Pharmacokinetics and biodistribution of polymeric micelles of paclitaxel with Pluronic P123

来源 :Acta Pharmacologica Sinica | 被引量 : 0次 | 上传用户:yue_pan
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
Aim:To investigate the preparation,in vitro release,in vivo pharmacokineticsand tissue distribution of a novel polymeric micellar formulation of paclitaxel(PTX)with Pluronic P123.Methods:The polymeric micelles of paclitaxel with PluronicP123 were prepared by a solid dispersion method.The characteristics of micellesincluding particle size distribution,morphology and in vitro release of PTX frommicelles were carried out.FFX-loaded micellar solutions were administered throughthe tail vein to healthy Sprague-Dawley rats and Kunming strain mice to assessthe pharmacokinetics and tissue distribution of PTX,respectively.Taxol,thecommercially available intravenous formulation of PTX,was also administered ascontrol.Results:By using a dynamic light scattering sizer and a transmissionelectron microscopy,it was shown that the PTX-loaded micelles had a mean sizeof approximately 25 nm with narrow size distribution and a spherical shape.PTXwas continuously released from Pluronic P 123 micelles in release medium contain-ing 1 mol/L sodium salicylate for 24 h at 37℃.In the pharmacokinetic assessment,t_(1/2β)and AUC of micelle formulation were 2.3 and 2.9-fold higher than that of Taxolinjection.And the PTX-loaded micelles increased the uptake of PTX in the plasma,ovary and uterus,lung,and kidney,but decreased uptake in the liver and brain inthe biodistribution study.Conclusion:Polymeric micelles using Pluronic P123can effectively solubilize PTX,prolong blood circulation time and modify thebiodistribution of PTX. Aim: To investigate the preparation, in vitro release, in vivo pharmacokinetics and tissue distribution of a novel polymeric micellar formulation of paclitaxel (PTX) with Pluronic P123. Methods: The polymeric micelles of paclitaxel with Pluronic P123 were prepared by a solid dispersion method. of micellesincluding particle size distribution, morphology and in vitro release of PTX frommicelles were carried out. FFX-loaded micellar solutions were administered through the tail vein to healthy Sprague-Dawley rats and Kunming strain mice to assessthe pharmacokinetics and tissue distribution of PTX, respectively. Taxol , the commercially available available formulation of PTX, was also administered as control. Results: By using a dynamic light scattering sizer and a transmission electron microscopy, it was shown that the PTX-loaded micelles had a mean size of approximately 25 nm with narrow size distribution and a spherical shape.PTX was continuously released from Pluronic P 123 micelles in rele ase medium contain 1 mol / L sodium salicylate for 24 h at 37 ° C. In the pharmacokinetic assessment, t 1/2 (1/2 β) and AUC of micelle formulation were 2.3 and 2.9-fold higher than that of Taxolinjection. And the PTX- loaded micelles increased the uptake of PTX in the plasma, ovary and uterus, lung, and kidney, but decreased uptake in the liver and brain inthe biodistribution study. Conlusion: Polymeric micelles using Pluronic P123can effectively solubilize PTX, prolong blood circulation time and modify thebiodistribution of PTX.
其他文献
叶片变形是轴流式汽轮鼓风机振动的主要原因之一.本文详细叙述了叶片变形引起振动的原因和消除振动的基本方法. The deformation of the blade is one of the main reasons
本专利属于地质勘探中小口径深井钻进范围。铁砧9位于壳体的上部1,铁砧里面设有推杆10。碎岩工具的转动机构是带有回动弹簧15的轴11。它用带有滚动体的螺旋接头13与壳体下部
安静,美丽的梵净山下,忽然热闹了起来。震耳欲聋的马达轰鸣声和五颜六色的赛车为风景秀丽的梵净山增添了几分生气。 Quiet, beautiful Fanjingshan, suddenly bustled up. T
利用极化效应指数,建立了计算直链烷基衍生物同系物的标准汽化热的方法。110个可比较值的平均相对偏差为1.24% Using the polarization effect index, a method for calculating the
美学课上,教授把两张《蓝天》的照片张挂在黑板上,其中的一张,整张照片拍的都是蓝天,而另一张,蓝天之中点缀着几朵白云。教授问学生,这两张照片里的蓝天哪个更美呢?学生们一致认为那片点缀着几朵白云的蓝天更美。  “按说,几朵白云遮盖了蓝天的美丽,占据了蓝天的美丽,蓝天的美丽应该减少才是,可为什么反而会变得更加美丽呢?”教授问。  “因为白云衬托了蓝天的美丽,从而让蓝天变得更加美丽。”学生们说。  “那么
基于离散体的有限元法对粉末颗粒压制过程进行了细观数值模拟,考察了典型位置颗粒的应变过程、不同位置颗粒的变形差异以及颗粒在不同压制力下的应变情况。分析表明,压制过程
北京朝阳区东坝社区,有一个设施齐全的120平米家庭乐园,免费对孩子们开放。乐园的主人不是富豪,只是一位年轻的小继母。她创办乐园的初衷,是为了让8岁的继子告别儿童抑郁症。
磁电式记录仪中的一个十分重要部分是记录笔,它的质量直接影响到记录仪的水平,记录仪厂家大都把自己的主要力量投入到记录笔的研制中。记录笔是由三部分组成的:直线机构、电
我国自1962年生产出第一台1.6米口径的轴流泵64zLB-50以来,大型轴流泵的生产和泵站建设有了很大的发展.目前,最大的轴流泵口径已达4.5米,最大的混流泵口径为6米.据调查,截至
展望2013年,公路货运将继续平稳增长,并出现加速整合的趋势。而在整合的过程中,企业将面临着新的选择。公路货运相对于铁路运输、水路运输和航空运输来说,是一个完全市场化的