The influence of drug partition coefficient on follicular penetration: In vitro human skin studies

Frum, Yakov; Bonner, Michael; Eccleston, Gillian M.; Meidan, Victor M.

doi:10.1016/j.ejps.2006.11.014

Cited by 55 publications

(42 citation statements)

References 27 publications

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“…While there was a similar overall relationship between increased penetration and a higher partition coefficient, the authors also found that the partition coefficient would only have a significant impact on penetration above a critical value. Below this critical value, however, other factors were responsible for dictating the degree of penetration [28] .…”

Section: Discussionmentioning

confidence: 97%

“…In an in vitro study by Frum et al [28] , a novel skin sandwich system was utilized to examine the relationship between percent follicular penetration of a drug and partition coefficient. While there was a similar overall relationship between increased penetration and a higher partition coefficient, the authors also found that the partition coefficient would only have a significant impact on penetration above a critical value.…”

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Role of Physical Chemical Properties in Drug Relay into Skin Compartments

Fortenbach

Modjtahedi

Maibach

2008

Skin Pharmacol Physiol

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The ability of a drug to reach the interstitial fluid is an important aspect of drug efficacy – as a possible indicator of skin and cell compartment concentration. This overview addresses the relationship of the physical properties of several antibiotics to their ability to enter the interstitial fluid utilizing a cantharidin blister model. By collecting pharmacokinetic data for 12 antibiotics administered orally and 11 intravenously, we compared the fraction of drug that reaches the interstitial fluid (AUC_blister/AUC_serum) to partition coefficients. Following data analysis, we found no correlation (p = 0.98 and 0.09, respectively) between hydrophobicity and the ability to reach the interstitium. Both orally and intravenously administered antibiotics display a strong linear correlation (p < 0.001 and p = 0.006, respectively) in the total concentration found in the serum and interstitial fluid indicating that serum concentration may be an important factor in dictating interstitial fluid concentration. This correlation may prove useful in clinical application as a means of determining interstitial fluid concentration by measuring only serum levels.

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Section: Discussionmentioning

confidence: 97%

Section: Discussionmentioning

confidence: 99%

Role of Physical Chemical Properties in Drug Relay into Skin Compartments

Fortenbach

Modjtahedi

Maibach

2008

Skin Pharmacol Physiol

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“…Comparing the findings of our own research to those of international studies [35,51,52], it seems unrealistic that drug delivery by nanoparticles ≥40 nm through the intact skin barrier can be realized. Nevertheless, the pharmacological importance of nanoparticles for drug delivery, in the fields of dermatology and cosmetology, should not be underestimated.…”

Section: Triggered Release Of Drugs From Nanoparticlesmentioning

confidence: 49%

Drug Delivery with Topically Applied Nanoparticles: Science Fiction or Reality?

Lademann

Richter

Meinke

et al. 2013

Skin Pharmacol Physiol

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The efficacy of topically applied drugs is determined by their action mechanism and their potential capacity of passing the skin barrier. Nanoparticles are assumed to be efficient carrier systems for drug delivery through the skin barrier. For flexible nanoparticles like liposomes, this effect has been well demonstrated. The penetration properties of solid nanoparticles are currently under intensive investigation. The crucial advantage of nanoparticles over non-particulate substances is their capability to penetrate deeply into the hair follicles where they can be stored for several days. There is no evidence, yet, that solid particles ≥40 nm are capable of passing through the healthy skin barrier. Therefore and in spite of the long-standing research efforts in this field, commercially available solid nanoparticle-based products for drug delivery through the healthy skin are still missing. Nevertheless, the prospects for the clinical use of nanoparticles in drug delivery are tremendous. They can be designed as transport systems delivering drugs efficiently into the hair follicles in the vicinity of specific target structures. Once deposited at these structures, specific signals might trigger the release of the drugs and exert their effects on the target cells. In this article, examples of such triggered drug release are presented.

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“…131 Others suggested that there is a critical value of octanol/water partition coefficient beyond which the flux through the follicle is greatly diminished. 132 However, most studies omit the significance of sebum (a lipophilic product of the sebaceous gland) during drug delivery due to lack of representative experimental models. The presence of sebum in the HF and its upward flow may hinder the delivery of hydrophilic compounds and may favor the delivery of hydrophobic compounds.…”

Section: Drug Delivery Through the Hfmentioning

confidence: 99%