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Surface-modified PLGA nanoparticles with chitosan for oral delivery of tolbutamide

2017; Elsevier BV; Volume: 161; Linguagem: Inglês

10.1016/j.colsurfb.2017.10.037

1873-4367

Yongli Shi, Jintao Xue, Liyun Jia, Qian Du, Jie Niu, Dongyang Zhang,

Hydrogels: synthesis, properties, applications

The main purpose of present study was to develop novel chitosan-modified polylactic-co-glycolicacid nanoparticles ([email protected] NPs) for improving the bio-availability of tolbutamide (TOL). The TOL-loaded [email protected] NPs ([email protected] NPs) were fabricated with the solvent evaporation method. The cargo-free [email protected] NPs showed a diameter of 228.3 ± 2.5 nm monitored with a laser light particlesizer, and the transmission electron microscope (TEM) photographs revealed their "core-shell" structures. The Zeta potential of the original PLGA NPs and the cargo-free [email protected] NPs was measured to be −20.2 ± 3.21 mV and 24.2 ± 1.1 mV, respectively. The changes in Zeta potential indicated the CS chains were coated on the surfaces of the original PLGA NPs. The thermal gravity analysis (TGA) curves suggested that the CS chains improved the thermostability of the original PLGA NPs. The results of cells viability indicated the cargo-free [email protected] NPs were nontoxicity. The in vitro release profiles suggested that [email protected] NPs could release TOL in pH 7.4 phosphate buffer solution (PBS) at a sustained manner. Streptozotocin (STZ) was employed to build the diabetic rat models. The physiological changes in the islet β cells confirmed the obtaining of diabetic rats. After treatment by gavage, the [email protected] NPs showed an excellent hypoglycemic effect. Therefore, the [email protected] NPs had a potential application in oral delivery of TOL.