title: Preparation and characterization of glycoprotein-resistant starch complex as a coating material for oral bioadhesive microparticles for colon-targeted polypeptide delivery.
abstract: For effective oral delivery of polypeptide or protein and enhancement their oral bioavailability, a new resistant starch-glycoprotein complex bioadhesive carrier and an oral colon-targeted bioadhesive delivery microparticle system were developed. A glycoprotein, concanavalin A (Con A), was successfully conjugated to the molecules of resistant starch acetate (RSA), leading to the formation of resistant starch-glycoprotein complex. This Con A-conjugated RSA film as a coating material showed an excellent controlled-release property. In streptozotocin (STZ)-induced type II diabetic rats, the insulin-loaded microparticles coated with this Con A-conjugated RSA film exhibited good hypoglycemic response for keeping the plasma glucose level within the normal range for totally 44-52 h after oral administration with different insulin dosages. Oral glucose tolerance tests indicated that successive oral administration of these colon-targeted bioadhesive microparticles with insulin at a level of 50 IU/kg could achieve a hypoglycemic effect similar to that by injection of insulin at 35 IU/kg. Therefore, the potential of this new Con A-conjugated RSA film-coated microparticle system has been demonstrated to be capable of improving the oral bioavailability of bioactive proteins and peptides.
authors: Wenbei
authors: W
authors: Situ
authors: Xiaoxi
authors: X
authors: Li
authors: Jia
authors: J
authors: Liu
authors: Ling
authors: L
authors: Chen
mesh_terms: D000818:Animals; D003106:Colon / Q000187:drug effects*; D003208:Concanavalin A / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000494:pharmacology*; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy*; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D005260:Female; D006023:Glycoproteins / Q000737:chemistry*; D006801:Humans; D007328:Insulin / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008819:Mice, Nude; D051381:Rats; D017207:Rats, Sprague-Dawley; D013213:Starch / Q000031:analogs & derivatives* / Q000737:chemistry
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D006023:Glycoproteins; D007328:Insulin; D003208:Concanavalin A; D013213:Starch; C050766:starch acetate
keywords: hypoglycemic response; oral colon-targeted bioadhesive delivery; polypeptide controlled-release; resistant starch; resistant starch−glycoprotein complex