Chronic inflammation of the oral mucosa and gingiva is often observed accompanying intractable stomatitis.1) The stomatitis reduces the quality of life of patients because it brings intense pain and anorexia. The severity and duration of stomatitis are greatly influenced by immune responses and oral hygiene condition.
2)Lactoferrin, an iron-binding glycoprotein that consists of a single polypeptide chain, is an abundant protein in milk secretions.3) Lactoferrin is found in most exocrine secretions including tears, nasal secretions, saliva, intestinal mucus and genital secretions, 4,5) and is also identified as one of the major proteins present in neutrophils. 6) Lactoferrin shows its bactericidal effect by binding with iron ions that are essential for the growth of bacteria, [7][8][9] and also acts as a modulator for various immunologic functions.10) The bactericidal effect and the immune regulatory function of lactoferrin should act to prevent the deterioration of stomatitis. Previously, we prepared buccal adhesive tablets consisting of bovine lactoferrin (B-LF), pectin and xylitol and evaluated the ulcer healing effect of the tablets by using rats induced with buccal mucosal ulcer. From the results, the ulcer decreased significantly at the seventh day in the group treated with the B-LF tablets as compared with the untreated group. (The in vivo data was presented on the 125th annual meeting of the Pharmaceutical Society of Japan, 2005).Pectins are ionic plant polysaccharides that are widely used in the food industry for their gelling properties. Their main structural features consist of blocks of (1→4)-linked homogalacturonan interrupted by single (1→2)-linked rhamnose units. [11][12][13] The homogalacturonan blocks are copolymers of galacturonic acid and its methyl ester, and the degree of esterification characterizes the gelation of pectins. Fifty % or more of the carboxyl groups are methyl esterified in native pectins. They are categorized as highly methylated pectins (HM pectins). Pectins of lower ester content (LM pectins) can be prepared by controlled acid deesterification.14) As shown in Fig. 1, LM pectins readily form gels in aqueous solution by cross-linking with free Ca 2ϩ . [15][16][17][18] In this study, we attempted to investigate the influence of the degree of esterification and the molecular weight of pectins on the characteristics of B-LF bioadhesive tablets, because preparation characteristics such as bioadhesive force and B-LF release properties may influence the ulcer healing effect. Pectins of various degrees of esterification and LM pectins cross-linked with Ca 2ϩ were used to prepare B-LF bioadhesive tablets, and the usefulness of the pectins as a bioadhesive polymer were evaluated. Shinagawa-ku, Tokyo 142-8501, Japan. Received February 22, 2007; accepted May 12, 2007; published online May 14, 2007 For the treatment of chronic inflammation in the oral cavity, we attempted to develop bioadhesive tablets of bovine lactoferrin (B-LF). Pectin was used as a bioadhesive polymer, and the inf...