title: Phospholipid deformable vesicles for buccal delivery of insulin.
abstract: To investigate the possibility of the enhancing effect of deformable vesicles on buccal delivery of insulin, two kinds of vesicles with and without the presence of sodium deoxycholate (deformable vesicles and conventional vesicles) were prepared by reverse phase evaporation methods. The liposomal entrapment efficiency was determined by column chromatography. The particle size and morphology of the vesicles were also evaluated. The hypoglycemic effects, insulin concentrations, and residual amounts of insulin deposited in the buccal membrane after buccal administration of insulin vesicles to rabbits were investigated. Compared with subcutaneous administration of insulin solution, the relative pharmacological bioavailability and the relative bioavailability of buccal administration of insulin vesicles were determined. The results showed that the entrapment efficiencies of the deformable and conventional vesicles were 18.87+/-1.78% (n=3) and 22.07+/-2.16% (n=3), respectively. The particle sizes of the deformable and conventional vesicles were 42.5+/-20.5 nm and 59.7+/-33.8 nm, respectively. There were no significant differences in appearance between the two types of vesicle. Compared with subcutaneous administration of insulin solution, the relative pharmacological bioavailability and the relative bioavailability in the insulin-deformable vesicles group were 15.59% and 19.78%, respectively, which were higher than in the conventional insulin vesicles (p<0.05), blank deformable vesicles and insulin mixture groups (p<0.05). Deformable vesicles have an enhancing effect on buccal delivery of insulin and may be a better carrier than conventional vesicles for buccal delivery of protein drugs.
authors.affiliation: Department of Pharmaceutics, Peking University School of Pharmaceutical Sciences, Beijing, PR China.
authors.forename: Tian-Zhi
authors.initials: TZ
authors.lastname: Yang
authors.forename: Xiang-Tao
authors.initials: XT
authors.lastname: Wang
authors.forename: Xue-Ying
authors.initials: XY
authors.lastname: Yan
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhang
mesh_terms: D000278:Administration, Buccal; D000818:Animals; D001682:Biological Availability; D001786:Blood Glucose / Q000187:drug effects; D002610:Cheek / Q000502:physiology; D004337:Drug Carriers; D016503:Drug Delivery Systems; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics; D007328:Insulin / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics; D008297:Male; D023421:Models, Animal; D010743:Phospholipids / Q000737:chemistry*; D011817:Rabbits
chemical_list: D001786:Blood Glucose; D004337:Drug Carriers; D007004:Hypoglycemic Agents; D007328:Insulin; D010743:Phospholipids