Lamichhane Narottam, Dewkar Gajanan K, Sundaresan Gobalakrishnan, Mahon Rebecca N, Zweit Jamal
Center for Molecular Imaging, Department of Radiology, Virginia Commonwealth University, 1101 E. Marshall Street, Richmond, VA 23298-0031, USA.
Int J Mol Sci. 2017 May 18;18(5):1079. doi: 10.3390/ijms18051079.
Radiolabeled liposomes have been employed as diagnostic tools to monitor in vivo distribution of liposomes in real-time, which helps in optimizing the therapeutic efficacy of the liposomal drug delivery. This work utilizes the platform of [In]-Liposome as a drug delivery vehicle, encapsulating a novel F-labeled carboplatin drug derivative ([F]-FCP) as a dual-molecular imaging tool as both a radiolabeled drug and radiolabeled carrier. The approach has the potential for clinical translation in individual patients using a dual modal approach of clinically-relevant radionuclides of F positron emission tomography (PET) and In single photon emission computed tomography (SPECT). [In]-Liposome was synthesized and evaluated in vivo by biodistribution and SPECT imaging. The [F]-FCP encapsulated [In]-Liposome nano-construct was investigated, in vivo, using an optimized dual-tracer PET and SPECT imaging in a nude mouse. The biodistribution data and SPECT imaging showed spleen and liver uptake of [In]-Liposome and the subsequent clearance of activity with time. Dual-modality imaging of [F]-FCP encapsulated [In]-Liposome showed significant uptake in liver and spleen in both PET and SPECT images. Qualitative analysis of SPECT images and quantitative analysis of PET images showed the same pattern of activity during the imaging period and demonstrated the feasibility of dual-tracer imaging of a single dual-labeled nano-construct.
放射性标记脂质体已被用作诊断工具，以实时监测脂质体在体内的分布，这有助于优化脂质体药物递送的治疗效果。这项工作利用[铟]-脂质体平台作为药物递送载体，封装了一种新型氟标记的卡铂药物衍生物（[氟]-FCP）作为双分子成像工具，兼具放射性标记药物和放射性标记载体的功能。该方法有可能通过使用临床相关的氟正电子发射断层扫描（PET）和铟单光子发射计算机断层扫描（SPECT）的双模态方法，在个体患者中实现临床转化。[铟]-脂质体通过生物分布和SPECT成像在体内进行了合成和评估。使用优化的双示踪剂PET和SPECT成像，在裸鼠体内研究了封装有[氟]-FCP的[铟]-脂质体纳米构建体。生物分布数据和SPECT成像显示[铟]-脂质体在脾脏和肝脏摄取，随后活性随时间清除。封装有[氟]-FCP的[铟]-脂质体的双模态成像在PET和SPECT图像中均显示肝脏和脾脏有明显摄取。SPECT图像的定性分析和PET图像的定量分析显示成像期间活性模式相同，并证明了单一双标记纳米构建体双示踪剂成像的可行性。
