piperidines and sorbitan-monostearate

Niosomes, bilayer vesicles formed by the self-assembly of nonionic surfactants, are receiving increasing attention as potential oral drug delivery systems but the impact of niosomal formulation parameters on their oral capability has not been studied systematically. The aim of this study was to investigate the impact of surfactant composition and surface charge of niosomes in enhancing oral bioavailability of repaglinide (REG) as a BCS II model drug.. Niosomes (13 formulations) from various nonionic surfactants having HLB in the range of 4-28 (Tweens, Spans, Brijs, Myrj, poloxamer 188, TPGS and Labrasol) were prepared and characterized concerning their loading efficiency, hydrodynamic diameter, zeta potential, drug release profile, and stability. The oral pharmacokinetics of the selected formulations were studied in rats (8 in vivo groups).. The results revealed that type of surfactant markedly affected the in vitro and in vivo potentials of niosomes. The C. Cationic Tween 80-based niosomes may represent a promising platform to develop oral delivery systems for BCS II drugs.

Topics: Administration, Oral; Animals; Biological Availability; Caco-2 Cells; Carbamates; Drug Delivery Systems; Drug Liberation; Hexoses; Humans; Liposomes; Male; Piperidines; Polysorbates; Rats, Wistar; Surface-Active Agents