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Bioavailability Study of an Innovative Orobuccal Formulation of Glutathione.

Buonocore D, Grosini M, Giardina S, Michelotti A, Carrabetta M, Seneci A, Verri M, Dossena M, Marzatico F - Oxid Med Cell Longev (2015)

Bottom Line: When circulating GSH decreases, oral administration might be considered a therapeutic benefit.In addition, in vivo results, obtained from 15 healthy volunteers, were in favor of GSH level improvement in blood showing fast (after 30 and 60 minutes) absorption through oral mucosa.In conclusion, the intake of GSH formulated through optimized orobuccal fast-slow release tablets gave positive results in raising GSH blood concentration.

View Article: PubMed Central - PubMed

Affiliation: Laboratory of Pharmacobiochemistry, Nutrition and Nutraceuticals, Department of Biology and Biotechnology "L. Spallanzani", University of Pavia, 27100 Pavia, Italy.

ABSTRACT
Alteration of the ubiquitous thiol tripeptide glutathione (GSH) is involved in oxidative stress, which plays a role in ageing; consequently, GSH is closely related to this process characterized by progressive decline in the efficiency of physiological function and increased susceptibility to disease. When circulating GSH decreases, oral administration might be considered a therapeutic benefit. Unfortunately, due to the hydrolysis of the tripeptide by intestinal γ-glutamyltransferase, dietary glutathione is not a major determinant for its increase. Aim of this work was to evaluate improvement of GSH systemic availability testing, in vitro and in vivo, an optimized orobuccal fast-slow release formulation tablet containing pure stabilized GSH. In vitro evaluation of the penetration capability of the innovative GSH-release formulation showed that GSH was well absorbed by the reconstructed oral epithelium and its absorption has features of time-dependence. In addition, in vivo results, obtained from 15 healthy volunteers, were in favor of GSH level improvement in blood showing fast (after 30 and 60 minutes) absorption through oral mucosa. In conclusion, the intake of GSH formulated through optimized orobuccal fast-slow release tablets gave positive results in raising GSH blood concentration.

No MeSH data available.


In vitro data obtained from the GSH dosage as % in the experimental model are reported. The percentage (%) of GSH absorption values are calculated on the applied amount of GSH (0.125 mg) and reported on the bases of single monitored experimental time as total % of absorption (mean ± standard deviation SD). Tissue ∗(%) value of GSH evaluated in the homogenized tissue is resized (10x).
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fig2: In vitro data obtained from the GSH dosage as % in the experimental model are reported. The percentage (%) of GSH absorption values are calculated on the applied amount of GSH (0.125 mg) and reported on the bases of single monitored experimental time as total % of absorption (mean ± standard deviation SD). Tissue ∗(%) value of GSH evaluated in the homogenized tissue is resized (10x).

Mentions: The amount of GSH released into the medium decreased over time: 0.069 mg after 10 minutes, 0.015 mg after 20 minutes, and almost (0.003 mg) after 60 minutes. These results showed that GSH within an orobuccal fast-slow release formulation was able to penetrate reconstructed human oral epithelium. Moreover, obtained data showed a very small capacity of the tissue to hold the absorbed glutathione, contributing to its bioavailability (Table 2, Figures 1 and 2). We found only 0.001 mg of GSH (100 parts less than the applied amount of 0.125 mg) in the homogenized tissue at the end of the experimental time.


Bioavailability Study of an Innovative Orobuccal Formulation of Glutathione.

Buonocore D, Grosini M, Giardina S, Michelotti A, Carrabetta M, Seneci A, Verri M, Dossena M, Marzatico F - Oxid Med Cell Longev (2015)

In vitro data obtained from the GSH dosage as % in the experimental model are reported. The percentage (%) of GSH absorption values are calculated on the applied amount of GSH (0.125 mg) and reported on the bases of single monitored experimental time as total % of absorption (mean ± standard deviation SD). Tissue ∗(%) value of GSH evaluated in the homogenized tissue is resized (10x).
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4663342&req=5

fig2: In vitro data obtained from the GSH dosage as % in the experimental model are reported. The percentage (%) of GSH absorption values are calculated on the applied amount of GSH (0.125 mg) and reported on the bases of single monitored experimental time as total % of absorption (mean ± standard deviation SD). Tissue ∗(%) value of GSH evaluated in the homogenized tissue is resized (10x).
Mentions: The amount of GSH released into the medium decreased over time: 0.069 mg after 10 minutes, 0.015 mg after 20 minutes, and almost (0.003 mg) after 60 minutes. These results showed that GSH within an orobuccal fast-slow release formulation was able to penetrate reconstructed human oral epithelium. Moreover, obtained data showed a very small capacity of the tissue to hold the absorbed glutathione, contributing to its bioavailability (Table 2, Figures 1 and 2). We found only 0.001 mg of GSH (100 parts less than the applied amount of 0.125 mg) in the homogenized tissue at the end of the experimental time.

Bottom Line: When circulating GSH decreases, oral administration might be considered a therapeutic benefit.In addition, in vivo results, obtained from 15 healthy volunteers, were in favor of GSH level improvement in blood showing fast (after 30 and 60 minutes) absorption through oral mucosa.In conclusion, the intake of GSH formulated through optimized orobuccal fast-slow release tablets gave positive results in raising GSH blood concentration.

View Article: PubMed Central - PubMed

Affiliation: Laboratory of Pharmacobiochemistry, Nutrition and Nutraceuticals, Department of Biology and Biotechnology "L. Spallanzani", University of Pavia, 27100 Pavia, Italy.

ABSTRACT
Alteration of the ubiquitous thiol tripeptide glutathione (GSH) is involved in oxidative stress, which plays a role in ageing; consequently, GSH is closely related to this process characterized by progressive decline in the efficiency of physiological function and increased susceptibility to disease. When circulating GSH decreases, oral administration might be considered a therapeutic benefit. Unfortunately, due to the hydrolysis of the tripeptide by intestinal γ-glutamyltransferase, dietary glutathione is not a major determinant for its increase. Aim of this work was to evaluate improvement of GSH systemic availability testing, in vitro and in vivo, an optimized orobuccal fast-slow release formulation tablet containing pure stabilized GSH. In vitro evaluation of the penetration capability of the innovative GSH-release formulation showed that GSH was well absorbed by the reconstructed oral epithelium and its absorption has features of time-dependence. In addition, in vivo results, obtained from 15 healthy volunteers, were in favor of GSH level improvement in blood showing fast (after 30 and 60 minutes) absorption through oral mucosa. In conclusion, the intake of GSH formulated through optimized orobuccal fast-slow release tablets gave positive results in raising GSH blood concentration.

No MeSH data available.