Microemulsion Microstructure Influences the Skin Delivery of an Hydrophilic Drug

Naoui, W.; Bolzinger, Marie‐Alexandrine; Fenêt, Bernard; Pelletier, Jocelyne; Valour, Jean‐Pierre; Kalfat, Rafik; Chevalier, Yves

doi:10.1007/s11095-011-0404-y

Cited by 52 publications

(36 citation statements)

References 41 publications

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“…It was seen (Table 4.4) that the highest permeability of naproxen was obtained from OA and EU nanoemulsion formulations, which may be due to high solubility of naproxen in the stratum corneum from these formulations compared with controls. Naoui et al found significant differences in the amount of caffeine stored in the stratum corneum (202). It was previously claimed that diffusional resistance in the dermal matrix could significantly decrease the permeability of lipophilic solutes (203).…”

Section: Discussionmentioning

confidence: 99%

“…The O/W nanoemulsion is conductive, however, W/O emulsions show much greater resistance. Therefore, the conductivity switched between two plateaus corresponding to water-continuous and oil-continuous structure (202).…”

Section: Electrical Conductivity (Ec)mentioning

confidence: 99%

“…It is well established that the uppermost layer of the skin, the stratum corneum, is the main barrier to such penetration but can be overcome to Microemulsions, defined as single phase and thermodynamically stable isotropic systems composed of water, oil and amphiphilic molecules (170), are attractive systems for enhancing drug delivery to the skin because of their ease of formulation, thermodynamic stability and solubilisation (171). They are capable of incorporating and enhancing the skin delivery of both hydrophilic and lipophilic drugs (172,173) and are considered to be more stable than conventional emulsions because of their small droplet sizes preventing phase separation.…”

Section: Introductionmentioning

confidence: 99%

“…Mostly, these advanced formulations have been used topically. It is believed that drug permeation rates from nanoemulsions are significantly higher than from other formulations such as conventional emulsions and vehicles because the nanoemulsions combine several enhancing components (202). Nanoemulsions are a dispersed system of oil, water, surfactant and co-surfactant.…”

Section: Introductionmentioning

confidence: 99%

“…One of these theories claimed that contact of the drug with the skin could be improved by low interfacial tension between oil and water (176). The bioavailability of the drug increases due to the low interfacial tension and the fluctuating oil-water interface, which enhances material movement between lipophilic and hydrophilic domains of the nanoemulsion and the stratum corneum (202).…”

Section: Introductionmentioning

confidence: 99%

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Targeted skin delivery of topically applied drugs by optimised formulation design

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Early research concentrated on the relationship between a solute's physicochemical properties and its skin permeation, mostly from simple solutions. Relatively less is known about how vehicles, particularly complex ones, might also affect skin permeation by altering the properties of the skin, although this is an area that has attracted much interest. Key requirements for topical delivery is understanding the relationships between drug-vehicle, drug-skin or drug -vehicle -skin interaction. In this project, understanding this relationship was crucial to designing novel formulations able to deliver drugs with different lipophilicity topically or systemically. The first aim was to explore the impact of various solution compositions on skin permeation of some model drugs. I compared in vitro maximum penetration fluxes (Jmax) and solubilities of the vehicles (Sv) and of the stratum corneum (SSC) and derived diffusivities (D*) for four drugs (caffeine, minoxidil, lidocaine and naproxen) having a range of lipophilicities. I used a range of solvent vehicles that were hypothesised to affect the skin to differing degrees to evaluate vehicle effects on permeability parameters.If neither the vehicle nor the solute alters the properties of the skin, maximum (or saturated) solute flux is independent of both the vehicle composition and the solute's saturated solubility in that vehicle. These findings were confirmed in this study for all four drugs used.The permeation of caffeine, minoxidil, lidocaine and naproxen were found to be selectively enhanced by vehicles containing specific excipients that were hypothesised to alter the properties of the skin. The greatest effects were seen on flux and diffusivity by the eucalyptol (EU) and oleic acid (OA) vehicles on the more hydrophilic compounds, caffeine and minoxidil. We concluded that enhanced solute fluxes were mainly driven by increased diffusivity in the stratum corneum.I also examined the extent of skin permeation enhancement of the hydrophilic drug caffeine and lipophilic drug naproxen applied in nanoemulsions incorporating skin penetration enhancers. Infinite doses of fully characterised oil-in-water nanoemulsions containing the skin penetration enhancers oleic acid or eucalyptol as oil phases and caffeine (3%) or naproxen (2%) were applied to full-thickness skin and human epidermal membranes in Franz diffusion cells, along with aqueous control solutions. Caffeine and naproxen fluxes were determined over 8 h. Solute solubility in the formulations and in the stratum corneum, as well as the uptake of product components into the stratum corneum were measured.The nanoemulsions significantly enhanced the skin penetration of caffeine and naproxen compared to aqueous control solutions. The maximum flux enhancement of caffeine was III associated with a synergistic increase in both its solubility in the stratum corneum and skin diffusivity. Enhanced skin penetration in these systems is largely driven by uptake of formulation excipients containing the active compounds into th...

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Section: Discussionmentioning

confidence: 99%

Section: Electrical Conductivity (Ec)mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Targeted skin delivery of topically applied drugs by optimised formulation design

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Development of model systems for in vitro investigation of transdermal transport pathways

et al. 2017

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Skin is a complex structured system primarily involved in Transdermal Drug Delivery (TDD). The outer stratum corneum represents the main barrier to the entrance of external molecules. Nowadays, none of the recognized methods, used for the investigation of penetration processes, is able to give a complete overview of the transport mechanisms involved. Standard protocols are based on the use of human or animal skin samples, which are difficult and expensive to obtain. Here, we present a novel experimental setup to investigate TDD by using Confocal Laser Scanning Microscopy and image analysis. The methodology is based on diffusion experiments of fluorescent‐labelled fluids (water, oil, and oil‐in‐water emulsions), in a model matrix. Using an agarose gel as model for a proof of concept, different penetration efficiencies were observed, suggesting an important role of both chemical composition and fluid microstructure on the transport mechanism. An adequate model system should be used to better mimic the stratum corneum morphology and properties. To this aim, several bicontinuous emulsion gels, obtained from an emulsification process, were preliminary formulated and suggested as model systems to mimic the stratum corneum. In this work, we define the key directions for the development of an innovative approach to study the penetration of formulations through the skin.

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Probing Location of Anti-TB Drugs Loaded in Brij 96 Microemulsions Using Thermoanalytical and Photophysical Approach

Kaur

Mehta

2014

Journal of Pharmaceutical Sciences

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Microemulsion Microstructure Influences the Skin Delivery of an Hydrophilic Drug

Abstract: The structure of microemulsions is of relevance for skin absorption. The water-continuous structures allow faster transport of hydrophilic drugs.

Cited by 52 publications

References 41 publications

Targeted skin delivery of topically applied drugs by optimised formulation design

Targeted skin delivery of topically applied drugs by optimised formulation design

Development of model systems for in vitro investigation of transdermal transport pathways

Probing Location of Anti-TB Drugs Loaded in Brij 96 Microemulsions Using Thermoanalytical and Photophysical Approach

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