Molecular interactions of penetration enhancers within ceramides organization: A FTIR approach

Guillard, Emmanuelle; Tfayli, Ali; Laugel, Cécile; Baillet‐Guffroy, Arlette

doi:10.1016/j.ejps.2008.10.010

Cited by 44 publications

(29 citation statements)

References 25 publications

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“…The lipid content of a formulation can influence the thermodynamic activity of the active ingredient, resulting in a modified penetration profile [51] and penetration enhancers like oleic acid and ethanol changing the ceramide organization within the skin, and can reversibly reduce the barrier function of the stratum corneum [57] . Changes of lipid structure by Poloxamer 2.5% used for SLN stabilization have, however, been ruled out [58] , and intact SLNs 175 nm in size should not penetrate the skin [7] .…”

Section: Skin Uptake Studies: Creammentioning

confidence: 99%

Drug Release and Skin Penetration from Solid Lipid Nanoparticles and a Base Cream: A Systematic Approach from a Comparison of Three Glucocorticoids

Schlupp

Blaschke²,

Kramer³

et al. 2011

Skin Pharmacol Physiol

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Solid lipid nanoparticles (SLNs) can enhance drug penetration into the skin, yet the mechanism of the improved transport is not known in full. To unravel the influence of the drug-particle interaction on penetration enhancement, 3 glucocorticoids (GCs), prednisolone (PD), the diester prednicarbate (PC) and the monoester betamethasone 17-valerate (BMV), varying in structure and lipophilicity, were loaded onto SLNs. Theoretical permeability coefficients (cm/s) of the agents rank BMV (–6.38) ≧ PC (–6.57) > PD (–7.30). GC-particle interaction, drug release and skin penetration were investigated including a conventional oil-in-water cream for reference. Both with SLN and cream, PD release was clearly superior to PC release which exceeded BMV release. With the cream, the rank order did not change when studying skin penetration, and skin penetration is thus predominantly influenced by drug release. Yet, the penetration profile for the GCs loaded onto SLNs completely changed, and differences between the steroids were almost lost. Thus, SLNs influence skin penetration by an intrinsic mechanism linked to a specific interaction of the drug-carrier complex and the skin surface, which becomes possible by the lipid nature and nanosize of the carrier and appears not to be derived by testing drug release. Interestingly, PC and PD uptake from SLN even resulted in epidermal targeting. Thus, SLNs are not only able to improve skin penetration of topically applied drugs, but may also be of particular interest when specifically aiming to influence epidermal dysfunction.

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Section: Skin Uptake Studies: Creammentioning

confidence: 99%

Drug Release and Skin Penetration from Solid Lipid Nanoparticles and a Base Cream: A Systematic Approach from a Comparison of Three Glucocorticoids

Schlupp

Blaschke²,

Kramer³

et al. 2011

Skin Pharmacol Physiol

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“…The selection of these materials was based on the following reasons; methyl acetate is widely used as a solvent of polymers, chloroform and the mixture of ethanol and chloroform are used as a solvent of fats and lipids, while limonene has been known as a skin penetration enhancer of drug 25 and has been reported to interact strongly with ceramides 26 . The results presented in Fig.…”

Section: X-ray Diffractionmentioning

confidence: 99%

Thermal-history-dependent Phase Behavior of Ceramide Molecular Assembly in a UV-curable Acrylic Adhesive Resin

et al. 2018

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“…They reported that lipophilic enhancers have dominant fluidizing action on the ceramide alkyl chain organization that increases the space between lipid bilayer packing. Whereas, hydrophilic enhancers do not interact with lipid bilayer, rather decrease the strength of H-bonds within the polar head group of the ceramides (Guillard et al, 2009). Both types of mechanisms reduce the resistance of skin to drug diffusion.…”

Section: Chemical Enhancersmentioning

confidence: 98%

Recent advances in transdermal drug delivery

et al. 2010

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Transdermal delivery of pharmacologically active agents has been extensively studied for the past 40 years. Despite the strong efforts, currently, only about 40 products are in market on about 20 drug molecules, due to the requirements that the patch area should be small enough for the patients to feel comfortable, and to the barrier properties of the stratum corneum. Various approaches to overcome the barrier function of skin through physical and chemical means have been broadly studied. The development of an effective transdermal delivery system is dictated by the unique physicochemical property each drug molecule possesses. In this review, we have summarized various physical and chemical approaches for transdermal flux enhancement, including the application of electricity, ultrasound, microneedle and chemical enhancers. Pressure sensitive adhesive such as acrylics, rubbers and silicones are described together with recent developments. Factors affecting dosage form design, particularly for drug in adhesive system, like adhesion and crystallization are also discussed.

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Molecular interactions of penetration enhancers within ceramides organization: A FTIR approach

Cited by 44 publications

References 25 publications

Drug Release and Skin Penetration from Solid Lipid Nanoparticles and a Base Cream: A Systematic Approach from a Comparison of Three Glucocorticoids

Drug Release and Skin Penetration from Solid Lipid Nanoparticles and a Base Cream: A Systematic Approach from a Comparison of Three Glucocorticoids

Thermal-history-dependent Phase Behavior of Ceramide Molecular Assembly in a UV-curable Acrylic Adhesive Resin

Recent advances in transdermal drug delivery

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