A water gradient can be used to regulate drug transport across skin

Björklund, Sebastian; Engblom, Johan; Thuresson, Krister; Sparr, Emma

doi:10.1016/j.jconrel.2010.01.005

Cited by 80 publications

(113 citation statements)

References 54 publications

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“…All solvents investigated induce mobility in SC components. The changes in the proportion between fluid SC and solid lipids and proteins can have a large impact on the macroscopic properties of the SC, including transport barrier function, flexibility, and softness (2,6,13,16,17). The observed effects vary with the polarity of the solvent, its concentration, and SC hydration conditions.…”

Section: Extraction Of Mobile Lipids From Sc Due To Exposure To Excessmentioning

confidence: 99%

“…The macroscopic material properties of the SC barrier membrane naturally depend on the molecular properties of its building blocks. In particular, transport properties as well as mechanical properties and water-holding capacity can be altered by changing the balance between solid and fluid structures in the complex SC material (13,14,(16)(17)(18)(19). Increasing fluidity is expected to lead to higher solubility and a higher diffusion coefficient for most added compounds, and thus increased effective SC permeability (14,18,19).…”

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confidence: 99%

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Tracking solvents in the skin through atomically resolved measurements of molecular mobility in intact stratum corneum

Pham

Topgaard

Sparr

2016

Proc. Natl. Acad. Sci. U.S.A.

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Solvents are commonly used in pharmaceutical and cosmetic formulations and sanitary products and cleansers. The uptake of solvent into the skin may change the molecular organization of skin lipids and proteins, which may in turn alter the protective skin barrier function. We herein examine the molecular effects of 10 different solvents on the outermost layer of skin, the stratum corneum (SC), using polarization transfer solid-state NMR on natural abundance 13C in intact SC. With this approach it is possible to characterize the molecular dynamics of solvent molecules when present inside intact SC and to simultaneously monitor the effects caused by the added solvent on SC lipids and protein components. All solvents investigated cause an increased fluidity of SC lipids, with the most prominent effects shown for the apolar hydrocarbon solvents and 2-propanol. However, no solvent other than water shows the ability to fluidize amino acids in the keratin filaments. The solvent molecules themselves show reduced molecular mobility when incorporated in the SC matrix. Changes in the molecular properties of the SC, and in particular alternation in the balance between solid and fluid SC components, may have significant influences on the macroscopic SC barrier properties as well as mechanical properties of the skin. Deepened understanding of molecular effects of foreign compounds in SC fluidity can therefore have strong impact on the development of skin products in pharmaceutical, cosmetic, and sanitary applications.

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Section: Extraction Of Mobile Lipids From Sc Due To Exposure To Excessmentioning

confidence: 99%

mentioning

confidence: 99%

Tracking solvents in the skin through atomically resolved measurements of molecular mobility in intact stratum corneum

Pham

Topgaard

Sparr

2016

Proc. Natl. Acad. Sci. U.S.A.

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“…This is shown in Figure 3B as linear dependencies between J ss & ε, with R 2 values of 0.6 and 0.8 for membranes exposed to Cream A and Cream B, respectively. A higher ε value indicates that the extracellular lamellar lipid matrix in the stratum corneum has an increased fraction of lipids in the fluid state, and in many studies it has been shown that molecular diffusion in lipids is facilitated by a transition from the crystalline to the liquid crystalline state [22][23][24].…”

Section: Discussionmentioning

confidence: 99%

Topical Administration of Mometasone Furoate - A Combined Impedance Spectroscopy and In Vitro Drug Diffusion Study

Runnsjö¹

2015

JAPLR

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“…Deformable liposomes and ethosomes improve skin delivery (permeation and deposition) of the model hydrophilic drug ketotifen (KT) fumarate, with greater improvement of deposition than permeation. 31) The x-z axis serial images from CLSM (Fig. 5) show the different penetration depths of NaFI and Rh-PE from PLs with d-limonene.…”

Section: Fig 1 Atomic Force Microscopy (Amf) Images Of (A) Cls (B)mentioning

confidence: 98%

Terpene-Containing PEGylated Liposomes as Transdermal Carriers of a Hydrophilic Compound

Rangsimawong

Opanasopit

Rojanarata

et al. 2014

Biological & Pharmaceutical Bulletin

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We investigated the effect of PEGylated liposomes (PLs) containing a terpene on the penetration of a hydrophilic compound through porcine skin. PLs composed of N-(carbonyl-methoxypolyethyleneglycol-2000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine (PEG 2000 -DSPE), the sodium salt of PEG 2000 -DSPE, phosphatidylcholine (PC), cholesterol (Chol), Tween 20, and d-limonene were prepared as carriers for fluorescein sodium (NaFI). The physicochemical characteristics of PLs and their effects on in vitro skin penetration were evaluated. Tape stripping was used to evaluate NaFI deposition in skin layers, and confocal laser scanning microscopy (CLSM) was used to investigate the depth of skin penetration and the pathways used by NaFI-loaded vesicles. PLs containing d-limonene were smaller and conferred higher entrapment efficiency and skin penetration on NaFI than did PLs and conventional liposomes (CLs). The deposition of NaFI from PLs with d-limonene was greater in epidermis and dermis (6.10 1.74 µg) than stratum corneum (2.06 0.47 µg). CLSM images revealed that NaFI penetrated into the deepest skin layer with maximum fluorescence intensity. NaFI penetrated deeper (180 µm) in follicular than nonfollicular regions (145 µm), suggesting a transfollicular pathway predominates in skin penetration by NaFI-loaded PLs. In conclusion, grafting PEG onto ultra-deformable liposomes may enhance transdermal NaFI delivery and may be used as a carrier to prolong liposome circulation time.

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A water gradient can be used to regulate drug transport across skin

Cited by 80 publications

References 54 publications

Tracking solvents in the skin through atomically resolved measurements of molecular mobility in intact stratum corneum

Tracking solvents in the skin through atomically resolved measurements of molecular mobility in intact stratum corneum

Topical Administration of Mometasone Furoate - A Combined Impedance Spectroscopy and In Vitro Drug Diffusion Study

Terpene-Containing PEGylated Liposomes as Transdermal Carriers of a Hydrophilic Compound

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