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

Carlos M. Ugalde, Zhongfa Liu, Chen Ren, Kenneth K. Chan, Kapila A. Rodrigo, Yhonghua Ling, Peter E. Larsen, Guillermo E. Chacon, Gary D. Stoner, Russell J. Mumper, Henry W. Fields, Susan R. Mallery

Research output: Contribution to journalArticlepeer-review

32 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)977-986
Number of pages10
JournalPharmaceutical Research
Issue number4
StatePublished - Apr 2009
Externally publishedYes


  • Anthocyanins
  • Black raspberries
  • Chemoprevention
  • Local delivery
  • Oral cancer

ASJC Scopus subject areas

  • Biotechnology
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry
  • Pharmacology (medical)


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