Nanosphere based oral insulin delivery.
Zinc insulin is successfully encapsulated in various polyester and polyanhydride nanosphere formulations using Phase Inversion Nanoencapsulation (PIN). The encapsulated insulin maintains its biological activity and is released from the nanospheres over a span of approximately 6 h. A specific formulation, 1.6% zinc insulin in poly(lactide-co-glycolide) (PLGA) with fumaric anhydride oligimer and iron oxide additives has been shown to be active orally. This formulation is shown to have 11.4% of the efficacy of intraperitoneally delivered zinc insulin and is able to control plasma glucose levels when faced with a simultaneously administered glucose challenge. A number of properties of this formulation, including size, release kinetics, bioadhesiveness and ability to traverse the gastrointestinal epithelium, are likely to contribute to its oral efficacy.
Carino
G P
GP
Department of Molecular Pharmacology, Physiology and Biotechnology, Brown University, Providence, RI 02912, USA.
Jacob
J S
JS
Mathiowitz
E
E
D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001786:Blood Glucose / Q000378:metabolism; D002417:Cattle; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005951:Glucose Tolerance Test; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000097:blood / Q000494:pharmacology; D007274:Injections, Intraperitoneal; D007328:Insulin / Q000008:administration & dosage* / Q000097:blood / Q000494:pharmacology; D007408:Intestinal Absorption; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D010316:Particle Size; D051381:Rats
D001786:Blood Glucose; D007004:Hypoglycemic Agents; D007328:Insulin