Enhancement of bioavailability by lowering of fat content in topical formulations

Wirén, K.; Frithiof, H.; Sjöqvist, C.; Lodén, Marie

doi:10.1111/j.1365-2133.2008.08981.x

Cited by 28 publications

(24 citation statements)

References 18 publications

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“…This system has recently been evaluated in separate studies with regard to performance ), ability to visualize skin erythema ) and blanching (Zhai, 7/26 H. et al 2009) as well as in the assessment of the skin barrier function (Wiren, K. et al 2008). …”

Section: Tissue Viability Imager (Tivi)mentioning

confidence: 99%

Tissue viability imaging: Microvascular response to vasoactive drugs induced by iontophoresis

Henricson¹,

Nilsson²,

Tesselaar³

et al. 2009

Microvascular Research

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When one is studying the physiology of the cutaneous microcirculation there is a need for relevant non-invasive and versatile techniques. In this study we used a new optical device, the Tissue Viability Imager (TiVi), to map changes in cutaneous microvascular concentrations of red blood cells during iontophoresis of vasoactive substances (noradrenaline (NA) and phenylephrine (Phe) for vasoconstriction and acetylcholine (ACh) and sodium nitroprusside (SNP) for vasodilatation). We aimed to present data both individually and pooled, using a four-variable logistic dose response model that is commonly used in similar in vitro vascular studies. The accuracy of the TiVi was also investigated by calculating the coefficient of variation and comparing it with similar tests previously done using laser Doppler imaging.Tests were also performed using the TiVi and LDPI simultaneously to further compare the two methods.Results showed that the TiVi is capable of quantifying vascular responses to iontophorised noradrenaline and phenylephrine without the need to increase background flow first. Results further seem to suggest that when the blood perfusion increases during vasodilatation in skin the initial phase relies mainly on an increase in red blood cell concentration whereas the further perfusion increase is due to an increase in red blood cell velocity.

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Section: Tissue Viability Imager (Tivi)mentioning

confidence: 99%

Tissue viability imaging: Microvascular response to vasoactive drugs induced by iontophoresis

Henricson¹,

Nilsson²,

Tesselaar³

et al. 2009

Microvascular Research

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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%

“…The higher kinetic constants for SLN dispersions can be attributed to the lower viscosity of the outer aqueous phase [28] and to the increased thermodynamic activity of the GCs in the SLN dispersion due to the higher water content and therefore a decrease in the GC solubility in the formulation. Investigating volunteers Wirén et al [51] showed a higher activity of BMV (skin blanching) and benzyl nicotinate (erythema induction) by lowering the fat content in topi- ) were applied to a polyamide membrane (Higuchi plot). cal formulations which is attributed to a higher increase in drug concentration in the lower fat formulations with water evaporation when applied to the skin.…”

Section: Gc Release: Slnsmentioning

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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“…These features can be built in to a formulation without compromising its efficacy. For example, Wirén et al investigated the effect of changes in vehicle lipid content of o/w emulsions containing two active ingredients: benzyl nicotinate and β-methasone valerate on erythema and blanching of human skin in vivo [51]. Enhanced efficacy of both active ingredients (erythema with benzyl nicotinate and blanching with β-methasone valerate) was seen with the emulsions with the lowest (10%) lipid content, indicating that products can be designed with both efficacy and tactile acceptability in mind.…”

Section: Concentration Of the Components Of The Formulationmentioning

confidence: 99%

Delivery of drugs applied topically to the skin

Leite-Silva¹,

Almeida²,

Fradin

et al. 2012

Expert Review of Dermatology

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Enhancement of bioavailability by lowering of fat content in topical formulations

Abstract: The rate of penetration of the active ingredients was inversely related to the lipid content, i.e. simple changes of the cosmetic properties by modifications of the lipid content may affect the efficacy of a formulation.

Cited by 28 publications

References 18 publications

Tissue viability imaging: Microvascular response to vasoactive drugs induced by iontophoresis

Tissue viability imaging: Microvascular response to vasoactive drugs induced by iontophoresis

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

Delivery of drugs applied topically to the skin

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