been the strategy used in the design of transdermal systems. 21,22 Silver-and gold-based metal nanoparticles have been shown in the literature to permeate the skin. However, due to different experimental parameters and the limited number of studies, a definite conclusion regarding their permeation ability cannot be drawn with simplicity.…”

Section: Hsiao Et Almentioning

confidence: 99%

Enhancing the in vivo transdermal delivery of gold nanoparticles using poly(ethylene glycol) and its oleylamine conjugate

Hsiao

Peng

Tang

et al. 2016

IJN

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In this study, we investigated the effect of (ethylene glycol) (PEG) and PEG–oleylamine (OAm) functionalization on the skin permeation property of gold nanoparticles (GNS) in vivo. Chemisorption of polymers onto GNS was verified by a red shift in the ultraviolet–visible spectrum as well as by a change in the nanoparticle surface charge. The physicochemical properties of pristine and functionalized nanoparticles were analyzed by ultraviolet–visible spectroscopy, zeta potential analyzer, and transmission electron microscopy. Transmission electron microscopy revealed that the interparticle distance between nanoparticles increased after GNS functionalization. Comparing the skin permeation profile of pristine and functionalized GNS, the follicular deposition of GNS increased twofold after PEG–OAm functionalization. Moreover, PEG- and PEG–OAm-functionalized nanoparticles were able to overcome the skin barrier and deposit in the deeper subcutaneous adipose tissue. These findings demonstrate the potential of PEG- and PEG–OAm-functionalized GNS in serving a multitude of applications in transdermal pharmaceuticals.

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“…Every formulation (formulations [1][2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18][19][20] were prepared mixing evenly 500 mg of albumin (as active ingredient) with 2 or 4 mL of each solvent of table 1 and 2 (as enhancers), to make a lotion, using mechanical overhead mixer (Heidolph, RZR 2020, Germany) at 3000 rpm for 20 minutes.…”

Section: Preparation Of Formulationsmentioning

confidence: 99%

“…It binds water, cations (such as Ca 2+ , Na + and K + ), fatty acids, etc. Albumin and other nutrient proteins have been used in many cosmetic products and albumin is sometimes used as a surfactant [16][17][18][19][20] . Also we considered the albumin as a model protein.…”

Section: Introductionmentioning

confidence: 99%

Untitled

2014

IJPSR

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ABSTRACT:Objectives: Transdermal drug delivery suggests several advantages and has been vastly investigated over last decades. Chemical enhancers improve the quantity of drug penetration through the skin. In this study, hydrophilic solvents have been used as enhancers to promote dermal penetration of albumin. Methods: 20 different formulations containing albumin and hydrophilic solvents were prepared. Transdermal absorption experiments for each formulation were performed using a diffusion cell and a slice of chicken skin as model at 32°C for 3 hours. Samples from the medium were withdrawn and analyzed for albumin concentration. Cumulative amounts of albumin were plotted for each formulation. Results: After 3 hours, 6.8, 5.8, 69.0, 7.9, 11.1, 25.2, 32.0, 98.0, 21.3 and 74.3 mg of albumin were passed through the skin, using formulations containing deionized water (DW), acetic acid, ethyl acetate (EA), methanol, ethanol, 2-propanol, isopropyl alcohol (IPA), glycerol, ethylene glycol (EG) and propylene glycol (PG), respectively. Conclusion: PG, EA and glycerol could act as enhancers for transdermal delivery of albumin. Such delivery was increased using 4 mL of them instead of 2 mL and using exposure time of 3 hours instead of 1.5 hours. The most effective enhancer was found glycerol, showing a maximum albumin permeation of 98.0 mg. Therefore, the study suggested using glycerol as enhancer for transdermal delivery of albumin or other similar proteins in cosmeceutical products.

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Structure–Activity Relationship for Chemical Skin Permeation Enhancers: Probing the Chemical Microenvironment of the Site of Action

Cited by 46 publications

References 32 publications

Passive and Iontophoretic Transport through the Skin Polar Pathway

Passive and Iontophoretic Transport through the Skin Polar Pathway

Enhancing the in vivo transdermal delivery of gold nanoparticles using poly(ethylene glycol) and its oleylamine conjugate

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