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Yuan, Q, Wang, Y, Song, R, Hou, X, Yu, K, Zheng, J, Zhang, J, Pu, X, Han, J and Zong, L (2019) Study on Formulation, in vivo Exposure, and Passive Targeting of Intravenous Itraconazole Nanosuspensions. Frontiers in Pharmacology, 10. 225 -225. ISSN 1663-9812
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Abstract
The pharmacokinetic profile of a drug can be different when delivered as a nanosuspension compared with a true solution, which may in turn affect the therapeutic effect of the drug. The goal of this study was to prepare itraconazole nanosuspensions (ITZ-Nanos) stabilized by an amphipathic polymer, polyethylene glycol-poly(Benzyl aspartic acid ester), by the precipitation-homogenisation, and study the pharmacokinetic curve of the ITZ-Nanos. The particle size and morphology of nanosuspensions were assayed by Zetasizer and field emission scanning electron microscope (SEM), severally. The dissolution profile was evaluated using a paddle method according to Chinese Pharmacopoeia 2015. The level of ITZ in blood and tissues was measured by a HPLC method. The optimized ITZ-Nanos had a mean particle size of 268.1±6.5 nm and the particles were in a rectangular form. The dissolution profile of ITZ-Nanos resemble that of commercial ITZ injections, with nearly 90% ITZ released in the first five minutes. The ITZ-Nanos showed distinct pharmacokinetic properties compared with the commercial ITZ injections, including a reduced beginning drug concentration, enhanced t1/2 and MRT, and increased concentration in the liver, lung and spleen. The ITZ-Nanos can change the in vivo distribution of ITZ and result in passive targeting to the organs with mononuclear phagocyte systems.
Item Type: | Article |
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Additional Information: | This is the final published version of the article (version of record). It first appeared online via Frontiers Media at https://www.frontiersin.org/article/10.3389/fphar.2019.00225 - please refer to any applicable terms of use of the publisher. |
Uncontrolled Keywords: | itraconazole nanosuspension, process optimization, in vivo pharmacokinetics, tissue distribution, passive targeting |
Subjects: | R Medicine > RS Pharmacy and materia medica |
Divisions: | Faculty of Medicine and Health Sciences > School of Pharmacy |
Depositing User: | Symplectic |
Date Deposited: | 16 Apr 2019 14:36 |
Last Modified: | 16 Apr 2019 15:09 |
URI: | https://eprints.keele.ac.uk/id/eprint/6193 |