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Levels of sirolimus in saliva and blood following mouthwash application
Z Nudelman1, M Friedman, D Barasch
1Department of Pharmaceutics, Faculty of Medicine, The Institute for Drug Research, School of Pharmacy, The Hebrew University, Jerusalem, Israel.
Objectives:
Sirolimus (rapamycin) is a mammalian target of rapamycin (mTOR) inhibitor with antiproliferative activity. Its systemic administration is currently evaluated for the management of squamous cell carcinoma and various oral disorders. Topical oral application can enhance availability, efficacy and improve safety and compliance. Our objective was to evaluate the release profile and the safety of a sirolimus mouthwash.
Subjects And Methods:
A sirolimus mouthwash (0.05 mg ml(-1) ) was applied to ten healthy male volunteers. Saliva and blood samples were taken after rinsing. Mass spectrometry and chemiluminescent microparticle immunoassay were used to determine saliva and blood levels of sirolimus. A topical oral release profile measurement and safety evaluation were performed.
Results:
After rinsing with the mouthwash, a classic immediate release profile was noted in the oral cavity. Extremely high initial sirolimus levels rapidly declined over a 4-hour period. Systemic exposure was limited, with a maximum level significantly lower than therapeutic doses, and safety was confirmed.
Conclusions:
A single rinse with sirolimus mouthwash leads to high transient levels of the drug in the saliva. Although levels were variable, a therapeutic concentration was achieved topically along with minimal systemic absorption. These results broaden the potential clinical use of oral topical rapalogs.
Insights
A sirolimus mouthwash provides high, temporary drug levels in saliva for topical treatment. This method shows minimal systemic absorption, confirming its safety and potential for oral conditions.
Area of Science:
- Pharmacology
- Drug Delivery
- Oral Medicine
Background:
- Sirolimus (rapamycin) is an mTOR inhibitor with antiproliferative properties.
- Systemic sirolimus is explored for oral cancers and disorders.
- Topical oral delivery may improve efficacy, safety, and patient compliance.
Purpose of the Study:
- To assess the release profile of sirolimus from a mouthwash formulation.
- To evaluate the safety of topical oral sirolimus application.
- To determine sirolimus concentrations in saliva and blood after mouthwash use.
Main Methods:
- Ten healthy male volunteers used a sirolimus mouthwash (0.05 mg/mL).
- Saliva and blood samples were collected post-rinsing.
- Mass spectrometry and immunoassay quantified sirolimus levels.
- Topical release and safety were assessed.
Main Results:
- An immediate release profile was observed in the oral cavity.
- High initial salivary sirolimus levels rapidly decreased within 4 hours.
- Systemic exposure was minimal, with peak blood levels below therapeutic doses.
- The mouthwash was confirmed to be safe.
Conclusions:
- A single sirolimus mouthwash rinse achieves high, transient salivary drug concentrations.
- Variable but therapeutically relevant topical levels were reached with minimal systemic absorption.
- These findings support the expanded clinical application of oral topical rapalogs.
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