Rassu Giovanna, Porcu Elena Piera, Fancello Silvia, Obinu Antonella, Senes Nina, Galleri Grazia, Migheli Rossana, Gavini Elisabetta, Giunchedi Paolo
Department of Chemistry and Pharmacy, University of Sassari, via Muroni 23/a, 07100 Sassari, Italy.
Department of Clinical and Experimental Medicine, University of Sassari, viale San Pietro 43/b, 07100 Sassari, Italy.
Pharmaceutics. 2018 Dec 29;11(1):8. doi: 10.3390/pharmaceutics11010008.
Genistein has been reported to have antioxidant and neuroprotective activity. Despite encouraging in vitro and in vivo results, several disadvantages such as poor water solubility, rapid metabolism, and low oral bioavailability limit the clinical application of genistein. The aim of this study was to design and characterize genistein-loaded chitosan nanoparticles for intranasal drug delivery, prepared by the ionic gelation technique by using sodium hexametaphosphate. Nanoparticles were characterized in vitro and their cytotoxicity was tested on PC12 cells. Genistein-loaded nanoparticles were prepared, and sodium hexametaphosphate was used as a valid alternative to well-known cross-linkers. Nanoparticle characteristics as well as their physical stability were affected by formulation composition and manufacturing. Small (mean diameters of 200⁻300 nm) and homogeneous nanoparticles were obtained and were able to improve genistein penetration through the nasal mucosa as compared to pure genistein. Nanoparticle dispersions showed a pH consistent with the nasal fluid and preserved PC12 cell vitality.
据报道，金雀异黄素具有抗氧化和神经保护活性。尽管体外和体内实验结果令人鼓舞，但金雀异黄素存在一些缺点，如水溶性差、代谢快和口服生物利用度低，限制了其临床应用。本研究的目的是设计并表征用于鼻内给药的载金雀异黄素壳聚糖纳米颗粒，采用离子凝胶技术，以六偏磷酸钠为交联剂制备。对纳米颗粒进行体外表征，并在PC12细胞上测试其细胞毒性。制备了载金雀异黄素纳米颗粒，六偏磷酸钠被用作知名交联剂的有效替代品。纳米颗粒的特性及其物理稳定性受制剂组成和制备工艺的影响。获得了小尺寸（平均直径为200⁻300 nm）且均匀的纳米颗粒，与纯金雀异黄素相比，其能够提高金雀异黄素透过鼻黏膜的能力。纳米颗粒分散体的pH与鼻液一致，并保留了PC12细胞的活力。
