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The influence of different long-circulating materials on the pharmacokinetics of liposomal vincristine sulfate

Authors Zhang J, Chen Y, Li X, Liang X, Luo X

Received 30 March 2016

Accepted for publication 18 June 2016

Published 26 August 2016 Volume 2016:11 Pages 4187—4197


Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 2

Editor who approved publication: Dr Linlin Sun

Jing Zhang,1,* Yingchong Chen,1,* Xiang Li,1,2 Xinli Liang,1 Xiaojian Luo2

1Key Laboratory of Modern Preparation of TCM, Ministry of Education, 2State Key Laboratory of Innovative Drug and Efficient Energy-Saving Pharmaceutical Equipment, Jiangxi University of Traditional Chinese Medicine, Nanchang, People’s Republic of China

*These authors contributed equally to this work

Purpose: This study was designed to improve the in vivo pharmacokinetics of long-circulating vincristine sulfate (VS)-loaded liposomes; three different long-circulating materials, chitosan, poly(ethylene glycol)-1,2-distearoyl sn-glycero-3-phosphatidylethanolamine (PEG-DSPE), and poly(ethylene glycol)-poly-lactide-co-glycolide (PEG-PLGA), were evaluated at the same coating molar ratio with the commercial product Marqibo® (vincristine sulfate liposome injection [VSLI]).
Materials and methods: VS-loaded liposomes were prepared by a pH gradient method and were then coated with chitosan, PEG-DSPE, or PEG-PLGA. Physicochemical properties, including the morphology, particle size, zeta potential, encapsulation efficiency (EE%), pH, drug loading, and in vitro release, were determined. Preservation stability and pharmacokinetic studies were performed to compare the membrane-coated liposomes with either commercially available liposomes or the VS solution.
Results: The sphere-like morphology of the vesicles was confirmed by transmission electron microscope. Increased particle size, especially for the chitosan formulation, was observed after the coating process. However, the EE% was ~99.0% with drug loading at 2.0 mg/mL, which did not change after the coating process. The coating of long-circulation materials, except for chitosan, resulted in negatively charged and stable vesicles at physiological pH. The near-zero zeta potential exhibited by the PEG-DSPE formulation leads to a longer circulation lifetime and improved absorption for VS, when compared with the PEG-PLGA formulation. Compared with the commercial product, PEG was responsible for a higher plasma VS concentration and a longer half-life.
Conclusion: PEG-DSPE coating may be related to better absorption, based on the stability and a pharmacokinetic improvement in the blood circulation time.

Keywords: vincristine sulfate, long-circulating materials, zeta potential, stability, pharmaco­kinetics

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