A Review on Terpenes as Skin Penetration Enhancers in Transdermal Drug Delivery

Lim, Perry Fung Chye; Liu, Xiang Yang; Chan, Sui Yung

doi:10.1080/10412905.2009.9700208

Cited by 14 publications

(10 citation statements)

References 49 publications

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“…They have been found as efficient penetration enhancers for drugs with differing lipophilicities. Terpenes were reported to cause no or minimal skin irritancy and they have reversible effects on skin lipids [ 20 , 38 , 39 , 40 , 41 ]. We studied the effect of three different types of terpenes including limonene (a hydrocarbon lipophilic monoterpene), nerolidol (an amphiphilic sesquiterpene) and eucalyptol (an oxygen containing monoterpene) on in vitro permeation characteristics of OND from chitosan transdermal films across pig skin.…”

Section: Resultsmentioning

confidence: 99%

Optimization and Characterization of Chitosan Films for Transdermal Delivery of Ondansetron

et al. 2013

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The aim of this study was to develop novel transdermal films of ondansetron HCl with high molecular weight chitosan as matrix polymer and 2-(2-ethoxy-ethoxy) ethanol (Transcutol®) as plasticizer. In this context, firstly the physicochemical properties of gels used to formulate transdermal films were characterized and, physicochemical properties and bioadhesiveness of the transdermal films prepared with chitosan gels were assessed. The impact of three different types of terpenes, namely limonene, nerolidol and eucalyptol on in vitro skin permeation of ondansetron from transdermal films were also examined. ATR-FTIR measurements were performed to investigate the effects of the chitosan film formulations on in vitro conformational order of stratum corneum intercellular lipids after 24 h permeation study. The results showed that the chitosan gels consisting of Transcutol® as plasticizer and terpenes as penetration enhancer may be used to prepare transdermal films of ondansetron due to the good mechanical properties and bioadhesiveness of the transdermal films. Eucalyptol (1%) showed higher permeation enhancer effect than the other terpenes and control. ATR-FTIR data confirmed that finding in which eucalyptol induced a blue shift in the both CH2 asymmetric and symmetric absorbance peak positions indicating increased lipid fluidity of stratum corneum.

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Section: Resultsmentioning

confidence: 99%

Optimization and Characterization of Chitosan Films for Transdermal Delivery of Ondansetron

et al. 2013

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“…To solve this problem, numerous techniques have been used, such as the use of permeation enhancers (PEs) [ 3 , 4 , 5 , 6 ]. Essential oils (or volatile oils) are a type of natural permeation enhancers that can effectively promote the permeation of both hydrophilic and hydrophobic drugs [ 7 , 8 , 9 ]. Essential oils are biocompatible with commonly-used chemical synthetics PEs because they are safe, non-toxic, pharmacologically inert, non-irritating, hypo-allergenic and have a wide range of pharmacological functions, such as anti-inflammatory and anticancer applications [ 10 , 11 , 12 , 13 ].…”

Section: Introductionmentioning

confidence: 99%

Effects of Concentrations on the Transdermal Permeation Enhancing Mechanisms of Borneol: A Coarse-Grained Molecular Dynamics Simulation on Mixed-Bilayer Membranes

Dai

Yin

Wan

et al. 2016

IJMS

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Borneol is a natural permeation enhancer that is effective in drugs used in traditional clinical practices as well as in modern scientific research. However, its molecular mechanism is not fully understood. In this study, a mixed coarse-grained model of stratum corneum (SC) lipid bilayer comprised of Ceramide-N-sphingosine (CER NS) 24:0, cholesterol (CHOL) and free fatty acids (FFA) 24:0 (2:2:1) was used to examine the permeation enhancing mechanism of borneol on the model drug osthole. We found two different mechanisms that were dependent on concentrations levels of borneol. At low concentrations, the lipid system maintained a bilayer structure. The addition of borneol made the lipid bilayer loosen and improved drug permeation. The “pull” effect of borneol also improved drug permeation. However, for a strongly hydrophobic drug like osthole, the permeation enhancement of borneol was limited. When most borneol molecules permeated into bilayers and were located at the hydrophobic tail region, the spatial competition effect inhibited drug molecules from permeating deeper into the bilayer. At high concentrations, borneol led to the formation of water pores and long-lived reversed micelles. This improved the permeation of osthole and possibly other hydrophobic or hydrophilic drugs through the SC. Our simulation results were supported by Franz diffusion tests and transmission electron microscope (TEM) experiments.

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“…Terpenes and terpenes‐rich essential oils are also common ingredients of topical formulations, where they are used as fragrance or as functional ingredients: antibacterial, antifungal, antiviral and skin protectant [10]. Natural terpenes and sesquiterpenes, particularly d ‐limonene, menthone, menthol, 1,8‐cineole and nerolidol are well‐known penetration enhancers [11–13], and in some cases raw essential oils have been used to increase topical absorption of selected drugs [14–16]. Interestingly, a recent investigation has shown cooperative effects even among single components of an essential oil in their diffusion through human epidermis [17]; therefore, knowledge developed using isolated terpenes might not be representative of the effect of natural essential oils.…”

Section: Introductionmentioning

confidence: 99%

Lemon (Citrus limon, Burm.f.) essential oil enhances the trans‐epidermal release of lipid‐ (A, E) and water‐ (B₆, C) soluble vitamins from topical emulsions in reconstructed human epidermis

Valgimigli

Gabbanini²,

Berlini

et al. 2012

Intern J of Cosmetic Sci

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Topical bioavailability of lipid- and water-soluble vitamins is a critical issue for protecting or anti-ageing formulations. Using 17-day-old SkinEthic(®) reconstructed human epidermis, we investigated (at 34°C) the role of lemon EO in enhancing the penetration of α-tocopherol (E) and retinyl acetate (A), pyridoxine (B(6)) and ascorbic acid (C), released from O/W or W/O emulsions. D-limonene, α-pinene and p-cymene (65.9, 2.2 and 0.5%w/w of the oil) had skin permeability coefficients Ps (10(-3) cm h(-1)) of 0.56 ± 0.03 (or 0.73 ± 0.02), 0.72 ± 0.05 (or 0.98 ± 0.05) and 0.84 ± 0.04 (or 1.14 ± 0.04), respectively, when incorporated in a W/O (or O/W) emulsion. Vitamins B6, C and A had Ps values of (3.0 ± 0.4) × 10(-3), (7.9 ± 0.6) × 10(-3) and (0.37 ± 0.02) × 10(-5) cm h(-1), respectively, and their flux through the skin was enhanced by a factor of 4.1, 3.4 and 5.8, respectively, in the presence of lemon EO. The penetration of vitamin E was nine-fold enhanced. Lemon EO produced only reversible modification of TEWL, and it is a safe and effective penetration enhancer for topical administration of lipid- and water-soluble vitamins.

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A Review on Terpenes as Skin Penetration Enhancers in Transdermal Drug Delivery

Cited by 14 publications

References 49 publications

Optimization and Characterization of Chitosan Films for Transdermal Delivery of Ondansetron

Optimization and Characterization of Chitosan Films for Transdermal Delivery of Ondansetron

Effects of Concentrations on the Transdermal Permeation Enhancing Mechanisms of Borneol: A Coarse-Grained Molecular Dynamics Simulation on Mixed-Bilayer Membranes

Lemon (Citrus limon, Burm.f.) essential oil enhances the trans‐epidermal release of lipid‐ (A, E) and water‐ (B₆, C) soluble vitamins from topical emulsions in reconstructed human epidermis

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A Review on Terpenes as Skin Penetration Enhancers in Transdermal Drug Delivery

Cited by 14 publications

References 49 publications

Optimization and Characterization of Chitosan Films for Transdermal Delivery of Ondansetron

Optimization and Characterization of Chitosan Films for Transdermal Delivery of Ondansetron

Effects of Concentrations on the Transdermal Permeation Enhancing Mechanisms of Borneol: A Coarse-Grained Molecular Dynamics Simulation on Mixed-Bilayer Membranes

Lemon (Citrus limon, Burm.f.) essential oil enhances the trans‐epidermal release of lipid‐ (A, E) and water‐ (B6, C) soluble vitamins from topical emulsions in reconstructed human epidermis

Contact Info

Product

Resources

About

Lemon (Citrus limon, Burm.f.) essential oil enhances the trans‐epidermal release of lipid‐ (A, E) and water‐ (B₆, C) soluble vitamins from topical emulsions in reconstructed human epidermis