Uptake of Microemulsion Components into the Stratum Corneum and Their Molecular Effects on Skin Barrier Function

Hathout, Rania M.; Mansour, Samar; Mortada, Nahed D.; Geneidi, Ahmed S.; Guy, Richard H.

doi:10.1021/mp100068s

Cited by 92 publications

(59 citation statements)

References 28 publications

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“…The use of Transcutol ® in topical and transdermal drug delivery has been examined widely due to its nontoxicity and optimal solubilizing parameters for a number of drugs. [29][30][31][32] It is well known that microemulsion structures are strongly dependent on the ratio of the constituents. Pseudoternary phase diagrams can be used to note the physical boundary conditions (microemulsion, liquid crystalline, micelles) of oil, surfactants, and water necessary to formulate stable formulations.…”

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.…”

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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%

mentioning

confidence: 99%

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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show abstract

“…Interestingly, two contradicting observations were found to be prevalent in this composition. Firstly, it contained the maximum amount of Tween 80 (46.67%), out of all the studied compositions, which is reported to emulsify sebum and extract skin lipids that enhance the thermodynamic coefficient of the drug, allowing it to penetrate into the cells more effectively (45,46). On the other hand, the amount of phospholipid was observed to be least in G15 (7.78%).…”

Section: Ex Vivo Skin Permeation Studiesmentioning

confidence: 97%

Benzyl Benzoate-Loaded Microemulsion for Topical Applications: Enhanced Dermatokinetic Profile and Better Delivery Promises

et al. 2015

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Abstract. Benzyl benzoate (BB) is one of the oldest drugs used for the treatment of scabies and is recommended as the "first-line intervention" for the cost-effective treatment of the disease. Though a promising candidate, its application is reported to be associated with irritation of the skin and eye, resulting in poor patient compliance. Hence, the present study aims to develop BB-loaded topical microemulsion for the safer and effective delivery of BB. Pseudo-ternary phase diagrams with BB as the oily phase itself, along with Tween 80 as surfactant, and mixture of phospholipid and ethanol as the cosurfactant along with aqueous solution as the external phase were constructed and various compositions were formulated. The optimized formulation was characterized for particle-size, zeta-potential, drugcontent, globule-morphology pH, and refractive-index, whereas evaluated for skin permeation, retention, compliance, and dermatokinetics. The nanosized formulation offered threefold higher drug permeation vis-a-vis plain drug solution across LACA mice abdominal skin. The drug retention of the selected formulation was nearly twice of that from the marketed product, assuring depot formulation and sustained release. The skin histopathology revealed the non-irritant nature of the formulation, as no changes in the normal skin histology were observed. The dermatokinetic studies confirmed better permeation and enhanced skin bioavailability of BB to epidermis as well as dermis vis-à-vis the conventional product. The results indicate that the developed lipid-based microemulsion hydrogel can alleviate the concerns associated with BB and can provide a better and safer delivery option in substantial amounts to various skin layers.

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“…Moreover, the enhancing activities of these l-carvyl esters were evaluated using the model drug 5-fluorouracil (FU) in the in vitro skin permeation experiment. Several researchers agree that the enhancing activity of an enhancer may be determined by the amount of its uptake into the SC (11)(12)(13). However, the amount of an enhancer retained in the skin is rarely measured.…”

Section: Introductionmentioning

confidence: 99%

l-Carvyl Esters as Penetration Enhancers for the Transdermal Delivery of 5-Fluorouracil

Wang

Cun

et al. 2013

AAPS PharmSciTech

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Abstract. To develop effective and safe penetration enhancers, a series of l-carvyl esters, namely, 5-isopropenyl-2-methylcyclohex-2-en-1-yl heptanoate (C-HEP), 5-isopropenyl-2-methylcyclohex-2-en-1-yl octanoate (C-OCT), 5-isopropenyl-2-methylcyclohex-2-en-1-yl decanoate (C-DEC), 5-isopropenyl-2-methylcyclohex-2-en-1-yl dodecanoate (C-DOD), 5-isopropenyl-2-methylcyclohex-2-en-1-yl tetradecanoate (C-TET), and 5-isopropenyl-2-methylcyclohex-2-en-1-yl palmitate (C-PAL), was synthesized from l-carveol and saturated fatty acids (C7-C16). The volatility of l-carveol and l-carvyl esters was evaluated by a live weight loss experiment. The enhancing effects of l-carvyl esters on 5-fluorouracil (FU) were investigated in the in vitro permeation experiment on rat skin. The stratum corneum (SC) uptakes of the enhancers were tested in vitro by gas chromatography. Only the l-carvyl esters with a moderate SC uptake, namely, C-OCT (C8), C-DEC (C10), and C-DOD (C12), showed a potential to enhance FU skin permeation. An evident parabolic relationship was found between the permeation enhancement of FU and the SC uptake of the l-carvyl esters. The l-carvyl esters with a chain length of C8-C12 seemed to be favorable for FU.

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Uptake of Microemulsion Components into the Stratum Corneum and Their Molecular Effects on Skin Barrier Function

Cited by 92 publications

References 28 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

Benzyl Benzoate-Loaded Microemulsion for Topical Applications: Enhanced Dermatokinetic Profile and Better Delivery Promises

l-Carvyl Esters as Penetration Enhancers for the Transdermal Delivery of 5-Fluorouracil

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