The effect of drug concentration on solvent activity in silicone membranes

Santos, P.; Machado, M. C. C.; Watkinson, Adam C.; Hadgraft, Jonathan; Lane, ME

doi:10.1016/j.ijpharm.2009.05.002

Cited by 21 publications

(10 citation statements)

References 27 publications

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“…Permeation studies of NIA from the three formulations were conducted using silicone membrane and porcine skin and with various amounts of formulations, namely infinite, pseudo finite and finite doses. The silicone membrane was selected as a model membrane because of its homogeneity and it also allows insight into the influence of excipients on membrane transport [14,15].…”

Section: Permeation and Mass Balance Resultsmentioning

confidence: 99%

In vitro permeation and disposition of niacinamide in silicone and porcine skin of skin barrier-mimetic formulations

Haque¹,

Lane²,

Sil³

et al. 2017

International Journal of Pharmaceutics

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Niacinamide (NIA) is an amide form of vitamin B3 which is used in cosmetic formulations to improve various skin conditions and it has also been shown to increase stratum corneum thickness following repeated application. In this study, three doses (5, 20 and 50μL per cm) of two NIA containing oil-in-water skin barrier-mimetic formulations were evaluated in silicone membrane and porcine ear skin and compared with a commercial control formulation. Permeation studies were conducted over 24h in Franz cells and at the end of the experiment membranes were washed and niacinamide was extracted. For the three doses, retention or deposition of NIA was generally higher in porcine skin compared with silicone membrane, consistent with the hydrophilic nature of the active. Despite the control containing a higher amount of active, comparable amounts of NIA were deposited in skin for all formulations for all doses; total skin absorption values (permeation and retention) of NIA were also comparable across all formulations. For infinite (50μL) and finite (5μL) doses the absolute permeation of NIA from the control formulation was significantly higher in porcine skin compared with both test formulations. This likely reflects differences in formulation components and/or presence of skin penetration enhancers in the formulations. Higher permeation for the 50 and 20μL dose was also evident in porcine skin compared with silicone membrane but the opposite is the case for the finite dose. The findings point to the critical importance of dose and occlusion when evaluating topical formulations in vitro and also the likelihood of exaggerated effects of excipients on permeation at infinite and pseudo-finite dose applications.

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Section: Permeation and Mass Balance Resultsmentioning

confidence: 99%

In vitro permeation and disposition of niacinamide in silicone and porcine skin of skin barrier-mimetic formulations

Haque¹,

Lane²,

Sil³

et al. 2017

International Journal of Pharmaceutics

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“…The parameters P 1 (P 1 = Kh) and P 2 (P 2 = D/h 2 ) were estimated as representative of the vehicle-skin partition and diffusion coefficients because of the impossibility of knowing the exact path length (h) for drug diffusion across human skin. The finite dose model equations used in the fitting of the permeation data obtained with skin and model membranes were those already described by Santos et al (2009) and Oliveira et al (2010), respectively. Permeability coefficients (k p in cm min −1 or cm h −1 ) and pseudo steady-state fluxes (J in mmol cm −2 min −1 or mmol cm −2 h −1 ) for the permeation of compounds across silicone membranes were calculated using the values for K, D, P 1 and P 2 obtained from Scientist ® following Eqs.…”

Section: Discussionmentioning

confidence: 99%

The influence of volatile solvents on transport across model membranes and human skin

Oliveira

Hadgraft

Lane

2012

International Journal of Pharmaceutics

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“…Numerous TSSs contain a nonvolatile chemical enhancer that may reduce the rate of drug precipitation. Since the drug usually has a higher solubility in the volatile solvent than in the chemical enhancer, the inclusion of chemical enhancers in these products should not compromise the favorable thermodynamic drug changes [35,39,44]. The impact of chemical enhancers on the viscosity of the drug film deposited on skin surface, and therefore drug diffusivity has not yet been evaluated.…”

Section: Drugmentioning

confidence: 99%

Spray-on transdermal drug delivery systems

Ibrahim

2014

Expert Opinion on Drug Delivery

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TSS is easily applied, delivering flexible drug dosage and associated with lower incidence of skin irritation. TSS provides a fast-drying product where the volatile solvent enables uniform drug distribution with minimal vehicle deposition on skin. TSS ensures precise dose administration that is aesthetically appealing and eliminates concerns of residual drug associated with transdermal patches. Furthermore, it provides a better alternative to traditional transdermal products due to ease of product development and manufacturing.

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The effect of drug concentration on solvent activity in silicone membranes

Cited by 21 publications

References 27 publications

In vitro permeation and disposition of niacinamide in silicone and porcine skin of skin barrier-mimetic formulations

In vitro permeation and disposition of niacinamide in silicone and porcine skin of skin barrier-mimetic formulations

The influence of volatile solvents on transport across model membranes and human skin

Spray-on transdermal drug delivery systems

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