Formulation and evaluation of lactoferrin bioadhesive tablets

• Published in: International journal of pharmaceutics 2007-10, Vol.343 (1), p.220-227
• Main Authors: Takahashi, Y., Takeda, C., Seto, I., Kawano, G., Machida, Y.
• Format: Article
• Language: English
• Subjects: Absorption; Adhesives - administration & dosage; Adhesives - chemistry; Adhesives - therapeutic use; Administration, Buccal; Animals; Bioadhesive tablets; Biological and medical sciences; Chemistry, Pharmaceutical; Chronic inflammation; Excipients; General pharmacology; Humans; Lactoferrin; Lactoferrin - administration & dosage; Lactoferrin - chemistry; Lactoferrin - therapeutic use; Male; Medical sciences; Mice; Mice, Inbred Strains; Mouth Mucosa - chemistry; Oral mucosa; Oral Ulcer - drug therapy; Oral Ulcer - pathology; Particle Size; Pectin; Pectins - administration & dosage; Pectins - chemistry; Pectins - therapeutic use; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Rats; Rats, Sprague-Dawley; Tablets; Tensile Strength; Water - chemistry; Xylitol
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2007.05.032

For the treatment of chronic inflammation in the oral cavity, we attempted to develop bioadhesive tablets of bovine lactoferrin (B-LF) which has antibacterial properties and immune regulatory functions. B-LF tablets containing pectin, tamarind gum or carboxymethylcellulose (CMC) were prepared by direct compression. Tablets consisting of B-LF, pectin and xylitol passed through 60- or 100-mesh sieves were also prepared. The tablets containing CMC had insufficient bioadhesive force. Although the tablets containing tamarind gum showed the longest residence time in the oral cavity, an unpleasant taste gradually developed. The tablets containing pectin showed the highest value of bioadhesive force and the taste was acceptable. The characteristics of the B-LF tablets were improved by adding an appropriate amount of xylitol and using the ingredients sieved by a 100-mesh sieve. The therapeutic effect was evaluated by using rats with an ulcer on the oral mucosa. In the present study, swelling on the periphery of the ulcer was observed after administration of the B-LF tablets, and then the ulcer has reduced overall.