期刊
JOURNAL OF PHARMACEUTICAL SCIENCES
卷 112, 期 3, 页码 718-730出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.xphs.2022.09.018
关键词
Diabetes; Enteric coating; Insulin; Polyelectrolyte complex nanoparticle; Oral administration
Insulin-loaded PEC nanoparticles were prepared and optimized for oral administration, showing potential for reducing side effects and mimicking physiological pathway. The nanoparticles were encapsulated in enteric-coated capsules and demonstrated a promising delivery system for oral insulin.
Insulin is one of the most important drugs in the treatment of diabetes. There is an increasing interest in the oral administration of insulin as it mimics the physiological pathway and potentially reduces the side effects associated with subcutaneous injection. Therefore, insulin-loaded polyelectrolyte complex (PEC) nanopar-ticles were prepared by the ionic cross-linking method using protamine sulfate as the polycationic and sodium alginate as the anionic polymer. Taguchi experimental design was used for the optimization of nano-particles by varying the concentration of sodium alginate, the mass ratio of sodium alginate to protamine, and the amount of insulin. The optimized nanoparticle formulation was used for further in vitro characteriza-tion. Then, insulin-loaded PEC nanoparticles were placed in hard gelatin capsules and the capsules were enteric-coated by Eudragit L100-55 (PEC-eCAPs). Hypoglycemic effects PEC-eCAPs were determined in vivo by oral administration to diabetic rats. Furthermore, in vivo distribution of PEC nanoparticles was evaluated by fluorescein isothiocyanate (FITC) labelled nanoparticles. The experimental design led to nanoparticles with a size of 194.4 nm and a polydispersity index (PDI) of 0.31. The encapsulation efficiency (EE) was calcu-lated as 95.96%. In vivo studies showed that PEC-eCAPs significantly reduced the blood glucose level of rats at the 8th hour compared to oral insulin solution. It was concluded that PEC nanoparticles loaded into enteric-coated hard gelatin capsules provide a promising delivery system for the oral administration of insulin.(c) 2022 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.
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