在大鼠的药代动力学和生物分布中，（111）In-VNB-脂质体的放射性与化疗药物的相关性。
Correlation between radioactivity and chemotherapeutics of the (111)In-VNB-liposome in pharmacokinetics and biodistribution in rats.
机构信息
Institute of Traditional Medicine, School of Medicine, National Yang- Ming University, Taipei.
出版信息
Int J Nanomedicine. 2012;7:683-92. doi: 10.2147/IJN.S28279. Epub 2012 Feb 9.
BACKGROUND
The combination of a radioisotope with a chemotherapeutic agent in a liposomal carrier (ie, Indium-111-labeled polyethylene glycol pegylated liposomal vinorelbine, [(111)In-VNB-liposome]) has been reported to show better therapeutic efficiency in tumor growth suppression. Nevertheless, the challenge remains as to whether this therapeutic effect is attributable to the combination of a radioisotope with chemotherapeutics. The goal of this study was to investigate the pharmacokinetics, biodistribution, and correlation of Indium-111 radioactivity and vinorelbine concentration in the (111)In-VNB-liposome.
METHODS
The VNB-liposome and (111)In-VNB-liposome were administered to rats. Blood, liver, and spleen tissue were collected to determine the distribution profile of the (111)In-VNB-liposome. A liquid chromatography tandem mass spectrometry system and gamma counter were used to analyze the concentration of vinorelbine and radioactivity of Indium-111.
RESULTS
High uptake of the (111)In-VNB-liposome in the liver and spleen demonstrated the properties of a nanosized drug delivery system. Linear regression showed a good correlation (r = 0.97) between Indium-111 radioactivity and vinorelbine concentration in the plasma of rats administered the (111)In-VNB-liposome.
CONCLUSION
A significant positive correlation between the pharmacokinetics and biodistribution of (111)Indium radioactivity and vinorelbine in blood, spleen, and liver was found following administration of the (111)In-VNB-liposome. The liposome efficiently encapsulated both vinorelbine and Indium-111, and showed a similar concentration-radioactivity time profile, indicating the correlation between chemotherapy and radiotherapy could be identical in the liposomal formulation.
背景
将放射性同位素与化学治疗药物结合在脂质体载体中（即，铟-111 标记的聚乙二醇化脂质体长春瑞滨，[(111)In-VNB-脂质体]），已被报道在肿瘤生长抑制方面显示出更好的治疗效果。然而，挑战仍然在于这种治疗效果是否归因于放射性同位素与化学治疗药物的结合。本研究的目的是研究[(111)In-VNB-脂质体]中铟-111 放射性和长春瑞滨浓度的药代动力学、生物分布和相关性。
方法
将 VNB 脂质体和[(111)In-VNB-脂质体]给予大鼠。采集血液、肝脏和脾脏组织，以确定[(111)In-VNB-脂质体]的分布情况。使用液相色谱串联质谱系统和伽马计数器分析长春瑞滨的浓度和铟-111 的放射性。
结果
[(111)In-VNB-脂质体]在肝脏和脾脏中的高摄取表明其具有纳米药物递送系统的特性。线性回归显示，给予[(111)In-VNB-脂质体]的大鼠血浆中铟-111 放射性和长春瑞滨浓度之间存在良好的相关性（r=0.97）。
结论
给予[(111)In-VNB-脂质体]后，发现血液、脾脏和肝脏中铟-111 放射性和长春瑞滨的药代动力学和生物分布之间存在显著的正相关。该脂质体有效地包封了长春瑞滨和铟-111，并表现出相似的浓度-放射性时间曲线，表明在脂质体制剂中化疗和放疗之间的相关性可能是相同的。
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