羟基铝四-3-苯硫酞脂质体光敏剂在小鼠体内的药动学研究

A. Budko, Z. G. Deichman, G. Meerovich, L. Borisova, I. G. Мeerovich, A. Lantsova, Kulbachevskaya N.Yu. Kulbachevskaya N.Yu. Kulbachevskaya N.Yu.
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引用次数: 2

摘要

本文研究了基于羟基铝四‑3‑苯噻吩酞菁的红外光敏剂(PS)在空间稳定脂质体中的药代动力学。这项研究是在成年雌鼠身上进行的。PS以6mg / kg的剂量静脉注射一次。采用光谱荧光法每隔5分钟至7天对PS在小鼠组织和器官中的蓄积动态进行评估。PS光活性形式的最大蓄积量记录在肺部(在引入后5-30分钟内32µg / g),肝脏(在引入后4 - 24小时内20.8µg / g)和脾脏(在引入后4小时内28µg / g)。同时,在观察期结束时(给药后7天),肝脏和脾脏中仍检测到微量PS光活性形式,计算浓度为0.5 - 1µg / g,肌肉和皮肤中PS积累最少。PS在皮肤中积累的荧光信号几乎可以立即检测到,其浓度在长达3天的观察中保持在相同水平(1.2 - 1.5µg / g)。给药15分钟后,肌肉中PS浓度达到1.5µg / g, 24小时后逐渐降低至0.25µg / g。获得了PS在动物血液、基本器官和组织中的药动学数据,计算了药动学参数。给药后7 d,皮肤和肌肉中PS浓度均低于检测限。研究证实,聚乙二醇化的PS脂质体形式减缓了其被网状内皮系统捕获的过程。结果表明,PS在小鼠血液和脏器中循环时间较长,给药4小时后才完全分布。
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Study of pharmacokinetics of liposomal photosensitiser based on hydroxyaluminium tetra-3-phenylthiophthalocyanine on mice
The present work is devoted to the study of pharmacokinetics of infrared photosensitizer (PS) based on hydroxyaluminium tetra‑3‑phenylthiophthalocyanine in a sterically stabilized liposomal form. The study was carried out on adult female mice. The PS was administered once intravenously at a dose of 6 mg / kg. Evaluation of the PS accumulation dynamics in the mice tissues and organs was performed at time intervals from 5 minutes to 7 days using spectral‑fluorescent method. The maximum accumulation of the PS photoactive form was recorded in lungs (32 µg / g in the interval of 5–30 minutes after introduction), liver (20.8 µg / g in the interval of 4–24 hours after introduction) and spleen (28 µg / g 4 hours after introduction). At the same time, by the end of the observation period (7 days after administration), trace amounts of the PS photoactive form were still detected in the liver and the spleen at a calculated concentration of 0.5‑1 µg / g. The PS accumulated the least in muscles and skin. The fluorescent signal from the PS accumulated in skin was detectable almost immediately, and its concentration remained at the same level (1.2‑1.5 µg / g) for up to 3 days of observation. In the muscles, the concentration of the PS reached 1.5 µg / g 15 minutes after administration, and then gradually decreased until 0.25 µg / g at 24 hours. Data on the pharmacokinetics of PS in blood, basic organs and tissues of animals were obtained, pharmacokinetic parameters were calculated. 7 days after the administration, the PS concentration in the skin and muscles was below the detection limit. The studies confrmed that PEGylation of the PS liposomal form slows down the process of its capture by reticulo‑endothelial system. It was shown that the PS circulates in blood and organs of mice for a long time and it completely distributes only when 4 hours pass after administration.
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来源期刊
Biomedical Photonics
Biomedical Photonics Medicine-Surgery
CiteScore
1.80
自引率
0.00%
发文量
19
审稿时长
8 weeks
期刊介绍: The main goal of the journal – to promote the development of Russian biomedical photonics and implementation of its advances into medical practice. The primary objectives: - Presentation of up-to-date results of scientific and in research and scientific and practical (clinical and experimental) activity in the field of biomedical photonics. - Development of united Russian media for integration of knowledge and experience of scientists and practitioners in this field. - Distribution of best practices in laser medicine to regions. - Keeping the clinicians informed about new methods and devices for laser medicine - Approval of investigations of Ph.D candidates and applicants.
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