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 (pϽ0.05), blank deformable vesicles and insulin mixture groups (pϽ0.05). 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.

Eudragit S100 entrapped insulin microspheres for oral delivery

“…1 The delivery of insulin by nonparenteral routes has gained significant attention over last 2 decades. The alternate routes explored are ocular, 2,3 nasal, 4 buccal, 5,6 rectal, 7 pulmonary, 8,9 and oral. 10,11 Among all of the alternative routes of administration of insulin, the oral route offers the maximum advantage in terms of patient compliance.…”

Novel noninvasive techniques in management of diabetes

“…Comparative result showed that 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). [141] However, Cornparisons calculated at each period PF-127 gel without fatty acid versus PF-127 gel containing oleic acid, EPA or DHA (*P < 0.01). [139] the effect of salivary scavenging and accidental swallowing of delivery system; barrier property of buccal mucosa stands as the major limitations in the development of buccal adhesive drug delivery systems.…”

Routes of administration of insulin

“…A novel type of highly deformable lipid vesicle (transferosome), composed of soybean phosphatidylcholine, cholesterol and sodium deoxycholate, has been developed in recent years to enhance insulin bioavailability [24]. Compared with the subcutaneous administration of insulin solution, the relative pharmacological bioavailability in the insulin-deformable vesicles group was 15.59% and 19.78%, respectively, which was higher than in the conventional insulin vesicles, blank deformable vesicles and insulin mixture groups.…”