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Berberine‐loaded Janus nanocarriers for magnetic field‐enhanced therapy against hepatocellular carcinoma
Author(s) -
Wang Zheng,
Wang Yingshuai,
Chang Zhimin,
Li Li,
Zhang Yi,
Lu Mengmeng,
Zheng Xiao,
Li Mingqiang,
Shao Dan,
Li Jing,
Chen Li,
Dong Wenfei
Publication year - 2017
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12866
Subject(s) - berberine , nanocarriers , hepatocellular carcinoma , chemistry , mesoporous silica , nanomedicine , bioavailability , endocytosis , pharmacology , cancer research , mesoporous material , nanotechnology , biophysics , drug delivery , materials science , nanoparticle , biochemistry , medicine , cell , biology , catalysis
Berberine, an bioactive isoquinolin alkaloid from traditional Chinese herbs, is considered to be a promising agent based on its remarkable activity against hepatocellular carcinoma. However, the clinical application of this nature compound had been hampered owing to its properties such as poor aqueous solubility, low gastrointestinal absorption, and reduced bioavailability. Therefore, we developed Janus magnetic mesoporous silica nanoparticles (Fe 3 O 4 ‐ mSiO 2 NP s) consisting of a Fe 3 O 4 head for magnetic targeting and a mesoporous SiO 2 body for berberine delivery. A pH ‐sensitive group was introduced on the surface of mesoporous silica for berberine loading to develop a tumor microenvironment‐responsive nanocarrier, which exhibited uniform morphology, good superparamagnetic properties, high drug‐loading amounts, superior endocytic ability, and low cytotoxicity. Berberine‐loaded Fe 3 O 4 ‐ mSiO 2 NP s exerted extraordinarily high specificity for hepatocellular carcinoma cells, which was due to the pH ‐responsive berberine release, as well as higher endocytosis capacity in hepatocellular carcinoma cells rather than normal liver cells. More importantly, an external magnetic field could significantly improve antitumor activity of Ber‐loaded Fe 3 O 4 ‐ mSiO 2 NP s through enhancing berberine internalization. Taken together, our results suggest that Janus nanocarriers driven by the magnetic field may provide an effective and safe way to facilitate clinical use of berberine against hepatocellular carcinoma.