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Fospeg®(一种聚乙二醇化脂质体mTHPC制剂)在小鼠模型中全身给药后的药代动力学和生物分布研究。

Pharmacokinetic and biodistribution study following systemic administration of Fospeg®--a Pegylated liposomal mTHPC formulation in a murine model.

作者信息

Xie Haiyan, Svenmarker Pontus, Axelsson Johan, Gräfe Susanna, Kyriazi Maria, Bendsoe Niels, Andersson-Engels Stefan, Svanberg Katarina

机构信息

Department of Physics, Lund University, P.O. Box 118, 22100, Lund, Sweden.

出版信息

J Biophotonics. 2015 Jan;8(1-2):142-52. doi: 10.1002/jbio.201300133. Epub 2013 Dec 23.

Abstract

Fospeg® is a newly developed photosensitizer formulation based on meso-tetra(hydroxyphenyl)chlorin (mTHPC), with hydrophilic liposomes to carry the hydrophobic photosensitizer to the target tissue. In this study the pharmacokinetics and biodistribution of Fospeg® were investigated by high performance liquid chromatography at various times (0.5-18 hours) following systemic i.v. administration. As a model an experimental HT29 colon tumor in NMRI nu/nu mice was employed. Our study indicates a higher plasma peak concentration, a longer circulation time and a better tumor-to-skin ratio than those of Foslip®, another liposomal mTHPC formulation. Data from ex vivo tissue fluorescence and reflectance imaging exhibit good correlation with chemical extraction. Our results have shown that optical imaging provides the potential for fluorophore quantification in biological tissues.

摘要

Fospeg®是一种新开发的基于中-四(羟苯基)氯卟啉(mTHPC)的光敏剂制剂,其具有亲水性脂质体,可将疏水性光敏剂转运至靶组织。在本研究中,通过高效液相色谱法在全身静脉注射给药后的不同时间点(0.5 - 18小时)研究了Fospeg®的药代动力学和生物分布。以NMRI裸鼠中的实验性HT29结肠肿瘤作为模型。我们的研究表明,与另一种脂质体mTHPC制剂Foslip®相比,Fospeg®具有更高的血浆峰浓度、更长的循环时间和更好的肿瘤与皮肤比值。来自离体组织荧光和反射成像的数据与化学提取显示出良好的相关性。我们的结果表明,光学成像为生物组织中的荧光团定量提供了潜力。

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