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Background <p>The current study aims to develop a clinically applicable radiopharmaceutical agent for long-term imaging in the diagnosis and management of oncologic patients in the field of nuclear medicine. Liposomes, as pharmaceutical nanocarriers, have been extensively studied in pharmaceutical industry and depending on their structural characteristics could be formulated for accumulation in various pathological sites in the body. PEGylated liposomes have smaller volume of distribution and decreased clearance, consequently, due to their more prolonged presence in the bloodstream and their stability during this time, could be used for tumor imaging.</p> Study design and methods <p> In this work, liposomal formulations encapsulating albumin were synthesized by thin-film hydration technique, then extruded and after homogenization, their characteristics including size, zeta potential and encapsulation efficiency were measured. Then, these liposomes were labeled by <sup>111</sup>In-oxine and their stability in serum medium was assessed and the rate of their biodistribution in C26-colon carcinoma tumor-bearing mice was evaluated by two approaches, quantitatively radioactivity measurement and qualitatively gamma scintigraphy imaging.</p> Results <p>The result of our study displayed that <sup>111</sup>In -radiolabeled liposomes having a size of about 130 nanometers, were capable of accumulating in tumor sites based on enhanced penetration and retention (EPR) phenomenon. These liposomes also have high stability for maintaining encapsulated albumin for a long time up to 96&#xa0;h and even may be stable for longer time period. In the study of biodistribution of our formulation in tumor-bearing mice, they accumulated more in the kidney, liver, spleen and tumor sites, so that even after clearance of formulation in the bloodstream, they existed in significantly higher levels in the mentioned organs and likewise tumor sites up to 96&#xa0;h. In gamma scintigraphy, organs with high activity resulted from accumulation, were visible in the form of hot spots demonstrating formulation stability in the tumor sites from time of administration to 96&#xa0;h.</p> Conclusions <p>Our in vitro and in vivo studies demonstrated that this PEGylated radiolabeled liposomal formulation have considerable stability and efficiency for long-term tumor imaging which merit further studies for its transformation into clinical application.</p>

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Development of radiolabeled 111In-albumin liposomes for long-term imaging of tumors

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年5月18日

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  • Mohammad Ahrari,
  • Zahra Saberi,
  • Azam Abbasi,
  • Jafar Rahnama Yazdi,
  • Mahmoud Reza Jaafari,
  • Kayvan Sadri

摘要

Background

The current study aims to develop a clinically applicable radiopharmaceutical agent for long-term imaging in the diagnosis and management of oncologic patients in the field of nuclear medicine. Liposomes, as pharmaceutical nanocarriers, have been extensively studied in pharmaceutical industry and depending on their structural characteristics could be formulated for accumulation in various pathological sites in the body. PEGylated liposomes have smaller volume of distribution and decreased clearance, consequently, due to their more prolonged presence in the bloodstream and their stability during this time, could be used for tumor imaging.

Study design and methods

In this work, liposomal formulations encapsulating albumin were synthesized by thin-film hydration technique, then extruded and after homogenization, their characteristics including size, zeta potential and encapsulation efficiency were measured. Then, these liposomes were labeled by 111In-oxine and their stability in serum medium was assessed and the rate of their biodistribution in C26-colon carcinoma tumor-bearing mice was evaluated by two approaches, quantitatively radioactivity measurement and qualitatively gamma scintigraphy imaging.

Results

The result of our study displayed that 111In -radiolabeled liposomes having a size of about 130 nanometers, were capable of accumulating in tumor sites based on enhanced penetration and retention (EPR) phenomenon. These liposomes also have high stability for maintaining encapsulated albumin for a long time up to 96 h and even may be stable for longer time period. In the study of biodistribution of our formulation in tumor-bearing mice, they accumulated more in the kidney, liver, spleen and tumor sites, so that even after clearance of formulation in the bloodstream, they existed in significantly higher levels in the mentioned organs and likewise tumor sites up to 96 h. In gamma scintigraphy, organs with high activity resulted from accumulation, were visible in the form of hot spots demonstrating formulation stability in the tumor sites from time of administration to 96 h.

Conclusions

Our in vitro and in vivo studies demonstrated that this PEGylated radiolabeled liposomal formulation have considerable stability and efficiency for long-term tumor imaging which merit further studies for its transformation into clinical application.