Optimization of the preparation process of Xanthoceras sorbifolia Bunge saponin XS-8 chitosan nanoparticles and the study of their properties

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Abstract

In order to improve the bioavailability and ability to cross the blood-brain barrier of the larger molecular weight compound Xanthoceras sorbifolia Bunge saponin XS-8, the optimal conditions for the preparation of XS-8 chitosan nanoparticles were established. A series of characterization, property evaluation and cytological studies of XS-8 chitosan nanoparticles were carried out. The results showed that the angeloyl group of XS-8 was involved in the formation of nanoparticles and XS-8 was successfully loaded onto the surface of chitosan nanoparticles with uniform distribution by an encapsulation efficiency of 88.73%, drug loading of 8.97% and mean particle size of 258.4 ± 1.72 nm. The digestion rate of XS-8 chitosan nanoparticles in both intestinal and gastric juices was slower than that of XS-8, which will lead to the reduction of the stimulation damage to the gastrointestinal and digestive systems. PC12 cytology experiments showed that XS-8 chitosan nanoparticles had no significant effect on cell growth and the uptake of XS-8 chitosan nanoparticles by PC12 cells increased significantly in 1h and gradually raised with time. In vivo fluorescence distribution experiments in mice showed that XS-8 chitosan nanoparticles could cross the blood-brain barrier into the brain. All these results provided important data for the application of XS-8 in the treatment of AD and supplied a new solution strategy for the blood-brain barrier restricting the entry of drugs into the central nervous system.

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