Distribution of anthocyanins delivered from a bioadhesive black raspberry gel following topical intraoral application in normal healthy volunteers

Pharm Res. 2009 Apr;26(4):977-86. doi: 10.1007/s11095-008-9806-x. Epub 2009 Jan 10.


Purpose: Results from our oral cavity chemoprevention trial demonstrated appreciable interpatient variations regarding chemopreventive efficacy of a freeze dried black raspberry (FBR) gel. We speculated these data reflected individual patient-related differences in absorption, target tissue uptake and local compound metabolism of key FBR compounds (anthocyanins). Accordingly, this study assessed the distribution of anthocyanins from the 10% (w/w) FBR gel in saliva, oral tissues and plasma.

Methods: Human subject participation entailed collection of: (1) saliva, tissue and plasma (5 min following gel application, keratinized tissues), (2) saliva and plasma (5 min after sublingual gel application), (3) saliva and plasma at 1, 2, and 4 h post gel application (keratinized tissues), and (4) saliva (cyanidin 3-rutinoside incubations). Levels of FBR anthocyanins in the respective samples were analyzed by LC/MS/MS.

Results: Our data show: significantly higher anthocyanin levels in saliva and oral tissues relative to matched plasma samples, marked donor-specific variations in anthocyanin uptake, sustainability of anthocyanins at the target site, pH affects anthocyanin penetration and intraoral anthocyanin decomposition and/or metabolism.

Conclusions: No previous oral cavity chemoprevention trials evaluated compound distribution at the treatment site. Our data, which demonstrate a local delivery-derived pharmacologic advantage, provide insights which could advance oral cavity chemoprevention strategies.

Publication types

  • Clinical Trial
  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Adhesiveness
  • Administration, Oral
  • Administration, Topical
  • Adolescent
  • Adult
  • Anthocyanins / administration & dosage
  • Anthocyanins / blood
  • Anthocyanins / chemistry
  • Anthocyanins / pharmacokinetics*
  • Anticarcinogenic Agents / administration & dosage
  • Anticarcinogenic Agents / blood
  • Anticarcinogenic Agents / chemistry
  • Anticarcinogenic Agents / pharmacokinetics*
  • Biotransformation
  • Chromatography, Liquid
  • Female
  • Gels
  • Humans
  • Male
  • Mouth / metabolism*
  • Oral Surgical Procedures
  • Plant Preparations / pharmacokinetics
  • Rosaceae*
  • Saliva / metabolism*
  • Tandem Mass Spectrometry
  • Tissue Distribution
  • Young Adult


  • Anthocyanins
  • Anticarcinogenic Agents
  • Gels
  • Plant Preparations