Dermal penetration of propylene glycols: Measured absorption across human abdominal skin in vitro and comparison with a QSAR model

Fasano, William J.; Berge, W.F. ten; Banton, Marcy I.; Heneweer, Marjoke; Moore, Nigel P.

doi:10.1016/j.tiv.2011.07.003

Cited by 25 publications

(12 citation statements)

References 28 publications

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“…DiPG is a hydrophilic oligomer of PG, that has been widely used in skin formulations (Cosmetic Ingredient Review Expert Panel, 1985), but its effect on the skin barrier has not been studied in detail. Fasano et al (2011) investigated the permeation of both PG and DiPG across human abdominal skin using infinite dose in vitro studies under occlusion. The researchers also measured the skin impedance before and after the experiments.…”

Section: Permeation Studies Using Neat Solventsmentioning

confidence: 99%

Topical delivery of niacinamide: Influence of neat solvents

Iliopoulos¹,

Sil

Hossain³

et al. 2020

International Journal of Pharmaceutics

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Niacinamide (NIA) has been widely used in cosmetic and personal care formulations for several skin conditions. Permeation of topical NIA has been confirmed in a number of studies under infinite dose conditions. However, there is limited information in the literature regarding permeation of NIA following application of topical formulations in amounts that reflect the real-life use of such products by consumers. The aim of the present work was therefore to investigate skin delivery of NIA from single solvent systems in porcine skin under finite dose conditions. A secondary aim was to probe the processes underlying the previously reported low recovery of NIA following in vitro permeation and mass balance studies. The solubility and stability of NIA in various single solvent systems was examined.The solvents investigated included Transcutol® P (TC), propylene glycol (PG), 1-2 hexanediol (HEX), 1-2 pentanediol (1-2P), 1-5 pentanediol (1-5P), 1-3 butanediol (1-3B), glycerol (GLY) and dimethyl isosorbide (DMI). Skin permeation and deposition of the molecule was investigated in full thickness porcine skin in vitro finite dose Franz-type diffusion experiments followed by mass balance studies. Stability of NIA for 72 h in the solvents was confirmed. The solubility of NIA in the solvents ranged from 82.9 ± 0.8 to 311.9 ± 4.5 mg/mL. TC delivered the highest percentage permeation of NIA at 24 h, 32.6 ± 12.1 % of the applied dose. Low total recovery of NIA after mass balance studies was observed for some vehicles, with values ranging from 55.2 ± 12.8 % to 106.3 ± 2.3 %. This reflected the formation of a number of NIA degradation by-products in the receptor phase during the permeation studies. Identification of other vehicles for synergistic enhancement of NIA skin delivery will be the subject of future work.

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Section: Permeation Studies Using Neat Solventsmentioning

confidence: 99%

Topical delivery of niacinamide: Influence of neat solvents

Iliopoulos¹,

Sil

Hossain³

et al. 2020

International Journal of Pharmaceutics

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“…The in vitro settings commonly utilised include the Franz diffusion cell equipment 4. Animal models are also in use5–8; however, methods based on the physicochemical characteristic of the compound are now available and extensively developed to predict the fraction absorbed via the skin and its rate 9–11. Nonetheless, these models do not incorporate the inter‐individual variation of the skin constituents.…”

Section: Introductionmentioning

confidence: 99%

Prediction of Concentration–Time Profile and its Inter-Individual Variability following the Dermal Drug Absorption

Polak

Ghobadi

Mishra

et al. 2012

Journal of Pharmaceutical Sciences

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“…Since, for in vivo experiments of skin penetration, either on humans or animals, ethical principles must be considered there was a need to establish in vitro methods/models capable for dermal absorption prediction [ 10 , 11 ]. The number of in vitro methods for evaluation drugs skin permeability employs diffusion cells which typically consist of human or animal skin clip [ 12 , 13 , 14 ]. The quantitative structure-permeability relationships (QSPRs) models as well as chromatographic methods such as immobilized artificial membrane (IAM) or biopartitioning micelar chromatography (BMC) were also applied in dermal absorption prediction [ 8 , 14 , 15 , 16 ], but these methodologies do not fully reflect the human skin properties.…”

Section: Introductionmentioning

confidence: 99%

A PAMPA Assay as Fast Predictive Model of Passive Human Skin Permeability of New Synthesized Corticosteroid C-21 Esters

et al. 2012

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The permeation properties of twenty newly synthesized α-alkoxyalkanoyl and α-aryloxyalkanoyl C-21 esters of standard corticosteroids: Fluocinolone acetonide, dexamethasone, triamcinolone acetonide and hydrocortisone were established using a PAMPA assay (70% silicone oil and 30% isopropyl myristate). The data were compared with parent corticosteroids with addition of mometasone furoate and hydrocortisone acetate. All newly synthesized corticosteroid C-21 esters have effective permeability coefficients higher then -6, mostly followed with high values of retention factors and low permeation. The examined compounds were grouped through relationship between obtained retention factors and permeation parameters (groups I–III). The classification confirmed group I (membrane retentions as well as permeation lower then 30%) for all corticosteroid standards except mometasone furoate, a potent topical corticosteroid which, with high membrane retention (81%) and low permeation (7.7%) fits into group III. The largest number of new synthesized corticosteroids C-21 esters, among them all fluocinolone acetonide C-21 esters, have high membrane retentions (32.4%–86.5%) and low permeations (1.3%–27.1%), fitting in group III. The classification was related to previously obtained anti-inflammatory activity data for the fluocinolone acetonide C-21 esters series. According to the PAMPA results the new synthesized esters could be considered as potential new prodrugs with useful benefit/risk ratio.

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Dermal penetration of propylene glycols: Measured absorption across human abdominal skin in vitro and comparison with a QSAR model

Cited by 25 publications

References 28 publications

Topical delivery of niacinamide: Influence of neat solvents

Topical delivery of niacinamide: Influence of neat solvents

Prediction of Concentration–Time Profile and its Inter-Individual Variability following the Dermal Drug Absorption

A PAMPA Assay as Fast Predictive Model of Passive Human Skin Permeability of New Synthesized Corticosteroid C-21 Esters

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