Effect of l-menthol and 1,8-cineole on phase behavior and molecular organization of SC lipids and skin permeation of zidovudine

Narishetty, Sunil T.; Panchagnula, Ramesh

doi:10.1016/j.jconrel.2004.09.016

Cited by 113 publications

(63 citation statements)

References 39 publications

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“…The formation of hydrogen bonding between SLS and ceramide head groups may consequently induce the disruption of lateral hydrogen-bond networks of the SC lipid bilayer as previously described for terpene penetration enhancers. 24) At the highest concentration of 5% (w/v) SLS, the permeation enhancement effect could also be possibly related to the interaction of SLS with the protein domain in the SC. The cationic surfactant, CTAB, facilitated model drugs across shed skin by interacting with the SC through electrostatic and hydrophobic links.…”

Section: Mechanism(s) Of Surfactants As Skin Penetration Enhancersmentioning

confidence: 99%

“…These bands occurred near 2920 and 2850 cm , which correspond to asymmetric υ a (CH 2 ) and symmetric υ s (CH 2 ) vibrations, respectively. [24][25][26] The C-H 2 symmetric and asymmetric stretches are often used to study the alterations of SC lipid hydrocarbon chain packing and possible conformational changes induced by chemical enhancers. Normally, hydrocarbons within the lipid domain below their transition temperature exist in a trans conformation.…”

Section: 22)mentioning

confidence: 99%

“…When the lipid domain becomes fluidized, a trans gauche shift to a higher frequency (blue shift) occurs. [24][25][26][27] The intensity of a band (height and …”

Section: 22)mentioning

confidence: 99%

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Evaluation of the Mechanism of Skin Enhancing Surfactants on the Biomembrane of Shed Snake Skin

Wonglertnirant

Ngawhirunpat

Kumpugdee-Vollrath

2012

Biological & Pharmaceutical Bulletin

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The aim of the present work was to investigate the effects of different surfactants at various concentrations as a skin penetration enhancer through the biomembrane of the shed skin of Naja kaouthia. Additionally, the enhancer mechanism(s) of each class of surfactants were evaluated using physical characterization techniques, such as scanning electron microscopy (SEM), attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy, and small and wide angle X-ray scattering (SWAXS). Our results showed that skin permeability increased with increasing concentrations of surfactants and the degree of increase was higher for the model hydrophilic permeant, deuterium dioxide (D 2 O), than the lipophilic permeant, ketoprofen (KP). Ionic surfactants, sodium lauryl sulfate (SLS) and cetyl trimethyl ammonium bromide (CTAB), demonstrated higher enhancement ability than the polyoxyethylene (20) sorbitan mono-oleate (Tween 80) non-ionic surfactant, which was consistent with the results from physical characterization studies. Increasing amounts of permeated drug resulted in an increase in membrane interactions. From our observations, it can be assumed that SLS and CTAB can be localized inside the biomembrane and thereby enhance drug permeation mainly through interactions with intercellular lipids in the stratum corneum (SC) and the creation of a perturbed microenvironment among lipid alkyl chains and polar head groups.Key words surfactant; shed snake skin; enhancer mechanism; permeation; attenuated total reflectance-Fourier transform infrared spectroscopy; small-wide angle X-ray scattering The barrier function of the skin resides in the stratum corneum (SC), the outermost layer of the skin. Its multilayered wall-like structure contains terminally differentiated keratin-rich epidermal cells that are embedded in an intercellular lipid-rich matrix.

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Section: Mechanism(s) Of Surfactants As Skin Penetration Enhancersmentioning

confidence: 99%

Section: 22)mentioning

confidence: 99%

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Evaluation of the Mechanism of Skin Enhancing Surfactants on the Biomembrane of Shed Snake Skin

Wonglertnirant

Ngawhirunpat

Kumpugdee-Vollrath

2012

Biological & Pharmaceutical Bulletin

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“…Hence, delivery from a non-oral pathway such as transdermal route may be helpful in maintaining suitable plasma concentration and could be useful in improving bioavailability and patient compliance and in avoiding side effects (7,8). The benefits of transdermal delivery of AZT are well appreciated in the literatures (7,(9)(10)(11)(12). AZT is a polar molecule; diffusion of AZT across highly lipophilic stratum corneum is poor and below the level to achieve effective therapeutic plasma concentration (9).…”

Section: Introductionmentioning

confidence: 99%

“…The benefits of transdermal delivery of AZT are well appreciated in the literatures (7,(9)(10)(11)(12). AZT is a polar molecule; diffusion of AZT across highly lipophilic stratum corneum is poor and below the level to achieve effective therapeutic plasma concentration (9). Hence, using iontophoresis could be an effective enhancer in achieving therapeutic plasma levels for AZT.…”

Section: Introductionmentioning

confidence: 99%

Studies on Transdermal Delivery Enhancement of Zidovudine

2009

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Abstract. The purpose of this study was to investigate physicochemical characteristics and in vitro release of zidovudine from monolithic film of Eudragit RL 100 and ethyl cellulose. Films included 2.5% or 5% (w/w) zidovudine of the dry polymer weight were prepared in various ratios of polymers by solvent evaporation method from methanol/acetone solvent mixture. The release studies were carried out by vertical Franz cells (2.2 cm 2 area, 20 ml receptor fluid). Ex vivo studies were done on Wistar rat skin within the films F6 (Eudragit RL100) and F7 (Eudragit RL100/Ethylcellulose, 1:1) consisting 5% (w/w) zidovudine in comparison with the same amount of free drug. Either iontophoresis (0.1 and 0.5 mA/cm 2 direct currents, Ag/AgCl electrodes) or dimethyl sulfoxide (pretreatment of 1% and 5%, w/w, solutions) were used as enhancers. Films consisting of ethyl cellulose under the ratio of 50% (w/w) gave similar release profiles, and the highest in vitro cumulative released amount was achieved with F6 film which gave the closest results with the free drug. This result could be due to the high swelling capacity and recrystallization inhibition effect of RL 100 polymer which also influenced the film homogenization. All the films were fitted to Higuchi release kinetics. It was also observed that both 0.5-mA/cm 2 current and 5% (w/w) dimethyl sulfoxide applications significantly increased the cumulative permeated amount of zidovudine after 8 h; however, the flux enhancement ratio was higher for 0.5-mA/cm 2 current application, especially within F6 film. Thus, it was concluded that Eudragit RL100 film (F6) could be further evaluated for the transdermal application of zidovudine.

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Eucalyptus oil nanoemulsion for enhanced skin deposition of fluticasone propionate in psoriatic plaques: A combinatorial anti‐inflammatory effect to suppress implicated cytokines

Ashraf,

El‐Sawy,

El Zaafarany

et al. 2024

Archiv der Pharmazie

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Psoriasis is a chronic inflammatory skin disease that affects patients' quality of life. This study aimed to enhance the efficacy of topical application of fluticasone propionate (FP) using a eucalyptus oil‐based nanoemulsion, an oil possessing anti‐inflammatory activity and extracted from the leaves, fruits, and buds of Eucalyptus globulus or Eucalyptus maidenii, to improve the skin deposition of FP and aid its anti‐inflammatory effect. Box‐Behnken design was employed to optimize NE formulations, which were characterized for globule size, zeta potential, polydispersity index, rheological behavior, microscopic morphology, ex vivo skin permeation/deposition, and in vivo efficacy using imiquimod‐induced psoriatic lesions. The optimized formulation depicted a droplet size of 188 ± 22.4 nm, a zeta potential of −17.63 ± 1.66 mV, and a viscosity of 204.9 mPa s. In addition to the increased FP retention in different skin layers caused by the NE and the reduced PASI score compared to the marketed cream, the levels of inflammatory cytokines IL‐1α, IL‐6, IL17a were markedly lowered, indicating the improved anti‐psoriatic curable efficacy of the optimized formulation in comparison to the FP‐marketed product.

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Effect of l-menthol and 1,8-cineole on phase behavior and molecular organization of SC lipids and skin permeation of zidovudine

Cited by 113 publications

References 39 publications

Evaluation of the Mechanism of Skin Enhancing Surfactants on the Biomembrane of Shed Snake Skin

Evaluation of the Mechanism of Skin Enhancing Surfactants on the Biomembrane of Shed Snake Skin

Studies on Transdermal Delivery Enhancement of Zidovudine

Eucalyptus oil nanoemulsion for enhanced skin deposition of fluticasone propionate in psoriatic plaques: A combinatorial anti‐inflammatory effect to suppress implicated cytokines

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