中国中药杂志

2020, v.45(21) 5177-5183

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载五味子乙素F127修饰脂质聚合物纳米粒抑制乳腺癌肺转移的研究
Preparation and evaluation of schisandrin B-loaded F127 modified lipid-polymer nanoparticles for inhibition of breast cancer lung metastasis

闫飞;施江培;陈海珍;沈君怡;谢杏梅;蒋自飞;顾笑妍;刘颖;冯年平;
YAN Fei;SHI Jiang-pei;CHEN Hai-zhen;SHEN Jun-yi;XIE Xing-mei;JIANG Zi-fei;GU Xiao-yan;LIU Ying;FENG Nian-ping;School of Pharmacy, Shanghai University of Traditional Chinese Medicine;

摘要(Abstract):

构建载五味子乙素(schisandrin B,SchB)F127修饰脂质聚合物纳米粒(SchB-F-LPNs),增强SchB抑制乳腺癌转移的作用。采用改良的纳米沉淀法制备纳米粒。SchB-F-LPNs形态圆整,具有壳核结构,平均粒径为(234.60±6.11) nm,Zeta电位为(-5.88±0.49) mV。XRD分析结果表明SchB以无定形状态存在于脂质聚合物纳米粒中。F-LPNs体外猪黏液层穿越表观渗透系数是LPNs的1.43倍。大鼠口服体内药动学研究结果表明SchB混悬剂组、SchB-LPNs组和SchB-F-LPNs组C_(max)分别为(369.06±146.94),(1 121.34±91.65),(2 951.91±360.53)μg·L~(-1),以SchB混悬剂为参比制剂,SchB-F-LPNs的相对口服生物利用度为568.60%。SchB-F-LPNs可抑制在转化生长因子-β1(transforming growth factor-β1,TGF-β1)诱导下乳腺癌4T1细胞上皮间质转化产生的形态变化。此外,SchB-F-LPNs可显著降低4T1荷瘤小鼠肺转移结节数,揭示其具有抑制乳腺癌肺转移的作用。SchB-F-LPNs在抑制乳腺癌肺转移方面可能具有良好的潜力和应用前景。
In the current study, schisandrin B(SchB)-loaded F127 modified lipid-polymer hybrid nanoparticles(SchB-F-LPNs) were developed to improve the inhibition of breast cancer lung metastasis. Modified nanoprecipitation method was used to prepare SchB-F-LPNs. The nanoparticles were spherical in shape with shell-core structure by TEM observation. SchB-F-LPNs showed a mean particle size of(234.60±6.11) nm with zeta potential of(-5.88±0.49) mV. XRD results indicated that SchB existed in the nanoparticles in an amorphous state. The apparent permeability coefficient through porcine mucus of F-LPNs was 1.43-fold of that of LPNs as shown in the in vitro mucus penetration study. The pharmacokinetics study showed that the C_(max) of SchB was(369.06±146.94) μg·L~(-1),(1 121.34±91.65) μg·L~(-1) and(2 951.91±360.53) μg·L~(-1) respectively in SchB suspensions group, SchB-LPNs group and SchB-F-LPNs group after oral administration in rats. With SchB suspensions as the reference formulation, the relative bioavailability of SchB-F-LPNs was 568.60%. SchB-F-LPNs inhibited the morphological change during transforming growth factor-β1(TGF-β1)-induced epithelial-mesenchymal transition. In addition, SchB-F-LPNs significantly decreased the number of metastatic pulmonary nodules in 4 T1 tumor-bearing mice, suggesting that SchB-F-LPNs may inhibit the metastasis of breast cancer. These results reveal the promising potential of SchB-F-LPNs in treatment of breast cancer lung metastasis.

关键词(KeyWords): 五味子乙素;F127修饰脂质聚合物纳米粒;乳腺癌肺转移;口服;生物利用度;TGF-β1
schisandrin B;F127 modified lipid-polymer nanoparticles;breast cancer lung metastasis;oral administration;bioa-vailability;TGF-β1

Abstract:

Keywords:

基金项目(Foundation): 国家自然科学基金项目(81773913)

作者(Author): 闫飞;施江培;陈海珍;沈君怡;谢杏梅;蒋自飞;顾笑妍;刘颖;冯年平;
YAN Fei;SHI Jiang-pei;CHEN Hai-zhen;SHEN Jun-yi;XIE Xing-mei;JIANG Zi-fei;GU Xiao-yan;LIU Ying;FENG Nian-ping;School of Pharmacy, Shanghai University of Traditional Chinese Medicine;

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DOI: 10.19540/j.cnki.cjcmm.20200819.305

参考文献(References):

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