标题:Novel PEG-grafted nanostructured lipid carrier for systematic delivery of a poorly soluble anti-leukemia agent Tamibarotene: characterization and evaluation
作者:Liu, Xin; Zhang, Zhihua; Jiang, Yuqi; Hu, Yue; Wang, Zhonglan; Liu, Junli; Feng, Ruihua; Zhang, Jie; Huang, Guihua
作者机构:[Liu, Xin; Zhang, Zhihua; Jiang, Yuqi; Hu, Yue; Wang, Zhonglan; Liu, Junli; Feng, Ruihua; Zhang, Jie; Huang, Guihua] Shandong Univ, Sch Pharmaceut Sci 更多
通讯作者:Huang, GH
通讯作者地址:[Huang, GH]Shandong Univ, Sch Pharmaceut Sci, 44 Wenhua Xi Rd, Jinan, Shandong, Peoples R China.
来源:DRUG DELIVERY
出版年:2015
卷:22
期:2
页码:223-229
DOI:10.3109/10717544.2014.885614
关键词:Biodistribution; intravenous delivery; nanostructured lipid carrier;; PEGylated; pharmacokinetic; Tamibarotene
摘要:Tamibarotene (Am80), a poorly water-soluble drug for the treatment of acute promyelocytic leukemia (APL), loaded nanostructured lipid carrier (Am80-NLC) was developed and characterized previously. The purpose of the present work was to develop PEGylated nanostructured lipid carrier (PEG-NLC) for intravenous delivery of Am80, with the aim to further extend the circulation in blood and decrease the adverse events. Am80-loaded PEG-NLC (Am80-PEG-NLC) modified with PEG-40 stearate (PEG40-SA, molecular weight 2000 Da) was formulated by the method of melt-emulsification and low temperature-solidification technique. Am80-NLC was developed as well as control. Based on the optimized results of single-factor screening experiment, the average drug entrapment efficiency, the mean particle size, and zeta potential of Am80-NLC and Am80-PEG-NLC were found to be 89.8-94.3%, 178.9-201.6 nm, and -37.74 to -20.1 mV, respectively. In vitro drug release of Am80-NLC and Am80-PEG-NLC possessed a sustained release characteristic and their release behavior was in accordance with the Ritger-Peppas equation. In vivo, after intravenous (i.v.) injection to rats, the mean residence time (MRT) of Am80-PEG-NLC group was significantly prolonged and the AUC value was improved as well compared with the Am80-NLC group. Furthermore, the biodistribution in mice showed that Am80-PEG-NLC preferentially decreased the accumulation of Am80 in kidney and increased the drug concentration in brain after i.v. injection. In conclusion, Am80-PEG-NLC may be a potential delivery system for Am80 in the treatment of APL.
收录类别:SCOPUS;SCIE
WOS核心被引频次:11
Scopus被引频次:13
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84921630467&doi=10.3109%2f10717544.2014.885614&partnerID=40&md5=cfe7fe5491765b7f265421df07ce6c31
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