In vitro permeation through porcine buccal mucosa of caffeic acid phenetyl ester (CAPE) from a topical mucoadhesive gel containing propolis

Ceschel, G. C.; Maffei, Paola; Sforzini, A.; Borgia, S. Lombardi; Yasin, A.; Ronchi, Celestino

doi:10.1016/s0367-326x(02)00190-9

Cited by 47 publications

(21 citation statements)

References 13 publications

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“…20 -25 Concerning vascular disease, CAPE also inhibited NF-B activation in rat carotid arteries induced by balloon injury in vivo. 13 As Ceschel et al reported that CAPE has good permeability across mucosa in vitro, 26 CAPE may also have good bioavailability pharmacologically in vivo.…”

Section: Discussionmentioning

confidence: 99%

Oral Flavonoid Supplementation Attenuates Atherosclerosis Development in Apolipoprotein E–Deficient Mice

Hishikawa

Nakaki

Fujita

2005

ATVB

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Objective-Caffeic acid phenethyl ester (CAPE), a natural flavonoid, specifically blocks activation of nuclear factor-B (NF-B). We examined the effects of oral CAPE supplementation on atherogenesis in apolipoprotein E-deficient (apoEϪ/Ϫ) mice. Methods and Results-Ten-week-old male apoEϪ/Ϫ mice were supplemented orally with CAPE (30 mg/kg body weight) for 12 weeks. At the end of administration, atherosclerosis progression, NF-B activity, gene expression profiling by microarray analysis, and oxidative stress were studied. Treatment of apoEϪ/Ϫ mice with CAPE significantly reduced aortic atherosclerosis, NF-B activity, and expression of NF-B-related genes in the aorta. Moreover, expression of other gene clusters such as basic transcription factors, growth factors, cytokines, cell adhesion proteins, and extracellular matrix were also significantly reduced by treatment with CAPE. Plasma isoprostane level in apoEϪ/Ϫ mice was also significantly reduced by CAPE. Conclusion-In N uclear factor-B (NF-B) is a good therapeutic targetfor cardiovascular disease, 1,2 and numerous efforts are being made to develop safe NF-B inhibitors. Among the candidates are natural flavonoids, which constitute a promising class of dietary antioxidants that are found ubiquitously in fruits, vegetables, and tea. For example, resveratol, which is found in red wine, can inhibit NF-B activity, the abrogation of which may contribute to the ability of red wine to reduce mortality from coronary heart disease and cancer. 3,4 Curcumin, another NF-B inhibitor, is an effective inhibitor of tumor initiation and promotion in different carcinogen-induced models. 5 Among these natural flavonoids, the most promising is caffeic acid phenethyl ester (CAPE), which is structurally related to 3,4-dihydroxycinnamic acid and can be obtained from propolis, a honey constituent. 6 CAPE is the only compound that has been shown to inhibit the HIV integrase enzyme needed for integration of HIV DNA into the host genome 7 and is a potent and specific NF-B inhibitor. 8 We clarified recently that CAPE induced apoptosis in human breast cancer cells, but not in normal cells, by inhibiting NF-B, leading to fas aggregation. 9 The present studies were designed to examine whether CAPE could prevent atherosclerosis by inhibiting NF-B activity in vivo. Methods Animals and CompoundAll experimental procedures were in accordance with institutional guidelines for animal research. Apolipoprotein E-deficient (apoEϪ/Ϫ) mice were purchased from Taconic. CAPE was obtained from Bachem AG. ApoEϪ/Ϫ mice received CAPE-supplemented chow for 12 weeks. Compliance with CAPE supplementation was confirmed by measuring the consumption of chow supplemented with CAPE every day. The average chow intake was 5 to 6 g per day in control and CAPE-supplemented groups. Quantitation of Aortic AtherosclerosisThe extent of atherosclerosis in the mouse aorta was determined using an en-face method. 10 Aortas were fixed in paraformaldehyde and stained with oil red O. Morphometric image analysis of the captured digitali...

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Section: Discussionmentioning

confidence: 99%

Oral Flavonoid Supplementation Attenuates Atherosclerosis Development in Apolipoprotein E–Deficient Mice

Hishikawa

Nakaki

Fujita

2005

ATVB

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“…The receiver chambers of these diffusion cells are typically maintained at 37°C while the donor chamber is kept at ambient temperature, typically 22-24°C (31)(32)(33)(34)(35)(36)(37)(38)(39)(40)(41)(42)(43). Such an experimental setup for in vitro permeation studies across the buccal mucosa does not mimic the in vivo condition.…”

Section: Introductionmentioning

confidence: 99%

Effect of Experimental Temperature on the Permeation of Model Diffusants Across Porcine Buccal Mucosa

Kulkarni

Ravichandran

et al. 2011

AAPS PharmSciTech

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Abstract. The influence of experimental temperature on the permeability of model diffusants across porcine buccal mucosa was investigated in vitro. The permeability increased significantly as the experimental temperature was increased in increments of approximately 7°C. It was observed that the apparent permeability and temperature were related by an exponential relationship that conformed to the Arrhenius equation. Diffusants with higher lipophilicities-buspirone and bupivacaine-had lower activation energies for diffusion when compared to hydrophilic diffusants-antipyrine and caffeine. The activation energy for diffusion of the model diffusants decreased linearly with increasing distribution coefficients across porcine buccal mucosa. The results suggested that the buccal mucosa acts as a stronger barrier to the diffusion of hydrophilic diffusants than the lipophilic ones. The log-linear relationship between permeability and temperature indicates that temperature should be carefully controlled in diffusion experiments. These results also point to the possibility of developing heat-generating buccal delivery devices, especially for hydrophobic diffusants.

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“…So far, several methods have been developed for the determination of CAPE using high performance liquid chromatography connected to ultraviolet detector (HPLC-UV) [26,33,34], liquid chromatography mass spectrometry (LC-MS) [35] and LC-MS/MS [36,37]. Moreover, a variety of methods has been established to identity or quantify CA in various matrices including plant tissues [38][39][40][41], rat plasma [42,43], human plasma [44,45] and human serum [46].…”

Section: Introductionmentioning

confidence: 99%

Simultaneous determination of caffeic acid phenethyl ester and its metabolite caffeic acid in dog plasma using liquid chromatography tandem mass spectrometry

Tang

Sojinu

2012

Talanta

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In vitro permeation through porcine buccal mucosa of caffeic acid phenetyl ester (CAPE) from a topical mucoadhesive gel containing propolis

Cited by 47 publications

References 13 publications

Oral Flavonoid Supplementation Attenuates Atherosclerosis Development in Apolipoprotein E–Deficient Mice

Oral Flavonoid Supplementation Attenuates Atherosclerosis Development in Apolipoprotein E–Deficient Mice

Effect of Experimental Temperature on the Permeation of Model Diffusants Across Porcine Buccal Mucosa

Simultaneous determination of caffeic acid phenethyl ester and its metabolite caffeic acid in dog plasma using liquid chromatography tandem mass spectrometry

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