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A novel tetrandrine-loaded chitosan microsphere: characterization and in vivo evaluation

Authors Guo K, Cang J

Received 25 December 2015

Accepted for publication 10 February 2016

Published 30 March 2016 Volume 2016:10 Pages 1291—1298

DOI https://doi.org/10.2147/DDDT.S103169

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Lucy Goodman

Peer reviewer comments 4

Editor who approved publication: Prof. Dr. Wei Duan


Kefang Guo, Jing Cang

Department of Anesthesia, Zhongshan Hospital, Fudan University, Shanghai, People’s Republic of China

Abstract: In this study, novel tetrandrine-loaded chitosan microspheres were prepared by the emulsion cross-linking method. The systems were then characterized for physicochemical properties and in vitro drug release. In addition, the pharmacokinetics and tissue distribution of microspheres were further verified in animal models. Particle-size distribution indicated that the size of microspheres was within the range of 7–15 µm, with a median diameter of 12.4 µm. The drug loading and entrapment efficiency of the formulation were 34.6%±12.5% and 87.3%±9.7% (mean ± SD), respectively. In vitro release showed a typical sustained and long-term drug release behavior. The Higuchi equation was the model that fit best with release data. Maintaining a relatively constant plasma concentration in the long-term drug treatment is an outstanding pharmacokinetic advantage of tetrandrine microspheres in vivo. Moreover, compared with tetrandrine solution, tetrandrine microspheres produced a lower drug concentration in the heart, liver, and kidneys. This indicated that the microspheres used in this study were preferable for targeting lung tissue versus other tissues. No damage to the tissues of the lung was found in histopathological examination.

Keywords: tetrandrine, chitosan microspheres, emulsion cross-linking, pharmacokinetics, tissue distribution

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