Investigation of the mechanism of enhanced skin penetration by ultradeformable liposomes

Subongkot, Thirapit; Pamornpathomkul, Boonnada; Rojanarata, Theerasak; Opanasopit, Praneet; Ngawhirunpat, Tanasait

doi:10.2147/ijn.s65287

Cited by 12 publications

(4 citation statements)

References 32 publications

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“…Subongkot et al . propose that vesicles could traverse the skin intact through follicular channels 35 . Our experience leads us to support a version of the proposal by Honeywell-Nguyen and Bowstra, namely that liposomes, once applied on the skin, rupture and diffuse as a lipidic mixture that acts as a penetration enhancer.…”

Section: Discussionmentioning

confidence: 99%

Liposomes can both enhance or reduce drugs penetration through the skin

Peralta

Guzmán

Perez

et al. 2018

Sci Rep

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The adequate formulation of topical vehicles to treat skin diseases is particularly complex. A desirable formulation should enhance the accumulation of the active drugs in the target tissue (the skin), while avoiding the penetration enhancement to be so large that the drugs reach the systemic circulation in toxic amounts. We have evaluated the transcutaneous penetration of three drugs chosen for their widely variable physicochemical properties: Amphotericin B, Imiquimod and Indole. We incorporated the drugs in fluid or ultra-flexible liposomes. Ultra-flexible liposomes produced enhancement of drug penetration into/through human skin in all cases in comparison with fluid liposomes without detergent, regardless of drug molecular weight. At the same time, our results indicate that liposomes can impede the transcutaneous penetration of molecules, in particular small ones.

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Section: Discussionmentioning

confidence: 99%

Liposomes can both enhance or reduce drugs penetration through the skin

Peralta

Guzmán

Perez

et al. 2018

Sci Rep

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“…The proposed transdermal penetration of FLUVs has previously been described to occur by two different mechanisms: The first being that the FLUVs being ultra-flexible can squeeze their way through the SC and act as a drug carrier system, the second mechanism being that the FLUVs function as chemical penetration enhancers. Cevc et al reported intact drug loaded FLUVs in the blood stream of mice after treatment with fluorescently labeled vesicles [ 17 ], and others have found penetration of loaded vesicles through frozen abdominal porcine skin from intrapartum stillborn animals using Franz diffusion cells[ 35 ]. On the other hand, others, using human skin, have suggested that the penetration of intact liposomes into the human epidermis is highly unlikely due to low amounts of vesicle material found in the deeper layers of the SC [ 36 ].…”

Section: Discussionmentioning

confidence: 99%

Superresolution and Fluorescence Dynamics Evidence Reveal That Intact Liposomes Do Not Cross the Human Skin Barrier

2016

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In this study we use the combination of super resolution optical microscopy and raster image correlation spectroscopy (RICS) to study the mechanism of action of liposomes as transdermal drug delivery systems in human skin. Two different compositions of liposomes were applied to newly excised human skin, a POPC liposome and a more flexible liposome containing the surfactant sodium cholate. Stimulated emission depletion microscopy (STED) images of intact skin and cryo-sections of skin treated with labeled liposomes were recorded displaying an optical resolution low enough to resolve the 100 nm liposomes in the skin. The images revealed that virtually none of the liposomes remained intact beneath the skin surface. RICS two color cross correlation diffusion measurements of double labeled liposomes confirmed these observations. Our results suggest that the liposomes do not act as carriers that transport their cargo directly through the skin barrier, but mainly burst and fuse with the outer lipid layers of the stratum corneum. It was also found that the flexible liposomes showed a greater delivery of the fluorophore into the stratum corneum, indicating that they functioned as chemical permeability enhancers.

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“…The barrier of the stratum corneum limits skin penetration resulting from intercellular lipid lamellae [ 27 , 28 ] and keratin filaments inside corneocytes and corneodesmosomes that connect corneocytes between each layer of the stratum corneum [ 28 ]. According to the study by Subongkot et al [ 29 ], ULs with d-limonene could increase the skin penetration of fluorescein sodium from degradation of corneodesmosomes, keratin filament denaturation, and intercellular lipid disruption. There is evidence showing that oleic acid could enhance the skin penetration by increasing the stratum corneum lipid fluidity and forming permeable defects inside intercellular lipids [ 30 , 31 ].…”

Section: Resultsmentioning

confidence: 99%

Development of Ultradeformable Liposomes with Fatty Acids for Enhanced Dermal Rosmarinic Acid Delivery

2021

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This study aimed to develop ultradeformable liposomes (ULs) with fatty acids, namely, oleic, linoleic, and linolenic acid, to improve the skin penetration of rosmarinic acid. This study also investigated the vesicle-skin interaction and skin penetration pathway of ULs with fatty acids using the co-localization technique of multifluorescently labeled particles. The prepared ULs were characterized in terms of size, surface charge, size distribution, shape, % entrapment efficiency (% EE), and % loading efficiency (% LE). The prepared ULs with fatty acids had an average particle size between 50.37 ± 0.3 and 59.82 ± 17.3 nm with a size distribution within an acceptable range and exhibited a negative surface charge. The average % EE and % LE were 9 and 24.02, respectively. The in vitro skin penetration study found that ULs with oleic acid could significantly increase the skin penetration of rosmarinic acid compared to ULs. According to confocal laser scanning microscopy observations, this study suggested that UL vesicles attach to the skin before releasing the entrapped drug to penetrate the skin. These findings suggested that ULs with oleic acid penetrated the skin via the transfollicular pathway as a major penetration pathway.

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Investigation of the mechanism of enhanced skin penetration by ultradeformable liposomes

Cited by 12 publications

References 32 publications

Liposomes can both enhance or reduce drugs penetration through the skin

Liposomes can both enhance or reduce drugs penetration through the skin

Superresolution and Fluorescence Dynamics Evidence Reveal That Intact Liposomes Do Not Cross the Human Skin Barrier

Development of Ultradeformable Liposomes with Fatty Acids for Enhanced Dermal Rosmarinic Acid Delivery

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