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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

Date

01/13/2009

Pubmed ID

19137418

Pubmed Central ID

PMC2678548

DOI

10.1007/s11095-008-9806-x

Scopus ID

2-s2.0-61449102467 (requires institutional sign-in at Scopus site)   34 Citations

Abstract

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.

Author List

Ugalde CM, Liu Z, Ren C, Chan KK, Rodrigo KA, Ling Y, Larsen PE, Chacon GE, Stoner GD, Mumper RJ, Fields HW, Mallery SR



MESH terms used to index this publication - Major topics in bold

Adhesiveness
Administration, Oral
Administration, Topical
Adolescent
Adult
Anthocyanins
Anticarcinogenic Agents
Biotransformation
Chromatography, Liquid
Female
Gels
Humans
Male
Mouth
Oral Surgical Procedures
Plant Preparations
Rosaceae
Saliva
Tandem Mass Spectrometry
Tissue Distribution
Young Adult