Influence of d-limonene on the transdermal penetration of felodipine

Diez, I.; Peraire, Concepción; Obach, R.; Domènech, Josep Mestres i

doi:10.1007/bf03189820

Cited by 12 publications

(5 citation statements)

References 14 publications

(7 reference statements)

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“…Thus, we decided to continue with PG, OA and L at concentrations that give physically stable formulations (Table II). Previous studies on similar topics also helped us to confirm concentrations of selected penetration enhancers [10,34]. We also saw that OA and L were physically incompatible with G and OC, respectively.…”

Section: Ex Vivo Skin Permeation and Penetration Studysupporting

confidence: 60%

Influence of Vehicles and Penetration Enhancers on Anti-Inflammatory Effect of 18-Β Glycyrrhetinic Acid: Kinetic Modelling of Drug Release, in Vivo and Ex Vivo Experiments

Karaman¹,

Çelik²,

Özdemir³

et al. 2020

FARMACIA

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Topical formulations of 18-β glycyrrhetinic acid (18-β GA) were designed for use in relieving inflammatory and painful conditions of the skin. Formulations were containing penetration enhancers that differ in penetration enhancing mechanisms. Anti-inflammatory effects of formulations and effects of penetration enhancers on penetration and permeation of the drug through rat skin were investigated. The total amount of 18-β GA permeated from the base oil/water emulsion (53.19 ± 22.25 mcg/cm 2 ) was approximately twice higher than the base oleaginous cream (29.17 ± 3.85 mcg/cm 2 ) while there was no 18-β GA permeation from the base hydrogel formulation to the skin (p < 0.05). Incorporation of propylene glycol was generally found to increase 18-β GA permeation to the skin. The highest oedema inhibiting activity was achieved in the oil/water emulsion containing propylene glycol followed by the base oil/water emulsion without a penetration enhancer (p < 0.05). This result was consistent with the ex vivo study. Limonene and oleic acid were found to be insufficient in 18-β GA permeation to the skin. RezumatAu fost elaborate formulări topice ale acidului gliciretinic 18-β (GA 18-β), cu promotori de penetrare, pentru utilizarea acestora în ameliorarea bolilor inflamatorii ale pielii. Au fost cercetate efectele antiinflamatoare ale formulărilor și efectele promotorilor de penetrare asupra penetrării și permeării medicamentului prin pielea șobolanului. Cantitatea totală de 18-β GA pătrunsă în piele din emulsia de bază U/A (53,19 ± 22,25 mcg/cm 2 ) a fost aproximativ de două ori mai mare decât din crema oleaginoasă (29,17 ± 3,85 mcg/cm 2 ). Nu a existat o permeare de 18-β GA din formularea hidrogelului de bază (p < 0,05). Încorporarea propilenglicolului a crescut permeabilitatea GA-18-β în piele. Cea mai mare activitate de inhibare a edemelor a fost obținută cu emulsia U/A conținând propilenglicol, urmată de emulsia U/A de bază fără promotor de penetrare (p < 0,05). Acest rezultat a fost în concordanță cu studiul ex vivo. Limonenul și acidul oleic s-au dovedit a fi insuficiente în creșterea permeabilității GA-18-β prin piele.

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Section: Ex Vivo Skin Permeation and Penetration Studysupporting

confidence: 60%

Influence of Vehicles and Penetration Enhancers on Anti-Inflammatory Effect of 18-Β Glycyrrhetinic Acid: Kinetic Modelling of Drug Release, in Vivo and Ex Vivo Experiments

Karaman¹,

Çelik²,

Özdemir³

et al. 2020

FARMACIA

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“…17 However, other in vitro studies reported no appreciable differences in transdermal penetration of certain drugs when d -limonene was used between 1% and 10% concentrations. 18…”

Section: Discussionmentioning

confidence: 99%

“…17 However, other in vitro studies reported no appreciable differences in transdermal penetration of certain drugs when d-limonene was used between 1% and 10% concentrations. 18 The reaffirmation of a lack of significant human skin penetration of d-limonene is also interesting in light of the use of d-limonene as a penetration enhancer of various chemicals. 19,20 However, the percutaneous enhancing properties of limonene depend on its interaction with compounds such as propylene glycol and in most cases, penetration enhancement has been documented at levels (usually greater than 5%) that are much higher than those used in fragrance and cosmetic uses (maximum level 3.5%).…”

Section: Discussionmentioning

confidence: 99%

The Fate of Dermally Applied [¹⁴C]d-Limonene in Rats and Humans

Api

Ritacco

Hawkins³

2013

Int J Toxicol

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The fate of dermally applied [(14)C]d-limonene was evaluated in humans and Long-Evans rats. In rats, 5 mg/kg body weight of [(14)C]d-limonene applied dermally to the shaved back under occlusion, resulted in the absorption of approximately 12% of the dose. The absorbed d-limonene was completely metabolized and excreted rapidly, primarily from the urine (80%) with a small fraction (20%) excreted in the feces. There was no long-term retention of the test material in body tissues. In humans, following dermal application of 12 mg of [(14)C]d-limonene in ethanol (1 mL) to the back under nonocclusive conditions (for 1 h after application to allow the material to dry, thereafter under occlusion), only 0.16% of the dose was absorbed and the radioactivity was recovered from the urine. Radioactivity in human feces was below the limit of detection. These results indicate that under conditions of simulated use of fragrances and cosmetics, d-limonene has a low potential for dermal absorption and tissue accumulation, and the d-limonene that is absorbed is rapidly excreted in the urine. Based upon these findings and the knowledge that d-limonene possesses a low-systemic toxicity profile, it is reasonable to conclude that dermal exposure to d-limonene from fragrance and cosmetic applications is highly unlikely to result in any clinically significant human toxicity.

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“…The existence of d-limonene in the felodipine transdermal formulation has produced an increase in the permeability of the drug through skin 34 .…”

Section: D-limonenementioning

confidence: 99%

Oils as Penetration Enhancers for Improved Transdermal Drug Delivery: A Review

Lakshmi¹,

K²,

Prasanthi³

et al. 2017

Int. Res. J. Pharm.

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Transdermal drug delivery system is the most suitable system for delivering the drugs with shorter half-life and poor solubility. It improves the drug safety and therapeutic efficacy as the drug delivery through it occurs in a controlled manner. Interpretation of the biochemical composition and barrier function exerted by the stratum corneum has lead for the exploration of different sources for improving the percutaneous absorption. Skin is the suitable site for drug administration for local and systemic actions. Penetration enhancement is an improving technology that leads to the increase in the count of drugs for TDDS. The present review reports the role of Natural oils in enhancing the permeation of drugs through skin because of possessing different features like natural origin, favorable penetration enhancement and partitioning action in the skin by the oils. Various natural oils, their classification and influence as penetration enhancers were discussed in this study.

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Influence of d-limonene on the transdermal penetration of felodipine

Cited by 12 publications

References 14 publications

Influence of Vehicles and Penetration Enhancers on Anti-Inflammatory Effect of 18-Β Glycyrrhetinic Acid: Kinetic Modelling of Drug Release, in Vivo and Ex Vivo Experiments

Influence of Vehicles and Penetration Enhancers on Anti-Inflammatory Effect of 18-Β Glycyrrhetinic Acid: Kinetic Modelling of Drug Release, in Vivo and Ex Vivo Experiments

The Fate of Dermally Applied [¹⁴C]d-Limonene in Rats and Humans

Oils as Penetration Enhancers for Improved Transdermal Drug Delivery: A Review

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Influence of d-limonene on the transdermal penetration of felodipine

Cited by 12 publications

References 14 publications

Influence of Vehicles and Penetration Enhancers on Anti-Inflammatory Effect of 18-Β Glycyrrhetinic Acid: Kinetic Modelling of Drug Release, in Vivo and Ex Vivo Experiments

Influence of Vehicles and Penetration Enhancers on Anti-Inflammatory Effect of 18-Β Glycyrrhetinic Acid: Kinetic Modelling of Drug Release, in Vivo and Ex Vivo Experiments

The Fate of Dermally Applied [14C]d-Limonene in Rats and Humans

Oils as Penetration Enhancers for Improved Transdermal Drug Delivery: A Review

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Product

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The Fate of Dermally Applied [¹⁴C]d-Limonene in Rats and Humans