In:
Chemical Biology & Drug Design, Wiley, Vol. 89, No. 3 ( 2017-03), p. 464-469
Abstract:
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.
Type of Medium:
Online Resource
ISSN:
1747-0277
,
1747-0285
DOI:
10.1111/cbdd.2017.89.issue-3
Language:
English
Publisher:
Wiley
Publication Date:
2017
detail.hit.zdb_id:
2216600-2
SSG:
12
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