Evaluation of starch-maltodextrin-Carbopol 974 P mixtures for the nasal delivery of insulin in rabbits.
In this study insulin was administered nasally to rabbits as a dry powder formulation. The powders consisted of drum-dried waxy maize starch (DDWM) or maltodextrins with different DE values and Carbopol 974 P. The powders were prepared by freeze-drying a dispersion of these excipients with insulin. Bioavailabilities obtained with the powder formulations containing DDWM/Carbopol 974 P (5 and 10%) were significantly higher (p<0.05) than those containing maltodextrins-Carbopol 974 P mixtures. The bioavailability of the powder formulation containing DDWM and 10% Carbopol 974 P was significantly higher (14.4%) than the bioavailability of the same mixture containing 5% Carbopol 974 P (9.9%). The bioavailability, t(max) and C(max) values of the formulation with 5% Carbopol 974 P were significantly higher in comparison with the formulation without Carbopol 974 P. 10% Carbopol 974 P was required when maltodextrins were used in order to obtain a significantly higher bioavailability compared with the formulations without Carbopol 974 P. Freeze-drying seemed a prerequisite for a good bioavailability from the powder formulation as well as the ratio of insulin versus bioadhesive powder (1 IU and 2 IU/mg of bioadhesive powder).
Callens
C
C
Laboratory of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, University of Gent, Harelbekestraat 72, B-9000, Gent, Belgium.
Remon
J P
JP
D000179:Acrylates; D000281:Administration, Intranasal; D000818:Animals; D005612:Freeze Drying; D007328:Insulin / Q000008:administration & dosage*; D007700:Kinetics; D011134:Polysaccharides; D011817:Rabbits; D013213:Starch
D000179:Acrylates; D007328:Insulin; D011134:Polysaccharides; C117167:carbopol 974P NF; C008315:maltodextrin; D013213:Starch