ABSTRACT
Objective: To prepare foliate-conjugated chitosan nanoparticles loaded with berberine hydrochloride (BH/FA-CTS-NPs) and investigate the optimizing technology, physicochemical characterizations, and inhibitory effect on CNE-1. Methods: Folate-conjugated chitosan (FA-CTS) was prepared by amino reaction of folic acid active ester and chitosan molecules; BH/FA-CTS-NPs were prepared using ion cross-linking technique with BH as a model drug. The morphology, particle size, and physicochemical characteristics such as entrapment efficiency (EE), drug-loading, and release in vitro of nanoparticles were studied. The effect of cell anti-migratory and anti-invasive actions of BH/FA-CTS-NPs was investigated using MTT assays, wound healing assays and Annexin-V-FITC single staining assays, respectively. Results: The prepared BH/FA-CTS NPs were round, and the size uniformity adhesion was not found. The results of mean particle size, EE, and drug-loading amount were (282.4 ± 4.5) nm, (89.82 ± 2.91)%, and (9.16 ± 1.01)%, respectively. (80.32 ± 3.24)% of BH in nanoparticles was released within 5 h and then released slowly, and the accumulative release rate within 24 h was (90.92 ± 5.21)%. These results by MTT assay and wound healing assay indicated that BH/FA-CTS NPs not only inhibited the proliferation of CNE-1 cells in a concentration- and time-dependent manner, but can induced apoptosis. Conclusion: BH/FA-CTS NPs with the sustained release effect could be prepared successfully by the ionic crosslinking method. Considering these properties, block proliferation and impair the migration of the CNE-1 cell line, BH/FA-CTS NPs could be an important compound for consideration in the treatment of nasopharyngeal carcinoma.