title: A quantitative evaluation of radiolabelled lectin retention on oral mucosa in vitro and in vivo.
abstract: Previous work has identified lectins that bind to the cells present on the oral mucosa for their potential use as a means of retaining a drug delivery system on the mucosal surfaces of the mouth. In this study, a radiolabelling technique was developed to allow the quantification of lectin binding to human buccal cells in vitro, and the retention of the lectins in the oral cavity of a rat model in vivo. Lectins were labelled with 99mTc using a cyclic diethylene triamine pentaacetic acid conjugation technique. In the in vitro study, human buccal cells were obtained by scraping the inner surface of the cheek. The suspended cells were exposed to the labelled lectin solution for 30 min and after washing with buffer the activity associated with the cells determined. In the in vivo study, male Wistar rats were briefly anaesthetized during which 10 microl of a solution containing labelled lectin was applied into the buccal pouch. At set times the rats were killed and the lower buccal cavity mucosal tissue and tongue dissected out and monitored for bound lectin. The in vitro study indicated that the lectins from Arachis Hypogaea, Canavalia ensiformis and Triticum vulgaris bound to oral mucosal cells. The T. vulgaris lectin showed the greatest binding, calculated to be 6.77 x 10(9) molecules per cell. The in vivo retention of C. ensiformis and T. vulgaris lectins on rat oral mucosal tissue was also evident. The T. vulgaris lectin showed significantly higher levels of retained lectin after 30 min (29.54 +/- 4.20 microg SD) on the oral mucosal tissue and 28.37 microg (+/-2.13 SD) on the tongue and was still detected at similar levels after 2 h. These studies indicate that significant lectin binding to human buccal cells occurs in vitro and retention in an animal model occurs for over 2 h in vivo. The T. vulgaris lectin showed most promise for further work.
authors.affiliation: Biomaterials and Drug Delivery Group, School of Pharmacy and Biomedical Sciences, University of Portsmouth, UK. john.smart@port.ac.uk
authors.forename: John D
authors.initials: JD
authors.lastname: Smart
authors.forename: Paul K K
authors.initials: PK
authors.lastname: Nantwi
authors.forename: David J
authors.initials: DJ
authors.lastname: Rogers
authors.forename: Keith L
authors.initials: KL
authors.lastname: Green
mesh_terms: D000818:Animals; D002478:Cells, Cultured; D004337:Drug Carriers / Q000378:metabolism*; D006801:Humans; D037102:Lectins / Q000378:metabolism; D008297:Male; D009061:Mouth Mucosa / Q000166:cytology / Q000378:metabolism*; D011869:Radioligand Assay; D051381:Rats; D016284:Technetium Tc 99m Pentetate
chemical_list: D004337:Drug Carriers; D037102:Lectins; D016284:Technetium Tc 99m Pentetate