A Study on the Influence of Emulsion Droplet Size on the Skin Penetration of Tetracaine

Izquierdo, Paqui; Wiechers, Johann W.; Escribano, Elvira; García-Celma, María José; Tadros, Tharwat F.; Esquena, Jordi; Dederen, J. C.; Solans, Conxita

doi:10.1159/000106076

Cited by 39 publications

(26 citation statements)

References 32 publications

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“…5 mALA also shows less of an inflammatory response in skin compared with its parent form. 13,14 Oil-in-water (O/W) and water-in-oil (W/O) emulsions are used in clinical studies, all with therapeutic success in dermatology. The primary aim of this study was to develop and evaluate O/W and W/O nanoemulsions to increase the absorption of ALA and mALA.…”

Section: Introductionmentioning

confidence: 99%

“…23 For nanocarriers, issues such as the thermodynamic activity of the permeant relative to the vehicle are very important, as they determine the push into the skin. 13 Differences in the internal structure of the emulsions can modify the thermodynamic activity of ALA, which could favor its partitioning into the SC. O/W soybean oil emulsions may provide higher thermodynamic activity for ALA and mALA than squalene-containing carriers.…”

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confidence: 99%

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Oil components modulate the skin delivery of 5-aminolevulinic acid and its ester prodrug from oil-in-water and water-in-oil nanoemulsions

Zhang

Al‐Suwayeh²,

Hung³

et al. 2011

IJN

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The study evaluated the potential of nanoemulsions for the topical delivery of 5-aminolevulinic acid (ALA) and methyl ALA (mALA). The drugs were incorporated in oil-in-water (O/W) and water-in-oil (W/O) formulations obtained by using soybean oil or squalene as the oil phase. The droplet size, zeta potential, and environmental polarity of the nanocarriers were assessed as physicochemical properties. The O/W and W/O emulsions showed diameters of 216–256 and 18–125 nm, which, respectively, were within the range of submicron- and nano-sized dispersions. In vitro diffusion experiments using Franz-type cells and porcine skin were performed. Nude mice were used, and skin fluorescence derived from protoporphyrin IX was documented by confocal laser scanning microscopy (CLSM). The loading of ALA or mALA into the emulsions resulted in slower release across cellulose membranes. The release rate and skin flux of topical drug application were adjusted by changing the type of nanocarrier, the soybean oil O/W systems showing the highest skin permeation. This formulation increased ALA flux via porcine skin to 180 nmol/cm 2 /h, which was 2.6-fold that of the aqueous control. The CLSM results showed that soybean oil systems promoted mALA permeation to deeper layers of the skin from ∼100 μm to ∼140 μm, which would be beneficial for treating subepidermal and subcutaneous lesions. Drug permeation from W/O systems did not surpass that from the aqueous solution. An in vivo dermal irritation test indicated that the emulsions were safe for topical administration of ALA and mALA.

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Section: Introductionmentioning

confidence: 99%

mentioning

confidence: 99%

Oil components modulate the skin delivery of 5-aminolevulinic acid and its ester prodrug from oil-in-water and water-in-oil nanoemulsions

Zhang

Al‐Suwayeh²,

Hung³

et al. 2011

IJN

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“…Smaller particles seem to enhance the permeation to a greater extent than larger particles [130,131,132]. However, this conclusion is contradictory since it has already been shown that for the same kind of nanoemulsion there was no influence of the emulsion droplet size on the skin penetration of the encapsulated substance when applied to dermatomed human skin [133]. In comparison to nanocapsules, the nanoemulsions present a higher capacity to penetrate and/or permeate the skin, probably due to their flexibility [132] and lack of polymer which has an affinity with the stratum corneum [33].…”

Section: Lipid Systemsmentioning

confidence: 95%

Transport of Substances and Nanoparticles across the Skin and in Vitro Models to Evaluate Skin Permeation and/or Penetration

Contri

Fiel

Pohlmann

et al. 2011

Nanocosmetics and Nanomedicines

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Abstract. Nanotechnology can be used to modify the drug permeation/penetration of encapsulated substances, through the manipulation of many different factors, including direct contact with the skin surface and controlled release. In general, nanoparticles cannot cross the skin barrier, which can be explained by the cell cohesion and lipids of the stratum corneum, the outermost skin layer. The device most commonly used to study the transport of substances and nanoparticles across the skin is the Franz vertical diffusion cell, followed by the substance quantification in the receptor fluid or determination of the amount retained in the skin. Microscopy techniques have also been applied in skin penetration or permeation experiments. This chapter will present the fundamental considerations regarding the transport of encapsulated substances and/or nanoparticles across the skin, the experimental models applied in these studies and a review of the main studies reported in the literature in order to allow the reader to gain insight into the current knowledge available in this area.

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“…(7) There is no clear consensus in the literature regarding the influence of droplet size of the microemulsion on drug permeation. A recent study by Izquierdo et al [71] showed no apparent relationship between droplet size and dermal or transdermal delivery of tetracaine after 24 h. Specific examples of each of these possible mechanisms with reference to specific drugs are discussed in more detail in later sections. …”

Section: Mechanisms Of Percutaneous Enhancementmentioning

confidence: 97%

Application of Microemulsions in Dermal and Transdermal Drug Delivery

Santos¹,

Watkinson²,

Hadgraft³

et al. 2008

Skin Pharmacol Physiol

126

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Microemulsions are thermodynamically stable colloidal dispersions of water and oil stabilized by a surfactant and, in many cases, also a cosurfactant. In the pharmaceutical field, microemulsions have been used as drug carriers for percutaneous, ocular, oral and parenteral administration. This review discusses some of the applications of microemulsions specifically for topical and transdermal applications. Microemulsion nomenclature and composition, with particular emphasis on choice of surfactant and cosurfactant, is discussed. Methods used to characterize microemulsions are reviewed. Microemulsion formulations for dermal and transdermal delivery of pharmaceutical agents with particular emphasis on anti-inflammatory and anaesthetic agents are critically evaluated. Finally, the issues which warrant further investigation by researchers in order to realize the full potential of the technology are discussed.

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A Study on the Influence of Emulsion Droplet Size on the Skin Penetration of Tetracaine

Cited by 39 publications

References 32 publications

Oil components modulate the skin delivery of 5-aminolevulinic acid and its ester prodrug from oil-in-water and water-in-oil nanoemulsions

Oil components modulate the skin delivery of 5-aminolevulinic acid and its ester prodrug from oil-in-water and water-in-oil nanoemulsions

Transport of Substances and Nanoparticles across the Skin and in Vitro Models to Evaluate Skin Permeation and/or Penetration

Application of Microemulsions in Dermal and Transdermal Drug Delivery

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