Levels of sirolimus in saliva and blood following oral topical sustained-release varnish delivery system application

Abstract

After an application of sirolimus sustained-release varnish drug delivery system, prolonged drug levels can be achieved in the saliva. The oral topical sirolimus concentrations were potentially therapeutic along with minimal systemic exposure. These results broaden the potential clinical use of sustained-release oral topical rapalogs.

Therapeutic drug monitoring of immunosuppressants by liquid chromatography–mass spectrometry

“…The authors reported subtherapeutic (~0.2 to 1.1 ng/mL) blood levels and considered the mouthwash safe, since there was minimal passage to blood. A similar study was performed with a sustained-release oral cavity release system, and similar sub-therapeutic blood levels were found in blood [45]. Due to the poor correlations of the drug levels between saliva and blood, salivary TDM does not seem practical at this time.…”

Recent advances in analytical methods for the therapeutic drug monitoring of immunosuppressive drugs

“…In addition to the blood samples for the TDM of ISDs, other potential and convenient specimens, including saliva, hair, and ocular fluids, have also been explored when whole‐blood levels are within the therapeutic range . Belostotsky et al investigated whether a reliable correlation exists between the saliva and whole‐blood TAC levels using an LC–MS/MS method.…”

Polymeric drug delivery systems for intraoral site‐specific chemoprevention of oral cancer

“…However, the systemic administration of multiple agents may not be an ideal approach due to significant adverse effects. Local drug delivery provides the flexibility of using different types of delivery systems (e.g., solution for field coverage, patch for limited coverage) or a polymeric system containing multiple agents for the effective management of OSCC, with no/minimal adverse effects . In addition, polymeric local drug delivery systems can be easily tuned for the short‐ and long‐term management of OSCC .…”

“…Oral solutions/rinses are prepared by dissolving chemopreventive agent(s) in a suitable liquid vehicle or solvent . The drug solution is either painted over the precancerous lesions using a brush/cotton wool or vigorously gargled in the mouth for 2–5 min .…”

“…The use of purified water as a vehicle for the intraoral delivery of black raspberry anthocyanins provided better aqueous stability and higher mucosal levels of anthocyanins . Aqueous‐based vehicles II and III contains numerous excipients, such as buffering agents, co‐solvents, flavoring and sweetening agents, preservatives, and antibacterial agents . Some of these agents can stimulate the release of saliva and enzymes (e.g., β‐glucosidase, lactase) into the mouth, which in turn may impact the stability of chemopreventive agents.…”