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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.


Related in: MedlinePlus

In vivo data obtained from the glutathione (GSH) dosage in whole blood are reported. Results are expressed as mean ± SD in nmol GSH per gram of Hb at different experimental times T30 and T60 versus basal (before starting orobuccal fast-slow release tablet absorption). Statistical analysis was carried out using repeated measures analysis of variance in order to compare the mean values at subsequent times. The GSH level increased significantly (∗p = 0.014) with absorption time.
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fig3: In vivo data obtained from the glutathione (GSH) dosage in whole blood are reported. Results are expressed as mean ± SD in nmol GSH per gram of Hb at different experimental times T30 and T60 versus basal (before starting orobuccal fast-slow release tablet absorption). Statistical analysis was carried out using repeated measures analysis of variance in order to compare the mean values at subsequent times. The GSH level increased significantly (∗p = 0.014) with absorption time.

Mentions: The analysis of the obtained results in acute study showed a fast absorption of the glutathione through the in vivo oral mucosa. GSH blood concentration was increased both 30 minutes and 60 minutes after taking the orobuccal fast-slow GSH release formulation compared to the basal time before starting absorption. This increase was statistically significant when comparing the baseline concentration levels and those of concentration after 30 and 60 minutes. It could therefore be inferred that GSH was actually absorbed through mucous membrane, in a rapid manner, going to increase the quantity of reduced glutathione present in the blood (as it was expressed in Table 4 and represented in Figure 3). Finally, obtained in vivo results suggested that glutathione, taken by tablets with orobuccal fast-slow release, showed good bioavailability. Optimized orobuccal fast-slow release tablet was able to increase GSH blood level.


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 vivo data obtained from the glutathione (GSH) dosage in whole blood are reported. Results are expressed as mean ± SD in nmol GSH per gram of Hb at different experimental times T30 and T60 versus basal (before starting orobuccal fast-slow release tablet absorption). Statistical analysis was carried out using repeated measures analysis of variance in order to compare the mean values at subsequent times. The GSH level increased significantly (∗p = 0.014) with absorption time.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig3: In vivo data obtained from the glutathione (GSH) dosage in whole blood are reported. Results are expressed as mean ± SD in nmol GSH per gram of Hb at different experimental times T30 and T60 versus basal (before starting orobuccal fast-slow release tablet absorption). Statistical analysis was carried out using repeated measures analysis of variance in order to compare the mean values at subsequent times. The GSH level increased significantly (∗p = 0.014) with absorption time.
Mentions: The analysis of the obtained results in acute study showed a fast absorption of the glutathione through the in vivo oral mucosa. GSH blood concentration was increased both 30 minutes and 60 minutes after taking the orobuccal fast-slow GSH release formulation compared to the basal time before starting absorption. This increase was statistically significant when comparing the baseline concentration levels and those of concentration after 30 and 60 minutes. It could therefore be inferred that GSH was actually absorbed through mucous membrane, in a rapid manner, going to increase the quantity of reduced glutathione present in the blood (as it was expressed in Table 4 and represented in Figure 3). Finally, obtained in vivo results suggested that glutathione, taken by tablets with orobuccal fast-slow release, showed good bioavailability. Optimized orobuccal fast-slow release tablet was able to increase GSH blood level.

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.


Related in: MedlinePlus