Study on the drug permeation mechanism from flurbiprofen-loaded glyceryl monooleyl ether-based lyotropic liquid crystalline nanoparticles across the skin: Synchrotron X-ray diffraction and confocal laser scanning microscopy study

Uchino, Tomonobu; Kato, S.; Hatta, Ichiro; Miyazaki, Yasunori; Suzuki, Tomonori; Sasaki, Kiyotaka; Kagawa, Yoshiyuki

doi:10.1016/j.ijpharm.2018.11.031

Cited by 13 publications

(12 citation statements)

References 43 publications

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“…The static XRD experiments showed that the peak width of the XRD narrowed at the water content of 25 wt , but the spacing did not change 8,9 . On the other hand, the dynamic XRD experiments using the solution cell revealed that after water was applied to the hairless mice SC 50,51 , the spacing expanded, and the expansion was smaller than the size of one water molecule. The result that the water molecule is located at the two crystallographic positions, obtained from the neutron diffraction experiments of the skin lipid model 31 , may be related to this phenomenon.…”

Section: Water Content 25 Wt% That Is One Of the Key Water Contents In Stratum Corneummentioning

confidence: 99%

“…Although the SC may impede transdermal penetration of nanoparticles, drug-loaded nanoparticles have been examined as formulations 50,51 . Among them phospholipid nanoparticle has been frequently used because they are thermodynamically stable and spontaneously formed due to amphiphilic nature of phospholipid molecules 50 .…”

Section: Penetration Of Drug-loades Nanoparticles Into Stratum Corneummentioning

confidence: 99%

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Stratum Corneum Function: A Structural Study with Dynamic Synchrotron X-ray Diffraction Experiments

et al. 2021

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cells are formed by cell division. Upon leaving the basal layer, cells start to differentiate and migrate in the direction of the surface of the skin via stratum spinosum. At the stratum granulosum terminal differentiation occurs, during which the viable cells are transformed into corneocytes. In the stratum corneum SC the corneocyte is surrounded by a cornified cell envelope composed of cross-linked proteins and covalently bound lipids. The SC part is enlarged, as Abstract: Studies on the effectiveness of substances such as drugs and cosmetics that act on the skin require structural evidence at the molecular level in the stratum corneum to clarify their interaction with intercellular lipid and soft keratin. For this purpose, when applying the substances to the stratum corneum X-ray diffraction experiment is one of the powerful tools. To detect minute structural changes in a stratum corneum sample, using a "solution cell", dynamic synchrotron X-ray diffraction measurements were performed when applying aqueous solution of the substances to the stratum corneum: (1) It was found that a surfactant, sodium dodecyl sulfate, significantly disrupted the long-period lamellar structure. (2) To study the effects of water, structural modifications of the short-period lamellar structure and the soft keratin in corneocytes were measured as a function of time. At the initial water content of 15 wt%, the spacings of the short-period lamellar structure and the soft keratin increased toward those at the water content of 25 wt%, that is a key water content in the stratum corneum. (3) Nanoparticles composed of assembly of amphiphilic molecules are one of the leading pharmaceutical formulations. When the nanoparticles were applied, a new assembly of amphiphilic molecules originated from the nanoparticle appeared. This phenomenon suggests that the formation of the new assembly at the surface of skin is concerned with the release of the drug from the nanoparticles. (4) When ethanol was applied to the stratum corneum, only the liquid state in the intercellular lipid matrix was dissolved. After the removal of ethanol from this stratum corneum, the ordered hydrocarbon-chain packing structures appeared. From this fact we would propose that the liquid state region is the main pathway for hydrophobic drugs with a small molecular weight in connection with the so-called 500 Da rule. Here, not only the technique but also the background to these studies and the characteristic results obtained from these studies are explained.

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Section: Water Content 25 Wt% That Is One Of the Key Water Contents In Stratum Corneummentioning

confidence: 99%

Section: Penetration Of Drug-loades Nanoparticles Into Stratum Corneummentioning

confidence: 99%

Stratum Corneum Function: A Structural Study with Dynamic Synchrotron X-ray Diffraction Experiments

et al. 2021

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“…Earlier studies had used a solution cell [19] and analysed the subtle changes in the X‐ray diffraction profiles of the SC samples when different solutions were applied to the SC. For example, it has been found that on applying ethanol to the SC, the liquid state in the intercellular lipids melted and successively by evacuating ethanol from the solution, the hydrocarbon chain packing structure (crystallized structure) appeared [20]; on applying an aqueous solution of sodium dodecyl sulphate only the long lamellar structure was disrupted, and then, the molecular origin of the structural damage in the SC was revealed [21]; on applying a drug‐loaded glycerol monooleyl ether‐based hexosome nanoparticle to the SC, the drug‐loaded hexosome transformed to the drug‐free hexosome as a result of drug release into the SC [22]. Collectively, these studies revealed the efficiency of X‐ray diffraction for analysing structural changes due to sample processing.…”

Section: Introductionmentioning

confidence: 99%

Moisturizing mechanism of glycerol and diglycerol on human stratum corneum studied by synchrotron X‐ray diffraction

Yamada

Habuka

Hatta

2020

Intern J of Cosmetic Sci

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ObjectivePolyols are moisturizers used in cosmetics. Using X‐ray diffraction, we studied the moisturizingmechanism of polyol solutions in the stratum corneum (SC). We examined whether glycerol disrupts the ordered hydrocarbon chain packing structure in isolated SC, as previously proposed in an SC lipid model.MethodsThe SC samples were prepared by treatment with water and aqueous solutions of glycerol, diglycerol and glycerol/diglycerol. To examine the differences in the water‐retention efficiency of polyols, using a solution cell, we performed dynamic X‐ray diffraction to analyse the structural changes that occurred during water removal from the hydrated samples by a stream of dry nitrogen gas. We focused on two structures, the orthorhombic hydrocarbon chain packing structure in the intercellular lipids and the soft keratin in the corneocytes where most of the water is stored.ResultsThe spacing formed by the soft keratin in the corneocytes immersed in a solution of water and diglycerol solution decreased rapidly by water removal. In contrast, it decreased gradually in the corneocytes immersed in a solution of glycerol and glycerol/diglycerol, indicating that the glycerol‐containing solutions maintained the hydrated state of the corneocytes for longer. Furthermore, the characteristic change of the spacing in the orthorhombic hydrocarbon chain packing structure over time was observed during the drying process. The hydrated state was maintained longer, in water, followed by glycerol, diglycerol and glycerol/diglycerol, in increasing order. This is the first study to report such characteristic properties that could be indicators of the capacity of the SC to regulate water.ConclusionThe dynamic X‐ray diffraction experiment on the structure of the soft keratin and the orthorhombic hydrocarbon chain packing structure during the drying of the hydrated SC provides an insight into the moisturizing mechanism of the polyol solutions in the SC. The results show that the glycerol/diglycerol solution functions as an effective SC moisturizer at the molecular level. Further, it was confirmed that the behaviour of glycerol in the isolated SC varies from that proposed in the SC lipid model, wherein glycerol was proposed to prevent the formation of a regular hydrocarbon chain packing structure.

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“… Bouwstra et al have identified changes in the lamellar organization of skin lesions from patients with lamellar ichthyosis, psoriasis, Netherton syndrome, and atopic dermatitis compared with healthy skin, consistent with large variations in SC lipid composition and highly compromised barrier function . Moreover, SAXS has been used to evaluate barrier properties of stratum corneum substitutes and lipid model systems employed as in vitro percutaneous penetration models for prescreening applications, in addition to drug delivery applications to evaluate the effects of chemical permeation enhancers on lipid organization and drugs penetration . None of these methods have been reported as used to date for measuring barrier properties of skin following a mild compromise such as cleansing.…”

Section: Introductionmentioning

confidence: 99%

“…[44,47] Moreover, SAXS has been used to evaluate barrier properties of stratum corneum substitutes and lipid model systems employed as in vitro percutaneous penetration models for prescreening applications, [42,43,[48][49][50][51] in addition to drug delivery applications to evaluate the effects of chemical permeation enhancers on lipid organization and drugs penetration. [52,53] None of these methods have been reported as used to date for measuring barrier properties of skin following a mild compromise such as cleansing.…”

Section: Introductionmentioning

confidence: 99%

Cleansers' mildness: Stratum corneum lipid organization and water uptake after a single wash

Perticaroli

Meyers

Wireko

et al. 2020

J Raman Spectroscopy

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The modern marketplace for personal cleansing demands effective but also gentle products. The acute effects of skin exposure to personal cleansers are a key driver in product mildness. Yet many current clinical methods of assessing this mildness rely upon exaggerated test conditions that do not match the brief contact time with the skin in typical use. Here, we present an approach to quantitatively measure changes in composition, water uptake, and spacing of lipid lamellar structures in human stratum corneum after a single~2-minute wash protocol. The approach is based upon in vivo confocal Raman spectroscopy and small-angle X-ray scattering (SAXS) of ex vivo stratum corneum. Raman data, collected using cleansers with varying degrees of harshness, reveal changes in water uptake as a function of skin depth and detect depth of damage upon cleansing, a conduit to barrier integrity. By treating isolated human stratum corneum with cleansers for similarly short exposures, SAXS reveals structural perturbations associated with interactions of surfactants and skin lipid lamellar structure, also a measure of barrier strength. Disruption of the characteristic periodicity phases of the lipid lamellae or formation of new phases with intermediate periodicity due to surfactant intercalation are observed for different formulations. This approach provides molecular scale characterization of skin-product interactions and resulting skin barrier effects in more realistic consumer treatment conditions. It also provides feedback about cleansers' mildness in a rapid fashion and at lower cost, widening a bottleneck of identification and assessment of new ingredients in the early stages of formula design. K E Y W O R D Sin vivo confocal Raman spectroscopy, lipid lamellae, skin barrier, X-Ray scattering, water content

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Study on the drug permeation mechanism from flurbiprofen-loaded glyceryl monooleyl ether-based lyotropic liquid crystalline nanoparticles across the skin: Synchrotron X-ray diffraction and confocal laser scanning microscopy study

Cited by 13 publications

References 43 publications

Stratum Corneum Function: A Structural Study with Dynamic Synchrotron X-ray Diffraction Experiments

Stratum Corneum Function: A Structural Study with Dynamic Synchrotron X-ray Diffraction Experiments

Moisturizing mechanism of glycerol and diglycerol on human stratum corneum studied by synchrotron X‐ray diffraction

Cleansers' mildness: Stratum corneum lipid organization and water uptake after a single wash

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