Influence of polymers ratio on insulin-loaded nanoparticles based on poly-epsilon-caprolactone and Eudragit RS for oral administration.
Nanoparticles loaded with two different commercial insulins (Actrapid, Novorapid and based on different blends of a biodegradable polyester (poly-epsilon-caprolactone) and a polycationic non-biodegradable acrylic polymer (Eudragit RS) were characterized in vitro. The zeta potential was positive whenever Eudragit RS was part of the nanoparticles matrix. The encapsulation efficiency was ~ 96% except for Novorapid-loaded particles of poly-epsilon-caprolactone (only 35%). In vitro release studies revealed a burst release from nanoparticles, which may be of interest for oral delivery. Novorapid-loaded nanoparticles were orally administered to diabetic rats and allowed the glycemia to be decreased when compared with free nanoparticles.
Laboratory of Pharmaceutical Technology, School of Pharmacy, Nancy, France.
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D000180:Acrylic Resins / Q000008:administration & dosage / Q000737:chemistry*; D000284:Administration, Oral; D000818:Animals; D001672:Biocompatible Materials / Q000008:administration & dosage / Q000737:chemistry*; D001786:Blood Glucose / Q000032:analysis; D003921:Diabetes Mellitus, Experimental / Q000097:blood / Q000188:drug therapy; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D004339:Drug Compounding; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000627:therapeutic use; D007328:Insulin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000627:therapeutic use; D061267:Insulin Aspart; D061389:Insulin, Regular, Pork; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D011091:Polyesters / Q000008:administration & dosage / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D013311:Streptozocin
D000180:Acrylic Resins; D001672:Biocompatible Materials; D001786:Blood Glucose; D004337:Drug Carriers; D007004:Hypoglycemic Agents; D007328:Insulin; D061389:Insulin, Regular, Pork; D011091:Polyesters; C016240:polycaprolactone; C050528:Eudragit RS; D013311:Streptozocin; C000006:insulin, neutral; D061267:Insulin Aspart