Guo Yang, Zhong Ting, Duan Xiao-Chuan, Zhang Shuang, Yao Xin, Yin Yi-Fan, Huang Dan, Ren Wei, Zhang Qiang, Zhang Xuan
a Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, School of Pharmaceutical Sciences, Peking University , Beijing , China.
b Department of Pharmaceutics , School of Pharmaceutical Sciences, Peking University , Beijing , China , and.
Drug Deliv. 2017 Nov;24(1):270-277. doi: 10.1080/10717544.2016.1245371.
In the present study, we select the Sylysia 350 (Sylysia) as mesoporous material, distearoylphosphatidylethanolamine-poly(ethylene glycol) (DSPE-PEG) as absorption enhancer and hydroxy propyl methyl cellulose (HPMC) as crystallization inhibitor to prepare sorafenib tosylate (SFN) nanomitrix (MSNM@SFN) for improving the anti-tumor activity of SFN. The MSNM@SFN was prepared by solvent evaporation method. The solubility, dissolution, and bioavailability of SFN in MSNM@SFN were also investigated. The anti-tumor activity of MSNM@SFN was evaluated in vitro and in vivo. Our results indicated that the solubility and dissolution of SFN in MSNM@SFN were significantly increased. The oral bioavailability of SFN in MSNM@SFN was greatly improved 7.7-fold compared with that in SFN suspension. The enhanced anti-tumor activity of MSNM@SFN was confirmed in vitro and in vivo experiments. This nanomatrix developed in this study could be a promising drug delivery platform for improving the therapeutic efficacy of poorly water-soluble drugs.
在本研究中，我们选择Sylysia 350（硅藻土）作为介孔材料，二硬脂酰磷脂酰乙醇胺-聚乙二醇（DSPE-PEG）作为吸收增强剂，羟丙基甲基纤维素（HPMC）作为结晶抑制剂来制备甲苯磺酸索拉非尼（SFN）纳米基质（MSNM@SFN），以提高SFN的抗肿瘤活性。MSNM@SFN通过溶剂蒸发法制备。还研究了SFN在MSNM@SFN中的溶解度、溶出度和生物利用度。在体外和体内评估了MSNM@SFN的抗肿瘤活性。我们的结果表明，SFN在MSNM@SFN中的溶解度和溶出度显著提高。与SFN悬浮液相比，MSNM@SFN中SFN的口服生物利用度大大提高了7.7倍。在体外和体内实验中证实了MSNM@SFN增强的抗肿瘤活性。本研究开发的这种纳米基质可能是一个有前途的药物递送平台，用于提高难溶性药物的治疗效果。
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