Enhanced oral bioavailability and sustained delivery of glimepiride via niosomal encapsulation: in-vitro characterization and in-vivo evaluation.
This study was designed to investigate the potency of niosomes, for glimepiride (GLM) encapsulation, aiming at enhancing its oral bioavailability and hypoglycemic efficacy. Niosomes containing nonionic surfactants (NIS) were prepared by thin film hydration technique and characterized. In-vitro release study was performed using a dialysis technique. In-vivo pharmacodynamic studies, as well as pharmacokinetic evaluation were performed on alloxan-induced diabetic rats. GLM niosomes exhibited high-entrapment efficiency percentages (E.E. %) up to 98.70% and a particle size diameter ranging from 186.8 ± 18.69 to 797.7 ± 12.45 nm, with negatively charged zeta potential (ZP). Different GLM niosomal formulation showed retarded in vitro release, compared to free drug. In-vivo studies revealed the superiority of GLM niosomes in lowering blood glucose level (BGL) and in maintaining a therapeutic level of GLM for a longer period of time, as compared to free drug and market product. There was no significant difference between mean plasma AUC0-48 hrof GLM-loaded niosomes and that of market product. GLM-loaded niosomes exhibited seven-fold enhancement in relative bioavailability in comparison with free drug. These findings reinforce the potential use of niosomes for enhancing the oral bioavailability and prolonged delivery of GLM via oral administration.
a Pharmaceutical Technology Department , National Research Centre , Dokki, Cairo , Egypt.
Amira Mohamed
AM
Mohsen
a Pharmaceutical Technology Department , National Research Centre , Dokki, Cairo , Egypt.
Mona Mahmoud
MM
AbouSamra
b Narcotics, Poisons and Ergogenics Department, Medical Research Division , National Research Centre , Dokki, Cairo , Egypt.
Shaimaa Ahmed
SA
ElShebiney
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy*; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D008081:Liposomes / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013453:Sulfonylurea Compounds / Q000737:chemistry / Q000494:pharmacology*; D013501:Surface-Active Agents / Q000737:chemistry / Q000494:pharmacology*
D007004:Hypoglycemic Agents; D008081:Liposomes; D013453:Sulfonylurea Compounds; D013501:Surface-Active Agents; C057619:glimepiride
Glimepiride; antidiabetic; hypoglycemic; niosomes; oral bioavailability; sustained