Effects of Isopropanol–Isopropyl Myristate Binary Enhancers on In Vitro Transport of Estradiol in Human Epidermis: A Mechanistic Evaluation

Liu, Puchun; Cettina, Melinda; Wong, Judy M.Y.

doi:10.1002/jps.21459

Cited by 22 publications

(10 citation statements)

References 25 publications

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“…The data show that highest skin uptake was obtained for TC and DMI ( P > 0.05), whereas IPM had the lowest estimated value ( P < 0.05). The uptake of IPM determined in human SC is in line with published data .…”

Section: Resultssupporting

confidence: 88%

The role of vehicle interactions on permeation of an active through model membranes and human skin

Oliveira

Hadgraft

Lane

2012

Intern J of Cosmetic Sci

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Previous work from this group has focused on the molecular mechanism of alcohol interaction with model membranes, by conducting thermodynamic and kinetic analyses of alcohol uptake, membrane partitioning and transport studies of a model compound (i.e. methyl paraben) in silicone membranes. In this article, similar membrane transport and partitioning studies were conducted in silicone membranes to further extend the proposed model of alcohol interactions with silicone membranes to include other vehicles more commonly used in dermal formulations, that is, isopropyl myristate (IPM), dimethyl isosorbide (DMI), polyethylene glycol (PEG) 200, PEG 400 and Transcutol P® (TC). More importantly, membrane partitioning studies were conducted using human SC to evaluate the application of the proposed model of solvent-enhanced permeation in simple model membranes for the more complex biological tissue. The findings support a model of vehicle interactions with model membranes and skin where high solvent uptake promotes drug partitioning (i.e. K) by enabling the solute to exist within the solvent fraction/solvent-rich areas inside the membrane or skin in a concentration equivalent to that in the bulk solvent/vehicle. High solvent sorption may also ultimately impact on the membrane diffusional characteristics, and thus the diffusion coefficient of the solute across the membrane. The implications for skin transport are that increased partitioning of a drug into the SC may be achieved by (i) selecting vehicles that are highly taken up by the skin and also (ii) by having a relatively high concentration (i.e. molar fraction) of the drug in the vehicle. It follows that, in cases where significant co-transport of the solvent into and across the skin may occur, its depletion from the formulation and ultimately from the skin may lead to drug crystallization, thus affecting dermal absorption.

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Section: Resultssupporting

confidence: 88%

The role of vehicle interactions on permeation of an active through model membranes and human skin

Oliveira

Hadgraft

Lane

2012

Intern J of Cosmetic Sci

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“…Greater partitioning and higher skin retention was demonstrated for IPM compared with alkanols by Goldberg-Cettina et al (1995). Liu et al (2009) investigated the effects of IPM on estradiol skin permeation and noted that IPM uptake could be correlated with drug diffusivity in skin. The authors also demonstrated swelling of the SC in the presence of IPM.…”

Section: Accepted Manuscriptmentioning

confidence: 99%

Topical delivery of anthramycin I. Influence of neat solvents

Haque¹,

Rahman

Thurston

et al. 2017

European Journal of Pharmaceutical Sciences

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Anthramycin (ANT) was the first pyrrolobenzodiazepine (PBD) molecule to be isolated, and is a potent cytotoxic agent. Although the PBD family has been investigated for use in systemic chemotherapy, their application in the management of actinic keratoses (AK) or skin cancer has not been investigated to date. In the present work, anthramycin (ANT) was selected as a model PBD compound, and the skin penetration of the molecule was investigated using conventional Franz diffusion cells. Finite dose permeation studies of ANT were performed using propylene glycol (PG), 1,3-butanediol (BD), dipropylene glycol (DiPG), Transcutol P® (TC), propylene glycol monocaprylate (PGMC), propylene glycol monolaurate (PGML) and isopropyl myristate (IPM). The skin penetration of BD, DiPG, PG and TC was also measured. Penetration of ANT through human skin was evident for TC, PG and PGML with the active appearing to "track" the permeation of the vehicle in the case of TC and PG. Deposition of ANT in skin could be correlated with skin retention of the vehicle in the case of IPM, PGMC and PGML. These preliminary findings confirm the ability of ANT to penetrate human skin and, given the potency of the molecule, suggest that further investigation is justified. Additionally, the findings emphasise the critical importance of understanding the fate of the excipient for the rational design of topical formulations.

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“…Representative physical enhancers are iontophoresis , sonophoresis , electroporation , and microneedles . Chemical enhancers include some fatty acids , terpenes , esters , alcohols , peptides , and nanosized carriers such as lipid vesicles , and solid‐in‐oil (S/O) nanodispersions . With either type of enhancer, crossing the stratum corneum, the outermost layer in the skin, is the key to efficient transdermal drug delivery .…”

Section: Introductionmentioning

confidence: 99%

Solid‐in‐oil nanodispersions for transdermal drug delivery systems

Kitaoka

Wakabayashi

Kamiya

et al. 2016

Biotechnology Journal

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Transdermal administration of drugs has advantages over conventional oral administration or administration using injection equipment. The route of administration reduces the opportunity for drug evacuation before systemic circulation, and enables long‐lasting drug administration at a modest body concentration. In addition, the skin is an attractive route for vaccination, because there are many immune cells in the skin. Recently, solid‐in‐oil nanodisperison (S/O) technique has demonstrated to deliver cosmetic and pharmaceutical bioactives efficiently through the skin. S/O nanodispersions are nanosized drug carriers designed to overcome the skin barrier. This review discusses the rationale for preparation of efficient and stable S/O nanodispersions, as well as application examples in cosmetic and pharmaceutical materials including vaccines. Drug administration using a patch is user‐friendly, and may improve patient compliance. The technique is a potent transcutaneous immunization method without needles.

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Effects of Isopropanol–Isopropyl Myristate Binary Enhancers on In Vitro Transport of Estradiol in Human Epidermis: A Mechanistic Evaluation

Cited by 22 publications

References 25 publications

The role of vehicle interactions on permeation of an active through model membranes and human skin

The role of vehicle interactions on permeation of an active through model membranes and human skin

Topical delivery of anthramycin I. Influence of neat solvents

Solid‐in‐oil nanodispersions for transdermal drug delivery systems

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