Estimating Maximal In Vitro Skin Permeation Flux from Studies Using Non-sink Receptor Phase Conditions

Yousef, Shereen; Liu, Xin; Mostafa, Ahmed; Mohammed, Yousuf; Grice, Jeffrey E.; Anissimov, Yuri German; Sakran, Wedad; Roberts, Michael S.

doi:10.1007/s11095-016-1955-8

Cited by 20 publications

(7 citation statements)

References 43 publications

(47 reference statements)

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“…Animal models such as rat, mouse and rabbit have a weaker barrier than human skin and their use tends to over-estimate skin permeation relative to humans. In addition, experimental parameters such as the appropriate choice of receptor solutions that do not damage skin membranes, while providing sufficient receptor phase solubility to achieve sink conditions and suitable hydrodynamics to limit the formation of aqueous diffusion layers [ 52 ] need to be scrutinized, along with validated analytical methods and application protocols. In some cases high proportions of alcohols [ 53 , 54 , 55 , 56 , 57 ] or other known penetration enhancers such as DMSO [ 58 ] have been used to provide sink conditions in the receptor phase, with the potential to compromise the skin barrier and lead to over-estimation of drug flux.…”

Section: Skin Delivery From Nano and Microemulsionsmentioning

confidence: 99%

“…In some cases high proportions of alcohols [ 53 , 54 , 55 , 56 , 57 ] or other known penetration enhancers such as DMSO [ 58 ] have been used to provide sink conditions in the receptor phase, with the potential to compromise the skin barrier and lead to over-estimation of drug flux. Our work has also shown that even when non-sink conditions are used in in vitro permeation experiments, the results can be corrected to derive the equivalent sink condition data, provided the effects of aqueous diffusion layers are minimised [ 52 ].…”

Section: Skin Delivery From Nano and Microemulsionsmentioning

confidence: 99%

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Topical Nano and Microemulsions for Skin Delivery

et al. 2017

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Nanosystems such as microemulsions (ME) and nanoemulsions (NE) offer considerable opportunities for targeted drug delivery to and via the skin. ME and NE are stable colloidal systems composed of oil and water, stabilised by a mixture of surfactants and cosurfactants, that have received particular interest as topical skin delivery systems. There is considerable scope to manipulate the formulation components and characteristics to achieve optimal bioavailability and minimal skin irritancy. This includes the incorporation of established chemical penetration enhancers to fluidize the stratum corneum lipid bilayers, thus reducing the primary skin barrier and increasing permeation. This review discusses nanosystems with utility in skin delivery and focuses on the composition and characterization of ME and NE for topical and transdermal delivery. The mechanism of skin delivery across the stratum corneum and via hair follicles is reviewed with particular focus on the influence of formulation.

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Section: Skin Delivery From Nano and Microemulsionsmentioning

confidence: 99%

Section: Skin Delivery From Nano and Microemulsionsmentioning

confidence: 99%

Topical Nano and Microemulsions for Skin Delivery

et al. 2017

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“…Purity [19]) from the slope of the best-fit linear plot of the cumulative amount of the drug permeated per unit area versus time where flux is expressed as:…”

Section: Compoundmentioning

confidence: 99%

Permeation of pharmaceutical compounds through silicone membrane in the presence of surfactants

Bhuiyan

Waters

2017

Colloids and Surfaces A: Physicochemical and Engineering Aspect

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This study reports the effect of surfactant charge and concentration on the permeation of four model compounds (benzocaine, benzotriazole, ibuprofen and lidocaine). Surfactant charge was systematically varied using a range of surfactants that are known to possess specific head group charges, namely an anionic, a cationic, a zwitterionic and a neutral form over a series of surfactant concentrations, i.e. where possible, both above, and below, the critical micellar concentration for each surfactant. It was found that there was almost always a systematic reduction in permeation as the concentration of surfactant increased despite the wide range of physicochemical properties exhibited by the four model compounds studied. Overall, it was concluded that the presence of surfactant does generally seem to reduce permeation, regardless of the compound in question, and that the effect is surfactant concentration, as well as charge, dependent.

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“…It is very important to select a receptor fluid that maintains the sink condition in the receptor chamber (Yousef et al, 2016). 5.…”

Section: Preparation Of Membranes For In Vitro Skin Permeation Studiesmentioning

confidence: 99%

Stepwise Protocols for Preparation and Use of Porcine Ear Skin for in Vitro Skin Permeation Studies Using Franz Diffusion Cells

et al. 2022

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The skin, the largest organ of the body, is an attractive route of topical and systemic drug administration. During the development of topical formulations, in vitro skin permeation studies using biological membranes mounted in Franz diffusion cells are a useful tool to assess the permeation of substances through the skin, and are recommended by the Organization for Economic Cooperation and Development (OECD). Among the types of biological membranes used in such studies, porcine ear skin has been identified as the most promising, due to its similarities to human skin and its greater accessibility as compared to human skin. To standardize techniques for the preparation and use of porcine ear skin as biological membrane, here we present systematic procedures for the selection of porcine ears, their cleaning, the removal of skin from cartilage, its transformation into membranes, and its use for the in vitro assessment of the permeation of drugs from topical formulations. © 2022 Wiley Periodicals LLC. Basic Protocol 1: Obtaining porcine ear membranes Basic Protocol 2: Preparation of membranes from porcine ear skin and use of membranes for in vitro skin permeation studies

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Estimating Maximal In Vitro Skin Permeation Flux from Studies Using Non-sink Receptor Phase Conditions

Abstract: Non-sink receptor phase IVPT data can be used to derive equivalent sink receptor phase IVPT data provided the receptor phase solubility and hydrodynamics are sufficient to minimise the impact of aqueous diffusion layers on IVPT data.

Cited by 20 publications

References 43 publications

Topical Nano and Microemulsions for Skin Delivery

Topical Nano and Microemulsions for Skin Delivery

Permeation of pharmaceutical compounds through silicone membrane in the presence of surfactants

Stepwise Protocols for Preparation and Use of Porcine Ear Skin for in Vitro Skin Permeation Studies Using Franz Diffusion Cells

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