PENETRATION TEST OF CAFFEINE IN ETHOSOME AND DESMOSOME GEL USING AN IN VITRO METHOD

Objectives: Caffeine has many functions including its use in the field of cosmetics. Nonetheless, the percutaneous absorption of caffeine is very low(9%), and the penetration of a substance such as caffeine in the skin is not desirable. Ethosomes and desmosomes are lipid vesicles created by themodification of liposomes containing phospholipids and ethanol or dimethyl sulfoxide (DMSO) as the penetration enhancer. The purpose of this studywas to compare the effectiveness of ethosomes and desmosomes as vesicles in increasing the penetration of caffeine.Methods: Ethosomes and desmosomes were prepared using phosphatidylcholine, ethanol/DMSO, and caffeine. Phosphatidylcholine was used in theform of phospholipon 90 g that was obtained from soybeans. Observations were done including the characteristic of ethosomes and desmosomes,organoleptic observation, homogeneity observation, and in vitro penetration test using Franz diffusion cell method.Results: The cumulative penetration of caffeine ethosome gel is 3316.46±218.51 μg/cm2, with flux 249.45±30.06 μg·cm−2·hr−1, and 62.35±4.52%. Thecumulative penetration of the desmosome gel is 2954.95±222.87 μg/cm2 with flux 381.68±34.91 μg·cm−2·hr−1 and 53.4±3.65%.Conclusions: It can be concluded that ethosome is more effective than desmosome in increasing the penetration of caffeine.

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Ion mobility spectrometry as a high-throughput technique for in vitro transdermal Franz diffusion cell experiments of ibuprofen

Journal of Pharmaceutical and Biomedical Analysis ◽

10.1016/j.jpba.2011.02.027 ◽

2011 ◽

Vol 55 (3) ◽

pp. 472-478 ◽

Cited By ~ 13

Author(s):

B. Baert ◽

S. Vansteelandt ◽

B. De Spiegeleer

Keyword(s):

High Throughput ◽

Ion Mobility Spectrometry ◽

Ion Mobility ◽

Diffusion Cell ◽

Franz Diffusion Cell ◽

Diffusion Cell Experiments

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Methods for In Vitro Percutaneous Absorption Studies IV: the Flow-Through Diffusion Cell

Journal of Pharmaceutical Sciences ◽

10.1002/jps.2600740117 ◽

1985 ◽

Vol 74 (1) ◽

pp. 64-67 ◽

Cited By ~ 244

Author(s):

Robert L. Bronaugh ◽

Raymond F. Stewart

Keyword(s):

Percutaneous Absorption ◽

Diffusion Cell ◽

Absorption Studies ◽

Flow Through ◽

Through Diffusion ◽

In Vitro Percutaneous Absorption

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Studies on Corticosteroid Ointments. V. : Percutaneous Absorption of Hydrocortisone-4-14C. (1). : In Vitro Method of Percutaneous Absorption using Human Exised Skin

YAKUGAKU ZASSHI ◽

10.1248/yakushi1947.89.3_365 ◽

1969 ◽

Vol 89 (3) ◽

pp. 365-371 ◽

Cited By ~ 1

Author(s):

HIROYUKI SHINKAI

Keyword(s):

Percutaneous Absorption ◽

In Vitro Method

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In vitro Dermal Absorption: Sample Application and Seal Quality in a Franz Diffusion Cell System

Skin Pharmacology and Physiology ◽

10.1159/000375321 ◽

2015 ◽

Vol 28 (5) ◽

pp. 245-249 ◽

Cited By ~ 8

Author(s):

Bart Desmedt ◽

Patricia Courselle ◽

Jacques O. De Beer ◽

Vera Rogiers ◽

Eric Deconinck ◽

...

Keyword(s):

Cell System ◽

Dermal Absorption ◽

Diffusion Cell ◽

Franz Diffusion Cell ◽

Sample Application

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Validation of an In vitro-in vivo Assay System for Evaluation of Transdermal Delivery of Caffeine

Drug Delivery Letters ◽

10.2174/2210303108666180903102107 ◽

2019 ◽

Vol 9 (1) ◽

pp. 15-20 ◽

Cited By ~ 2

Author(s):

Fanni Farner ◽

Luca Bors ◽

Ágnes Bajza ◽

Gellért Karvaly ◽

István Antal ◽

...

Keyword(s):

Ex Vivo ◽

Assay System ◽

Diffusion Cell ◽

Rat Skin ◽

Topical Formulation ◽

Franz Diffusion Cell ◽

Topical Drugs ◽

In Vivo Assay

Introduction: Degree of skin penetration of topical drugs and cosmetics is a crucial point concerning their effects and tolerability. For testing drug delivery across the dermal barrier different in vitro and in vivo assays have been developed. Caffeine has been shown to have beneficial effects against skin aging, sunburn and hair-loss, and it is protective against melanoma and non-melanoma type skin cancers. Aim of our study was to set up an assay system to evaluate caffeine penetration from topical formulation into the skin. Methods: Franz diffusion cells consisting of either a filter paper or an artificial membrane or rat skin were used as in vitro/ex vivo test systems and transdermal microdialysis in anaesthetized rats was performed as an in vivo assay. Results: Results indicate that Franz diffusion cell studies provide a good approximation of the release of caffeine from the formulation but are not able to differentiate between 2% and 4% cream concentrations. The maximum concentrations (Cmax) in case of the 2% cream formulation were 708.3 (2.7 μm pore), 78.7 (0.8 µm pore), 45.3 (0.45 µm pore) and 44.9 (rat skin) µg/7.5 mL, respectively. The in vivo microdialysis experiments were in accordance with the in vitro and ex vivo results and gave more information on the dynamics and follicular and transcellular phases of drug penetration through the layers of the skin. Discussion and Conclusion: Taken together, Franz diffusion cell and transdermal microdialysis are a good combination to evaluate caffeine release and penetration into the skin from the formulations tested. This system might also be used for rapid testing of other hydrophilic topical drugs and has a benefit in the prediction for human skin absorption and tolerability studies, in an early phase of drug development.

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