An Insight into the Skin Penetration Enhancement Mechanism of <i>N</i>-Methylpyrrolidone

Cilurzo, Francesco; Vistoli, Giulio; Selmin, Francesca; Franzè, Silvia; Monte, Matteo Lo; Minghetti, Paola

doi:10.1021/mp400675d

Cited by 46 publications

(22 citation statements)

References 31 publications

(59 reference statements)

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“…The full-thickness skin was sealed in evacuated plastic bags and stored within 6 h after removal. Epidermis samples were prepared following an internal standard procedure [19]. Briefly, prior to the experiments, the skin was thawed at room temperature, and excess fat was carefully removed.…”

Section: Methodsmentioning

confidence: 99%

Topical Treatment of Infantile Haemangiomas: A Comparative Study on the Selection of a Semi-Solid Vehicle

Casiraghi

Musazzi²,

Rocco³

et al. 2016

Skin Pharmacol Physiol

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Background/Aim: Topical β-blockers have recently been proposed as a valid alternative to oral drugs for treating cutaneous infantile haemangiomas, but clinical results in the literature are inconsistent due to the empirical choice of topical preparations. The current investigation aimed to rationalize the selection of a semi-solid vehicle for a locally applied drug product containing 1% w/w propranolol hydrochloride (PR-Cl). Methods: A hydrophobic ointment of PR-Cl, two lipophilic creams, and a hydrophilic cream were prepared. In vitro release and skin permeation studies through human epidermis and full-thickness skin were performed by Franz diffusion cells. Results: The overall results highlighted that PR-Cl was able to permeate the human epidermis, and its penetration pattern was strongly influenced by the composition of the semi-solid vehicle. PR-Cl release and permeation from lipophilic vehicles were extremely limited and influenced by their composition. Best results were obtained by using the hydrophilic cream. Furthermore, the retention study evidenced that epidermis acted as a reservoir, releasing the PR-Cl accumulated after preparation removal. Conclusion: The 1% w/w PR-Cl cream resulted the most suitable formulation for improving drug permeation through the human epidermis. On the contrary, the negligible permeation profile through full-thickness skin pointed out that PR-Cl cannot diffuse significantly to reach the deeper layers of human skin.

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Section: Methodsmentioning

confidence: 99%

Topical Treatment of Infantile Haemangiomas: A Comparative Study on the Selection of a Semi-Solid Vehicle

Casiraghi

Musazzi²,

Rocco³

et al. 2016

Skin Pharmacol Physiol

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“…The skin bands obtained from skin intercellular lipids and keratin (corneocytes) were as follows: the modes were associated with protein as amide I (C=O) vibration (at approximately 1,640 cm . 54,55 In Figure 7, it can be clearly seen that the skin subjected to a stationary magnetic field shows a similar spectrum to the control. However, after exposure to an alternating magnetic field, the symmetric and asymmetric methylene stretching bands were shifted to lower values as shown in Figure 7B.…”

mentioning

confidence: 76%

Study of magnetic silk fibroin nanoparticles for massage-like transdermal drug delivery

Chen¹,

Chen²,

Wang³

et al. 2015

IJN

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A synergistic approach by the combination of magnetic nanoparticles with an alternating magnetic field for transdermal drug delivery was investigated. Methotrexate-loaded silk fibroin magnetic nanoparticles were prepared using suspension-enhanced dispersion by supercritical CO 2 . The physiochemical properties of the magnetic nanoparticles were characterized. In vitro studies on drug permeation across skin were performed under different magnetic fields in comparison with passive diffusion. The permeation flux enhancement factor was found to increase under a stationary magnetic field, while an alternating magnetic field enhanced drug permeation more effectively; the combination of stationary and alternating magnetic fields, which has a massage-like effect on the skin, achieved the best result. The mechanistic studies using attenuated total reflection Fourier-transform infrared spectroscopy demonstrate that an alternating magnetic field can change the ordered structure of the stratum corneum lipid bilayers from the gel to the lipid-crystalline state, which can increase the fluidity of the stratum corneum lipids, thus enhancing skin penetration. Compared with the other groups, the fluorescence signal with a bigger area detected in deeper regions of the skin also reveals that the simulated massage could enhance the drug permeation across the skin by increasing the follicular transport. The combination of magnetic nanoparticles with stationary/alternating magnetic fields has potential for effective massage-like transdermal drug delivery.

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“…Permeation enhancers or transdermal formulations containing alcohols, terpenes, fatty acids, and surfactants penetrate into the intercellular regions and reduce the barrier function of stratum corneum by destabilization and fluidization of lipid bilayers. 37,38,55 MTX-UDLs-T3 was selected for this study due to its efficient skin permeation among all MTX-UDLs. As shown in Figure 7A, the untreated skin showed endothermic transitions at 65.1°C, 82.5°C, and 115.4°C for the melting of intercellular lipids, protein-associated lipids, and denatured proteins in stratum corneum, respectively.…”

Section: Skin Penetration Of Fluorescence Marker (R6g)-entrapped Udlsmentioning

confidence: 99%

“…38 The isolated epidermis was treated with the optimized MTX-UDLs (MTX-UDLs-T3) for 4 hours on Franz diffusion cell under the same conditions as in vitro skin permeation studies. The epidermis treated with MTX-UDLs was washed carefully with PBS and subjected to DSC and FTIR after blot-drying.…”

mentioning

confidence: 99%

Improved skin permeation of methotrexate via nanosized ultradeformable liposomes

Zeb¹,

Qureshi²,

Kim³

et al. 2016

IJN

126

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The aim of this study is to investigate methotrexate-entrapped ultradeformable liposomes (MTX-UDLs) for potential transdermal application. MTX-UDLs were prepared by extrusion method with phosphatidylcholine as a bilayer matrix and sodium cholate or Tween 80 as an edge activator. The physicochemical properties of MTX-UDLs were determined in terms of particle size, polydispersity index, zeta potential, and entrapment efficiency. The deformability of MTX-UDLs was compared with that of methotrexate-entrapped conventional liposomes (MTX-CLs) using a steel pressure filter device. The skin permeation of MTX-UDLs was investigated using Franz diffusion cell, and the skin penetration depth of rhodamine 6G-entrapped UDLs was determined by confocal laser scanning microscopy. MTX-UDLs showed a narrow size distribution, with the particle size of ~100 nm. The deformability of MTX-UDLs was two to five times greater than that of MTX-CLs. The skin permeation of MTX-UDLs was significantly improved compared with MTX-CLs and free MTX solution. The optimized UDLs (phosphatidylcholine: Tween 80 =7:3, w/w) showed a higher fluorescence intensity than conventional liposomes at every increment of skin depth. Thus, the optimized UDLs could be promising nanocarriers for systemic delivery of MTX across skin.

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An Insight into the Skin Penetration Enhancement Mechanism of N-Methylpyrrolidone

Cited by 46 publications

References 31 publications

Topical Treatment of Infantile Haemangiomas: A Comparative Study on the Selection of a Semi-Solid Vehicle

Topical Treatment of Infantile Haemangiomas: A Comparative Study on the Selection of a Semi-Solid Vehicle

Study of magnetic silk fibroin nanoparticles for massage-like transdermal drug delivery

Improved skin permeation of methotrexate via nanosized ultradeformable liposomes

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