Effect of γ-cyclodextrin on the in vitro skin permeation of a steroidal drug from nanoemulsions: Impact of experimental setup

Klang, Victoria; Haberfeld, Silvia; Hartl, A.; Valenta, Claudia

doi:10.1016/j.ijpharm.2011.11.037

Cited by 16 publications

(5 citation statements)

References 31 publications

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“…This marked intracutaneous distribution has been described, for example, with tioconazole in guinea pig skin, detecting (after 2 h) around 300 µg/g in stratum corneum, but only 25 µg/g in epidermis [67]. These results confirm that if BFZ is relicted in the lipophilic skin regions then its apparent permeation through the dermis can be reduced dramatically [68,69] favoring its antifungal activity in the epidermic tissue.…”

Section: Discussionsupporting

confidence: 66%

Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery

et al. 2019

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Efficient topical delivery of imidazolic antifungals faces the challenge of overcoming its limited water solubility and its required long-lasting duration of treatments. In this paper, a hydrophilic multiple emulsion (ME) of Bifonazole (BFZ) is shown to maximize its skin retention, minimize its skin permeation, and maintain an acceptable level of being harmless in vivo. The formulations were pharmaceutically characterized and application properties were assessed based on viscosity measurements. Non-Newtonian pseudoplastic shear thinning with apparent thixotropy was observed, facilitating the formulation retention over the skin. The in vitro release profile with vertical diffusion cells showed a predominant square-root release kinetic suggesting an infinite dose depletion from the formulation. Ex vivo human skin permeation and penetration was additionally evaluated. Respective skin permeation was lower than values obtained with a commercial O/W formulation. The combination of amphoteric and non-ionic surfactants increased the bifonazole epidermal accumulation by a factor of twenty. This fact makes the possibility of increasing its current 24 h administration frequency more likely. Eventual alterations of skin integrity caused by the formulations were examined with epidermal histological analysis and in vivo preclinical measurements of skin elasticity and water retrograde permeation. Histological analysis demonstrated that the multiple emulsions were harmless. Additionally, modifications of in vivo skin integrity descriptors were considered as negligible.

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Section: Discussionsupporting

confidence: 66%

Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery

et al. 2019

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“…This phenomenon indicates that the percutaneous penetration enhancement of ACADFE may be achieved by using β-CD. A rapid drug permeation rate was observed for solutions containing the drug complex and physical mixture, where >50% of the drug permeated the skin within the first 1 h. Klang et al reported that a 10-fold increase in applied dose from 5 to 50 mg cm –2 and from 50 to 500 mg cm –2 was clearly reflected in the permeated drug amounts and fluxes ( p < 0.05) in both systems containing additional β-CD. Concurrently, the addition of CD magnified the increase in permeation with increasing doses.…”

Section: Resultsmentioning

confidence: 99%

Encapsulation of a Flavonoid-rich Allium cepa L. var. agrogatum Don Extract in β-Cyclodextrin for Transdermal Drug Delivery

Ding

Guo

et al. 2013

J. Agric. Food Chem.

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This work aims to evaluate the encapsulation of a flavonoid-rich Allium cepa L. var. agrogatum Don extract (ACADFE) in β-cyclodextrin (β-CD) by analyzing the percutaneous penetration in vitro and in vivo, leading to an explanation of the physical mechanism during transdermal transport. The optimal inclusion compound containing ACADFE in β-CD was prepared in a 1:3 molar ratio. The physicochemical characterization of the inclusion complex was performed using IR, UV-vis, simultaneous thermogravimetry (TG), and differential thermal analysis (DTA) studies. It was concluded that the inclusion complex could improve the aqueous solubility and bioavailability of ACADFE. The inclusion complex exhibited significant enhancement of percutaneous absorption both in vitro and in vivo. The dorsal skins of hairless mice were photographed using a confocal scanning laser microscope. Confocal scanning laser microscopy shows that penetration of the ACADFE-β-CD inclusion complex proceeds across skin via both follicular and transcellular routes.

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“…This is equivalent to the amount that is used by patients. Therefore, these experiments are more predictive for the situation in vivo …”

Section: Resultsmentioning

confidence: 99%

Oil-in-Oil-Emulsions with Enhanced Substantivity for the Treatment of Chronic Skin Diseases

Lunter

Rottke

Daniels

2014

Journal of Pharmaceutical Sciences

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Effect of γ-cyclodextrin on the in vitro skin permeation of a steroidal drug from nanoemulsions: Impact of experimental setup

Cited by 16 publications

References 31 publications

Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery

Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery

Encapsulation of a Flavonoid-rich Allium cepa L. var. agrogatum Don Extract in β-Cyclodextrin for Transdermal Drug Delivery

Oil-in-Oil-Emulsions with Enhanced Substantivity for the Treatment of Chronic Skin Diseases

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