Abstract: Effects of several transmucosal and transdermal absorption promoters on buccal insulin delivery in rats were evaluated. Insulin absorption has been assessed from cumulative response of serum glucose concentrations and by comparison with a s.c. insulin dose/response curve. In the absence of absorption promoters, buccal insulin was less than 7% as effective as s.c. insulin. The non-ionic surfactant, Brij78, obviously improved buccal insulin absorption, using phosphate buffer solution at pH 7.4 containing 5% adjuvant. One steroidal detergent, sodium deoxycholate, tested as absorption promoter was also effective. Another effective absorption promoter was sodium lauryl sulfate. In the presence of the most effective absorption-promoting systems, the pharmacological availability (PA) of buccal insulin was about one third as effective as s.c. insulin.

Key words: Insulin, Insulin, Buccal delivery, Buccal delivery, Absorption promoter, Absorption promoter