Simultaneous analysis of skin penetration of surfactant and active drug from fluorosurfactant-based microemulsions

Mahrhauser, Denise-Silvia; Hoppel, Magdalena; Schöll, Judith; Binder, Lisa; Kählig, Hanspeter; Valenta, Claudia

doi:10.1016/j.ejpb.2014.04.019

Cited by 20 publications

(15 citation statements)

References 18 publications

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“…36 The viscosity of a microemulsion is the function of the type of its components (oil, surfactant, cosurfactant, and water) and their concentrations. 37 Both microemulsions (ME1 and ME2) exhibited low viscosities, which are typically observed in microemulsions. 37 The apparent viscosity values of the microemulsions were between 70.76±0.12 and 83.58±0.46 cP, and the correlation coefficients between shear rate and shear stress were equal to 1, indicating Newtonian flow behavior as expected for microemulsion systems (Figure 2).…”

Section: Results and Discussion Preparation And Characterization Of Fmentioning

confidence: 99%

“…37 Both microemulsions (ME1 and ME2) exhibited low viscosities, which are typically observed in microemulsions. 37 The apparent viscosity values of the microemulsions were between 70.76±0.12 and 83.58±0.46 cP, and the correlation coefficients between shear rate and shear stress were equal to 1, indicating Newtonian flow behavior as expected for microemulsion systems (Figure 2). 36 The lower viscosity of ME1 compared to ME2 is in correlation with the finding that increased surfactant content can lower the viscosity of a microemulsion.…”

Section: Results and Discussion Preparation And Characterization Of Fmentioning

confidence: 99%

“…It has been reported that oleic acid fluidizes the stratum corneum intercellular lipids and induces phase separation, and thereby exerts a penetration enhancing effect. 31,37,40,41 Together with the oleic acid reported effects, the partitioning of the surfactant (Kolliphor ® EL or Kolliphor ® RH40) and the cosurfactant (Transcutol ® ) may have also contributed to the C-H symmetric and asymmetric blue shifts. The C-H symmetric stretching frequencies are known to be more susceptible to changes in lipid matrix organization.…”

mentioning

confidence: 99%

“…These data are in good agreement with our skin penetration experiments and also in accordance with the consideration that microemulsion components can interact with stratum corneum lipids and thereby facilitate drug transport across the skin barrier. 37 The type of the surfactant affected differently the permeability of the skin, and as a consequence, cutaneous drug delivery from the microemulsions. No remarkable shifts of the C-H stretching vibrations could be detected after the application of the marketed cream …”

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confidence: 99%

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Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations

Erdal¹,

Özhan²,

Mat³

et al. 2016

IJN

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In topical administration of antifungals, the drugs should pass the stratum corneum to reach lower layers of the skin in effective concentrations. Thus, the formulation of antifungal agents into a suitable delivery system is important for the topical treatment of fungal infections. Nanosized colloidal carriers have gained great interest during the recent years to serve as efficient promoters of drug penetration into the skin. Microemulsions are soft colloidal nanosized drug carriers, which are thermodynamically stable and isotropic systems. They have been extensively explored for the enhancement of skin delivery of drugs. This study was carried out to exploit the feasibility of colloidal carriers as to improve skin transport of naftifine, which is an allylamine antifungal drug. The microemulsions were formulated by construction of pseudoternary phase diagrams and composed of oleic acid (oil phase), Kolliphor ® EL or Kolliphor ® RH40 (surfactant), Transcutol ® (cosurfactant), and water (aqueous phase). The plain and drug-loaded microemulsions were characterized in terms of isotropy, particle size and size distribution, pH value, refractive index, viscosity, and conductivity. The in vitro skin uptake of naftifine from microemulsions was studied using tape stripping technique in pig skin. The drug penetrated significantly into stratum corneum from microemulsions compared to its marketed cream ( P <0.05). Moreover, the microemulsion formulations led to highly significant amount of naftifine deposition in deeper layers of skin than that of commercial formulation ( P <0.001). Microemulsion–skin interaction was confirmed by attenuated total reflectance – Fourier transformed infrared spectroscopy data, in vitro. The results of the in vivo tape stripping experiment showed similar trends as the in vitro skin penetration study. Topical application of the microemulsion on human forearms in vivo enhanced significantly the distribution and the amount of naftifine penetrated into the stratum corneum as compared to the marketed formulation ( P <0.05). The relative safety of the microemulsion formulations was demonstrated with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide viability test. This study indicated that the nanosized colloidal carriers developed could be considered as an effective and safe topical delivery system for naftifine.

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Section: Results and Discussion Preparation And Characterization Of Fmentioning

confidence: 99%

Section: Results and Discussion Preparation And Characterization Of Fmentioning

confidence: 99%

mentioning

confidence: 99%

mentioning

confidence: 99%

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Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations

Erdal¹,

Özhan²,

Mat³

et al. 2016

IJN

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“…The viscosity of a microemulsion is the function of the type of its components (oil, surfactant, co-surfactant and water) and their concentrations 35 . The viscosity of plain microemulsions was in the range of 22.15±0.06 -88.00±0.19 cPs (Table 2), and tended to increase as the amount of the oil and surfactant mixture in the formulation increased.…”

Section: Rheologymentioning

confidence: 99%

Development and in vitro characterization of microemulsions of isotretinoin

Gürbüz¹,

Güngör²,

Erdal³

2017

actapharm

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Colloidal carriers of isotretinoin for topical acne treatment: skin uptake, ATR-FTIR and in vitro cytotoxicity studies

et al. 2015

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Acne vulgaris is the chronical, multifactorial and complex disease of the pilosebaceous unit in the skin. The main goal of the topical therapy in acne is to target the drug to epidermal and deep dermal regions by minimizing systemic absorption . Isotretinoin, a retinoic acid derivative, is the most effective drug in acne pathogenesis. Because systemic treatment may cause many side effects, topical isotretinoin treatment is an option in the management of acne. However, due to its high lipophilic character, isotretinoin tends to accumulate in the upper stratum corneum, thus its penetration into the lower layers is limited, which restricts the efficiency of topical treatment. Microemulsions are fluid, isotropic, colloidal drug carriers that have been widely studied as drug delivery systems. The percutaneous transport of active agents can be enhanced by microemulsions when compared with their conventional formulations. The purpose of this study was to evaluate microemulsions as alternative topical carriers for isotretinoin with an objective to improve its skin uptake. After in vitro permeation studies, the dermal penetration of isotretinoin from microemulsions was investigated by tape stripping procedure. Confocal laser scanning microscopy provided insight about the localization of the drug in the skin. The interaction between the microemulsion components and stratum corneum lipids is studied by ATR-FTIR spectroscopy. The relative safety of the microemulsions was assessed in mouse embryonic fibroblasts using MTT viability test. The results indicate that microemulsion-based novel colloidal carriers have a potential for enhanced skin delivery and localization of isotretinoin.

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Simultaneous analysis of skin penetration of surfactant and active drug from fluorosurfactant-based microemulsions

Cited by 20 publications

References 18 publications

Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations

Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations

Development and in vitro characterization of microemulsions of isotretinoin

Colloidal carriers of isotretinoin for topical acne treatment: skin uptake, ATR-FTIR and in vitro cytotoxicity studies

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