Threshold size for optimal passive pulmonary targeting and retention of rigid microparticles in rats.
Threshold size for optimal passive pulmonary targeting and retention of rigid microparticles in rats.
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DOI：
10.1016/j.jconrel.2009.12.019
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发表时间：
2010-04-02
影响因子：
10.8
通讯作者：
Sinko, Patrick J.
中科院分区：
文献类型：
--
作者：
Kutscher, Hilliard L.;Chao, Piyun;Deshmukh, Manjeet;Singh, Yashveer;Hu, Peidi;Joseph, Laurie B.;Reimer, David C.;Stein, Stanley;Laskin, Debra L.;Sinko, Patrick J.
本文系统地研究了不同粒径（2、3、6和10μm）的刚性聚苯乙烯荧光微粒（MP）静脉注射给SD大鼠后，MP粒径与肺靶向性、肺内分布和滞留时间的关系。评估总荧光，发现2μm和3μm MP容易通过肺到达肝脏和脾脏，而10μm MP在研究的一周持续时间内完全截留在肺中。在接下来的2天内，最初截留在肺中的约84%的6μm MP被清除，15%在剩余的5天内被清除。Caliper IVIS® 100小动物成像系统证实，3μm MP未保留在肺中，但6μm和10μm MP广泛分布在整个肺中。此外，组织学检查显示MP截留在毛细血管中，而不是小动脉中。这些研究表明，对于刚性MP，在IV注射后实现瞬时但高效靶向肺毛细血管所需的最佳尺寸范围在大鼠中为>6μm但<10μm，并且全身施用最佳尺寸的MP可能是目前使用的基于吸入的递送至肺的有效替代方案。
The relationship between microparticle (MP) size and lung targeting efficiency, intra-lung distribution and retention time was systematically studied after intravenous administration of rigid fluorescent polystyrene MPs of various sizes (2, 3, 6 and 10μm) to Sprague-Dawley rats. Total fluorescence was assessed and it was found that 2μm and 3μm MPs readily passed through the lung to the liver and spleen while 10μm MPs were completely entrapped in the lung for the one-week duration of the study. Approximately 84% of 6μm MPs that were initially entrapped in the lung were cleared over the next 2 days and 15% were cleared over the remaining 5 days. A Caliper IVIS® 100 small animal imaging system confirmed that 3μm MPs were not retained in the lung but that 6μm and 10μm MPs were widely distributed throughout the lung. Moreover, histologic examination showed MP entrapment in capillaries but not arterioles. These studies suggest that for rigid MPs the optimal size range required to achieve transient but highly efficiently targeting to pulmonary capillaries after IV injection is >6μm but <10μm in rats and that systemic administration of optimally sized MPs may be an efficient alternative to currently used inhalation-based delivery to the lung.
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DOI：
10.1002/jps.3030361002
发表时间：
1947-01-01
期刊：
JOURNAL OF THE AMERICAN PHARMACEUTICAL ASSOCIATION-SCIENTIFIC EDITION
影响因子：
--
作者：
BREWER, JH;DUNNING, JHF
通讯作者：
DUNNING, JHF
影响因子：
3.7
作者：
Hirst, PH;Pitcairn, GR;Newman, SP
通讯作者：
Newman, SP
影响因子：
2.3
作者：
Chao P;Deshmukh M;Kutscher HL;Gao D;Rajan SS;Hu P;Laskin DL;Stein S;Sinko PJ
通讯作者：
Sinko PJ
影响因子：
3.3
作者：
Huang, YQ;Doerschuk, CM;Kamm, RD
通讯作者：
Kamm, RD
影响因子：
24.3
作者：
Janssens, HM;Devadason, SG;Tiddens, HAWM
通讯作者：
Tiddens, HAWM