Pluronic F-127 gels incorporating highly purified unsaturated fatty acids for buccal delivery of insulin.
The present study investigated the release profiles of insulin from Pluronic F-127 (PF-127) gel containing unsaturated fatty acids such as oleic acid (18:1), eicosapentaenoic acid (20:5) or docosahexaenoic acid (22:6) and the hypoglycemic effect of insulin following the buccal administration of the gel formulations in normal rats. Insulin release from the gels decreased in the presence of unsaturated fatty acids. Remarkable and continuous hypoglycemia was induced by all PF-127 gels (insulin dose, 25 IU/kg) containing unsaturated fatty acids. PF-127 gels containing oleic acid showed the highest pharmacological availability (15.9+/-7.9%). Our finding demonstrate that 20% PF-127 gels containing unsaturated fatty acids are potential formulations for the buccal delivery of insulin.
Morishita
M
M
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Hoshi University, Ebara 2-4-41, Shinagawa, 142-8501, Tokyo, Japan. morisita@hoshi.ac.jp
Barichello
J M
JM
Takayama
K
K
Chiba
Y
Y
Tokiwa
S
S
Nagai
T
T
D000818:Animals; D002610:Cheek; D005231:Fatty Acids, Unsaturated / Q000008:administration & dosage*; D005782:Gels; D007328:Insulin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D009061:Mouth Mucosa / Q000378:metabolism*; D020442:Poloxamer / Q000008:administration & dosage*; D051381:Rats; D017208:Rats, Wistar; D013501:Surface-Active Agents / Q000008:administration & dosage*
D005231:Fatty Acids, Unsaturated; D005782:Gels; D007328:Insulin; D013501:Surface-Active Agents; D020442:Poloxamer