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Drug Deliv. 2016 Nov;23(9):3674-3680. Epub 2016 Sep 30.

Sophoridine-loaded PLGA microspheres for lung targeting: preparation, in vitro, and in vivo evaluation.

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a School of Pharmacy, Ningxia Medical University , Yinchuan , Ningxia , China.
b Ningxia Engineering and Technology Research Center for Modernization of Hui Medicine & Key Lab of Hui Ethnic Medicine Modernization, Ministry of Education , Yinchuan , Ningxia , China.
c Departments of Biomedical Engineering and Pharmaceutics , Purdue University , West Lafayette , IN , USA , and.
d Department of Pharmaceutics , General Hospital of Ningxia Medical University , Yinchuan , Ningxia , China.


Lung-targeting sophoridine-loaded poly(lactide-co-glycolide) (PLGA) microspheres were constructed by a simple oil-in-oil emulsion-solvent evaporation method. The obtained microspheres were systematically studied on their morphology, size distribution, drug loading, encapsulation efficiency, in vitro release profile, and biodistribution in rats. The drug-loaded microparticles showed as tiny spheres under SEM and had an average size of 17 μm with 90% of the microspheres ranging from 12 to 24 μm. The drug loading and encapsulation efficiency were 65% and 6.5%, respectively. The in vitro drug release behavior of microspheres exhibited an initial burst of 16.6% at 4 h and a sustained-release period of 14 days. Drug concentration in lung tissue of rats was 220.10 μg/g for microspheres and 6.77 μg/g for solution after intraveneous injection for 30 min, respectively. And the microsphere formulation showed a significantly higher drug level in lung tissue than in other major organs and blood samples for 12 days. These results demonstrated that the obtained PLGA microspheres could potentially improve the treatment efficacy of sophoridine against lung cancer.


Sophoridine; biodistribution; lung targeting; microspheres; poly(lactide-co-glycolide) (PLGA)

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