Human skin sandwich for assessing shunt route penetration during passive and iontophoretic drug and liposome delivery

Essa, Ebtessam A.; Bonner, Michael; Barry, Brian W.

doi:10.1211/002235702135

Cited by 79 publications

(55 citation statements)

References 36 publications

(35 reference statements)

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“…However, researchers reported that the skin penetration was influenced by the existence of hair follicles. [15][16][17] The steady-state penetration rate of model drugs through appendage-free skin of hairless rat was two to four times larger than that of normal skin. 15) Aim of our research isn't to indicate the importance of appendage but is to show the correlation between the penetration parameters through LabCyte and HLM skin.…”

Section: Resultsmentioning

confidence: 99%

Prediction of Percutaneous Absorption in Human Using Three-Dimensional Human Cultured Epidermis LabCyte EPI-MODEL

Hikima

Kaneda

Matsuo

et al. 2012

Biological & Pharmaceutical Bulletin

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The objective of this study is to establish a relationship of the skin penetration parameters between the three-dimensional cultured human epidermis LabCyte EPI-MODEL (LabCyte) and hairless mouse (HLM) skin penetration in vitro and to predict the skin penetration and plasma concentration profile in human. The skin penetration experiments through LabCyte and HLM skin were investigated using 19 drugs that have a different molecular weight and lipophilicity. The penetration flux for LabCyte reached 30 times larger at maximum than that for HLM skin. The human data can be estimated from the in silico approach with the diffusion coefficient (D), the partition coefficient (K) and the skin surface concentration (C) of drugs by assuming the bi-layer skin model for both LabCyte and HLM skin. The human skin penetration of β-estradiol, prednisolone, testosterone and ethynylestradiol was well agreed between the simulated profiles and in vitro experimental data. Plasma concentration profiles of β-estradiol in human were also simulated and well agreed with the clinical data. The present alternative method may decrease human or animal skin experiment for in vitro skin penetration.Key words in silico correlation; reconstructed epidermis; LabCyte EPI-MODEL; hairless mouse Human skin permeability of drugs in vivo can be estimated from in vitro experiment using human skin. However, some researchers have ethical and cultural difficulty to get human skins. Thus, animal skins have been widely used for pharmaceutical, toxicological and cosmetic R&D although the skins have a species difference between human. Recently, the 7th Amendment of the EC Cosmetic Directive prohibits the sale of cosmetics and ingredients validated their safety by animal testing with an alternative method. 1) Thus, researchers utilize reconstructed human skin instead of animal skin. The experiments used reconstructed epidermis is approved by the European Centre for the Validation of Alternative Methods (ECVAM) as the scientifically validated methods for skin corrosion and irritation. 2,3) Permeability studies with Episkin ® , EpiDerm TM and SkinEthic ® comparison to human and animal skin were investigated and the authors reported that the penetration flux through the reconstructed skin was higher than that of skin. [4][5][6] The OECD regulations accepted the results from the reconstructed skin 7) but don't approve it as an alternative method for in vitro human skin penetration experiment yet.Skin penetration is widely expressed by the mathematical models on the basis of the process of diffusion and dissolution. Penetration parameters, diffusion coefficient D [cm 2 /s] and partition coefficient K [-], through stratum corneum (SC) and viable skin (VS) of hairless mouse skin are found to well agree with that of human skin. 8) Not only the skin penetration profile but the blood concentration profile in human is well simulated using the penetration parameters determined from hairless mouse skin, the thickness of human SC and VS, the skin enzymatic parameters (first-ord...

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Section: Resultsmentioning

confidence: 99%

Prediction of Percutaneous Absorption in Human Using Three-Dimensional Human Cultured Epidermis LabCyte EPI-MODEL

Hikima

Kaneda

Matsuo

et al. 2012

Biological & Pharmaceutical Bulletin

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“…In the last decade, several methods were developed to investigate follicular penetration selectively [17,42,43]. In the present study, the method of differential stripping has been utilized to differentiate the penetration of an aqueous sodium fluorescein solution into the stratum corneum and the hair follicle in different ethnic groups.…”

Section: Discussionmentioning

confidence: 99%

Ethnic Differences in Skin Physiology, Hair Follicle Morphology and Follicular Penetration

Luther

Darvin²,

Sterry³

et al. 2012

Skin Pharmacol Physiol

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Background/Aims: Inconsistent evidence is available that different ethnic groups exhibit differences in skin physiological parameters. Recently, variations in hair follicle morphology have been described, although the influence of such variations on the follicular penetration process has not been investigated until now. Methods: The aim of the present study was thus to investigate skin physiological parameters, follicle morphology and the penetration process in different ethnic groups. Results and Conclusion: Whereas no significant differences with regard to skin physiological parameters could be observed, morphological analysis of the hair follicles revealed, inter alia, that Caucasians had significantly larger terminal hair follicles than Asians and Africans. The surface of the hair follicle infundibulum was shown to be 3% in Caucasians, 2.6% in Africans and 2.4% in Asians. The investigations into penetration revealed no significant differences after a 30-min penetration time, whereas after 24 h, the Asian volunteers presented significantly larger amounts of sodium fluorescein in the hair follicles and the stratum corneum, which may be explained by cultural habits.

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“…It has already been postulated that certain molecules can hydrogen bond to groups present on the surfaces of follicular pores [75]. However, more studies have to be made in order to identify all the molecular properties that influence drug penetration into hair follicles.…”

Section: Routes Of Drug Penetration Through the Skinmentioning

confidence: 99%

“…In other investigations, it has been shown by differential stripping the influence of size microparticles in the skin penetration. It can act as efficient drug carriers or can be utilized as follicle blockers to stop the penetration of topically applied substances [75]. An alternative technique is multiphoton microscopy (MPM) especially two-photon excitation microscopy has been widely used in imaging biological specimens treated with nanoparticles [111][112][113][114].…”

Section: Advantages and Limitations Of Using Nanocarriers For Transdementioning

confidence: 99%

Nanocarrier Systems for Transdermal Drug Delivery

Escobar-Chávez¹,

Rodríguez-Cruz²,

Domínguez-Delgado³

et al. 2012

Recent Advances in Novel Drug Carrier Systems

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is an open discussion, in one hand, the nanotechnologist continue making new and more sophisticated nanocarriers and in the other hand, toxicologist continue evaluating possible damaging effects.Whatever it happens, nanotechnology is the new era and nanomedicine cannot be taking off. New nanocarriers will be created and the entire scientist working in nanomedicine bet for it to be the cure of diseases that in this moment are difficult to deal with [3] The application of preparations to the skin for medical purposes is as old as the history of medicine itself, with references to the use of ointments and salves found in the records of Babylonian and Egyptian medicine. The historical development of permeation research is well described by Hadgraft & Lane [4]. Over time, the skin has become an important route for drug delivery in which topical, regional or systemic effects are desired. Nevertheless, skin constitutes an excellent barrier and presents difficulties for the transdermal delivery of therapeutic agents, since few drugs possess the characteristics required to permeate across the stratum corneum in sufficient quantities to reach a therapeutic concentration in the blood. In order to enhance drug transdermal absorption different methodologies have been investigated developed and patented [5,6]. Improvement in physical permeationenhancement technologies has led to renewed interest in transdermal drug delivery. Some of these novel advanced transdermal permeation enhancement technologies include: iontophoresis, electroporation, ultrasound, microneedles to open up the skin and more recently the use of transdermal nanocarriers [3,[7][8][9][10].A number of excellent reviews that have been published contain detailed discussions concerning many aspects of transdermal nanocarriers [11][12][13][14][15][16][17]. The present chapter shows an updated overview of the use of submicron particles and other nanostructures in the pharmaceutical field, specifically in the area of topical and transdermal drugs. This focus is justified due to the magnitude of the experimental data available with the use of these nanocarriers. The development of submicron particles and other nanostructures in the pharmaceutical and cosmetic fields has been emerged in the last decades for designing best formulations for application through the skin [18][19][20][21]. The skinThe skin is the largest organ of the body [22][23][24], accounting for more than 10% of body mass, and the one that enables the body to interact more intimately with its environment. Essentially, the skin consists of four layers: The SC, that is the outer layer of the skin (nonviable epidermis), and forms the rate-controlling barrier for diffusion for almost all compounds. It is composed of dead flattened, keratin-rich cells, the corneocytes. These dense cells are surrounded by a complex mixture of intercellular lipids, namely, ceramides, free fatty acids, cholesterol, and cholesterol sulphate. Their most important feature is that they are structured as ordered bilayer arrays [25]...

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Human skin sandwich for assessing shunt route penetration during passive and iontophoretic drug and liposome delivery

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Cited by 79 publications

References 36 publications

Prediction of Percutaneous Absorption in Human Using Three-Dimensional Human Cultured Epidermis LabCyte EPI-MODEL

Prediction of Percutaneous Absorption in Human Using Three-Dimensional Human Cultured Epidermis LabCyte EPI-MODEL

Ethnic Differences in Skin Physiology, Hair Follicle Morphology and Follicular Penetration

Nanocarrier Systems for Transdermal Drug Delivery

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