Preparation and evaluation of a chitosan salt–poloxamer 407 based matrix for buccal drug delivery

• Published in: Journal of controlled release 2005-01, Vol.102 (1), p.159-169
• Main Authors: Cafaggi, S., Leardi, R., Parodi, B., Caviglioli, G., Russo, E., Bignardi, G.
• Format: Article
• Language: English
• Subjects: Administration, Buccal; Animals; Biological and medical sciences; Buccal delivery; Chitosan; Chitosan - administration & dosage; Chitosan - chemical synthesis; Chitosan - pharmacokinetics; Controlled release; Drug Delivery Systems - methods; Drug Evaluation, Preclinical - methods; General pharmacology; In Vitro Techniques; Medical sciences; Mouth Mucosa - drug effects; Mouth Mucosa - metabolism; Mucoadhesion; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Poloxamer - administration & dosage; Poloxamer - chemical synthesis; Poloxamer - pharmacokinetics; Poloxamer 407; Swine
• ISSN: 0168-3659; 1873-4995
• DOI: 10.1016/j.jconrel.2004.09.019

The aim of this work was to prepare and evaluate a matrix for buccal drug delivery composed of a chitosan salt and poloxamer 407. Different chitosan salts were formed by reacting chitosan with acetic, citric, and lactic acid. Various proportions of poloxamer 407 were added to the aqueous solution of chitosan salt, and the residue obtained by lyophilisation was compressed into discs, using a 30 kN compression force. An experimental design (3 2) was used to study the influence of the type of chitosan salt and of the relative amount of poloxamer on drug release capacity, swelling, erosion, and mucoadhesiveness of matrices. The results showed that matrix properties depended significantly on both relative amount of poloxamer and chitosan salt type. The rank orders of chitosan salts for the four processes evaluated were as follows: drug release: chitosan acetate>chitosan citrate>chitosan lactate; swelling: chitosan lactate>chitosan acetate=chitosan citrate; erosion: chitosan citrate>chitosan lactate>chitosan acetate; mucoadhesion: chitosan lactate>chitosan acetate=chitosan citrate. Mucoadhesion was particularly favoured when poloxamer 407 was present at about 30% (w/w). The matrix composed of chitosan lactate and poloxamer 407 showed the best characteristics for buccal administration.