Dermal and transdermal delivery of an anti-psoriatic agent via ethanolic liposomes

Dubey, Vaibhav; Mishra, Dinesh Kumar; Dutta, Tathagata; Nahar, Manoj; Saraf, D. K.; Jain, Narendra Kumar

doi:10.1016/j.jconrel.2007.08.005

Cited by 289 publications

(125 citation statements)

References 28 publications

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“…Control tests in in vivo studies of MTX drug, reported in the literature revealed that the skin penetration of MTX is weak and the rate of absorption in rat skin of a 1% acqueous solution of MTX is low. [31] In order to study MTX skin penetration, in vivo mice skin was topically treated with Au-3MPS@MTX conjugate or to MTX aloneAfter 24 h skin biopsy from both treated areas was used for UV-vis analysis to trace the MTX content. We made an investigation of the absorbance peaks of the supranatants recovered from the skin treated with Au-3MPS@MTX or MTX alone and reacted for 24 h with the dispase enzyme, which allowed to separate epidermis from dermis.…”

Section: In Vivo Mouse Skin Permeationmentioning

confidence: 99%

“…This drug is characterized by high molecular weight and is mostly in dissociated form at physiological pH, with insufficient penetration into the basal layer of epidermis [30]. In vivo studies using topical MTX drug, revealed that the skin penetration of MTX is weak and the rate of absorption in rat skin of a MTX 1% acqueous solution is very low [31]. Biologic agents have been approved by the FDA to treat moderate to severe psoriasis that not responded to an adequate trial of one or more of the traditional drugs.…”

Section: Introductionmentioning

confidence: 99%

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Functionalized gold nanoparticles for topical delivery of methotrexate for the possible treatment of psoriasis

Bessar

Venditti

Benassi

et al. 2016

Colloids and Surfaces B: Biointerfaces

108

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a b s t r a c tGold nanoparticles (AuNPs) represent an effective choice for topical drug delivery systems thanks to their small size, general non-toxicity, ease of functionalization and high surface to volume ratio. Even if systemic, methotrexate still plays an important role in psoriasis treatment: its topical use shows insufficient percutaneus penetration owing to limited passive diffusion, high molecular weight and dissociation at physiological pH. The aim of our study was to design a new drug delivery nanocarrier for Methotrexate and to improve its solubility, stability and biodistribution. AuNPs were on purpose prepared with a hydrophilic stabilizing layer, in order to improve the colloidal stability in water. Watersoluble gold nanoparticles functionalized by sodium 3-mercapto-1-propansulfonate (Au-3MPS) were prepared and loaded with methotrexate (MTX). The loading efficiency of MTX on Au-3MPS was assessed in the range 70-80%, with a fast release (80% in one hour). The release was studied up to 24 h reaching the value of 95%. The Au-3MPS@MTX conjugate was fully characterized by spectroscopic techniques (UV-vis, FTIR) and DLS. Preliminary toxicity tests in the presence of keratinocytes monolayers allowed to assess that the used Au-3MPS are not toxic. The conjugate was then topically used on C57BL/6 mouse normal skin in order to trace the absorption behavior. STEM images clearly revealed the distribution of gold nanoparticles inside the cells. In vitro studies showed that Methotrexate conjugated with Au-3MPS is much more efficient than Methotrexate alone. Moreover, DL50, based on MTT analysis, is 20 folds reduced at 48 h, by the presence of nanoparticles conjugation. UV-vis spectra for in vivo tracing of the conjugate on bare mouse skin after 24 h of application, show increased delivery of Methotrexate in the epidermis and dermis using Au-3MPS@MTX conjugate, compared to MTX alone. Moreover we observed absence of the Au-3MPS in the dermis and in the epidermis, suggesting that these layers of the skin do not retain the nanoparticles. Based on our data, we found that the novel Au-3MPS@MTX conjugate is an effective non-toxic carrier for the satisfactory percutaneous absorption of Methotrexate and could help in possible topical treatment of psoriasis.

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Section: In Vivo Mouse Skin Permeationmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Functionalized gold nanoparticles for topical delivery of methotrexate for the possible treatment of psoriasis

Bessar

Venditti

Benassi

et al. 2016

Colloids and Surfaces B: Biointerfaces

108

View full text Add to dashboard Cite

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“…The rat's excised skin was blotted and washed thrice using ethanol on inactive paper. The applied area was then removed into the pieces of 1 mm 2 size and subjected evaluate for the probe penetration (depth) with CLSM (Fluorescence Correlation MicroscopeOlympus FluoView FV1000, Olympus, Melville, NY) with an argon laser beam with excitation at 488 nm and emission at 590 nm (Dubey et al, 2007). The sliced skin pieces were visualized under the normal light and fluorescence microscope.…”

Section: Visualization Of the Formulation Into The Skin Penetrated Inmentioning

confidence: 99%

Nanoemulsion gel-based topical delivery of an antifungal drug:in vitroactivity andin vivoevaluation

Samad²,

et al. 2014

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Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard University, New Delhi, India AbstractObjective: In this study, attempt has been focused to prepare a nanoemulsion (NE) gel for topical delivery of amphotericin B (AmB) for enhanced as well as sustained skin permeation, in vitro antifungal activity and in vivo toxicity assessment. Materials and methods: A series of NE were prepared using sefsol-218 oil, Tween 80 and Transcutol-P by slow spontaneous titration method. Carbopol gel (0.5% w/w) was prepared containing 0.1% w/w AmB. Furthermore, NE gel (AmB-NE gel) was characterized for size, charge, pH, rheological behavior, drug release profile, skin permeability, hemolytic studies and ex vivo rat skin interaction with rat skin using differential scanning calorimeter. The drug permeability and skin irritation ability were examined with confocal laser scanning microscopy and Draize test, respectively. The in vitro antifungal activity was investigated against three fungal strains using the well agar diffusion method. Histopathological assessment was performed in rats to investigate their toxicological potential.Results and discussion: The AmB-NE gel (18.09 ± 0.6 mg/cm 2 /h) and NE (15.74 ± 0.4 mg/cm 2 /h) demonstrated the highest skin percutaneous permeation flux rate as compared to drug solution (4.59 ± 0.01 mg/cm 2 /h) suggesting better alternative to painful and nephrotoxic intravenous administration. Hemolytic and histopathological results revealed safe delivery of the drug. Based on combined results, NE and AmB-NE gel could be considered as an efficient, stable and safe carrier for enhanced and sustained topical delivery for AmB in local skin fungal infection. Conclusion: Topical delivery of AmB is suitable delivery system in NE gel carrier for skin fungal infection.

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“…Jain et al [42] developed methotrexate loaded ethosomes by thin film hydration technique using soya (1-3w/v %) and 3:1 chloroform and methanol. In their study, different concentrations of phospholipid and ethanol were applied for the development of ethosomes.…”

Section: Ethosomesmentioning

confidence: 99%

Untitled

Madhavi

2016

AJP

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Aim: The aim of the present work was to focus on the applicability of liposomes and ethosomes for transdermal delivery. In the current review, we had focused on transdermal delivery transdermal delivery of vesicular system vesicular systems, i.e., liposome and ethosomes, factors affecting their permeation and penetration efficiency, limitations, applications, method of preparations, evaluation parameters, and selection of lipids. In this review, we considered the mechanism of controlled drug release of vesicles by transdermal delivery and the impact of their physicochemical properties. Rheumatoid arthritis (RA) is most frequently suffering disease in the geriatric population. By transdermal delivery, conventional anti-RA (ARA) therapy associated with several disadvantages. The modern ARA therapy; disease-modifying antirheumatic drugs (DMARDs) are more effective in reducing down disease progression. The basic mechanism of action of DMARDs in RA is not clear. The vesicles have a potential role in RA; especially, we focused on the impact of liposomes and ethosomes on RA by transdermal delivery, vesicular mechanism to justification in ARA therapy. Conclusion: The liposomes and ethosomes were beneficial tools for transdermal delivery. They have a potential role to control RA by transdermal delivery.

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Dermal and transdermal delivery of an anti-psoriatic agent via ethanolic liposomes

Cited by 289 publications

References 28 publications

Functionalized gold nanoparticles for topical delivery of methotrexate for the possible treatment of psoriasis

Functionalized gold nanoparticles for topical delivery of methotrexate for the possible treatment of psoriasis

Nanoemulsion gel-based topical delivery of an antifungal drug:in vitroactivity andin vivoevaluation

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