Efficient delivery of ursolic acid by poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles for inhibiting the growth of hepatocellular carcinoma in vitro and in vivo.
Efficient delivery of ursolic acid by poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles for inhibiting the growth of hepatocellular carcinoma in vitro and in vivo.
复制标题
聚（N-乙烯基吡咯烷酮）-嵌段聚（ε-己内酯）纳米颗粒有效递送熊果酸，抑制体内外肝细胞癌的生长
DOI：
10.2147/ijn.s77125
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发表时间：
2015
影响因子：
8
通讯作者：
Sun W
中科院分区：
文献类型：
--
作者：
Zhang H;Zheng D;Ding J;Xu H;Li X;Sun W
以前的报道表明，熊果酸（UA）是一种从毛蕨根中提取的五环三萜，可以抑制一系列癌细胞的生长。然而，UA的临床应用潜力受到其溶解度差的极大阻碍，而UA的疏水性使其成为纳米级递送系统的有前途的模型药物。在本研究中，我们将UA装入两亲性聚（n -乙烯基吡咯烷酮）-嵌段聚（ε-己内酯）纳米颗粒中，并对其进行了理化表征和释放能力分析。体外实验表明，UA- nps比游离UA更有效地抑制肝癌细胞的生长和诱导细胞凋亡。此外，与同等剂量的UA相比，UA- nps显著延迟肿瘤生长并定位于肿瘤部位。此外，Western blotting和免疫组化均提示，UA-NPs的高效化可能与细胞凋亡相关蛋白的调控有关。因此，UA-NPs显示出作为肝癌治疗的纳米药物系统的潜力。
Previous reports have shown that ursolic acid (UA), a pentacyclic triterpenoid derived from Catharanthus trichophyllus roots, could inhibit the growth of a series of cancer cells. However, the potential for clinical application of UA is greatly hampered by its poor solubility, whereas the hydrophobicity of UA renders it a promising model drug for nanosized delivery systems. In the current study, we loaded UA into amphiphilic poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles and performed physiochemical characterization as well as analysis of the releasing capacity. In vitro experiments indicated that UA-NPs inhibited the growth of liver cancer cells and induced cellular apoptosis more efficiently than did free UA. Moreover, UA-NPs significantly delayed tumor growth and localized to the tumor site when compared with the equivalent dose of UA. In addition, both Western blotting and immunohistochemistry suggested that the possible mechanism of the superior efficiency of UA-NPs is mediation by the regulation of apoptosis-related proteins. Therefore, UA-NPs show potential as a promising nanosized drug system for liver cancer therapy.