RESUMEN
Nuclear medicine specialty involves the administration of unsealed radioactive substances to patients to allow specific diagnostics and treatments using radiopharmaceuticals, radiotracers, and materials. Developing a radiopharmaceutical must involve considering and addressing some limitations such as its retention by unintended organs, which can influence patient and worker safety, imaging findings, and diagnostic and therapeutic accuracy. This paper presents data on the changing biodistribution, localization, stability, and accuracy patterns of radiopharmaceuticals by liposome encapsulation. METHODS: Data are presented for 5 male New Zealand white rabbits. They were injected intravenously with the 99mTc-liposomes encapsulated MIBI through a marginal ear vein, and whole-body images were acquired using a dual-head gamma camera. Cationic PEGylated liposomes were prepared using the conventional thin-film-hydration method. The liposomes were tested for particle size, zeta potential, high-performance-liquid-chromatography (HPLC), and toxicity. RESULTS: The liver activity was slightly greater than or equivalent to heart uptake, using 99mTcsestamibi, MIBI, without liposome as a reference. The absorbed doses in myocardium cells after injecting rabbits with 99mTc-MIBI labeled with free positive lower pH liposomes was greater than in the liver, whereas 99mTc labeled with encapsulated MIBI within positive liposomes showed a significantly higher heart-to-liver ratio. The heart-to-spleen activity uptake ratio in 99mTc-MIBI was higher than or equal to one but increased in 99mTc labeled with MIBI and free positive liposomes. Injecting rabbits with 99mTc labeled with encapsulated MIBI raised myocardium uptake to 2-4 times more than the spleen. Heart-to-bowel activity began to rise with 99m Tc-labeld-MIBI and liposomes. CONCLUSION: This study provides findings in radiopharmaceutical biodistribution using liposomal agents. Adding free liposomes using a pH gradient technique enhanced the uptake and localization of the radiotracer. However, tracer encapsulation during the formation of the liposomes showed even better specificity.
Asunto(s)
Liposomas , Radiofármacos , Masculino , Animales , Conejos , Distribución Tisular , Tecnecio Tc 99m Sestamibi , TecnecioRESUMEN
Challenges posed by the retention of radiopharmaceuticals in unintended organs affect the quality of patient procedures when undergoing diagnostics and therapeutics. The aim of this study was to formulate a suitable tracer encapsulated in liposomes using different techniques and compounds to enhance the stability, uptake, clearance, and cytotoxic effect of the radiopharmaceutical. Cationic liposomes were prepared by a thin-film method using dipalmitoyl phosphatidylcholine (DPPC) and cholesterol. Whole-body gamma camera images were acquired of intravenously injected New Zealand rabbits. Additionally, liposomes were assessed using stability, toxicity, zeta potential, and particle size tests. In the control cases, Technetium-99m (99mTc)-sestamibi exhibited the lowest heart uptake the blood pool and delayed images compared to both 99mTc-liposomal agents. Liver and spleen uptake in the control samples with 99mTc-sestamibi increased in 1-h-delayed images, unlike with 99mTc-liposomal agents, which were decreased in delayed images. The mean maximum count in the bladder for 99mTc-sestamibi loaded liposomes 1 h post-injection was 2354.6 (±2.6%) compared to 178.4 (±0.54%) for 99mTc-sestamibi without liposomes. Liposomal encapsulation reduced the cytotoxic effect of the sestamibi. 99mTc-MIBI-cationic liposomes exhibited excellent early uptake and clearance compared to 99mTc-MIBI without liposomes. Adding cholesterol during liposome formation enhanced the stability and specificity of the targeted organs.