The radiolabeling of the liposome surface can be a useful tool for in vivo tracking of therapeutic drug loaded liposomes. We investigated radiolabeling therapeutic drug (i.e. an antibiotic, amikacin) loaded liposomes with (99m)Tc, nebulization properties of (99m)Tc-labeled liposomal amikacin for inhalation ((99m)Tc-LAI), and its stability by size exclusion low-pressure liquid chromatography (LPLC). LAI was reacted with (99m)Tc using SnCl2 dissolved in ascorbic acid as a reducing agent for 10 min at room temperature. The labeled products were then purified by anion exchange resin. The purified (99m)Tc-LAI in 1.5% NaCl solution was incubated at 4 °C to assess its stability by LPLC. The purified (99m)Tc-LAI was subjected to studies with a clinically used nebulizer (PARI eFlow®) and the Anderson Cascade Impactor (ACI). The use of ascorbic acid at 0.91 mM resulted in a quantitative labeling efficiency. The LPLC profile showed that the liposomal peak of LAI detected by a UV monitor at both 200 nm and 254 nm overlapped with the radioactivity peak of (99m)Tc-LAI, indicating that (99m)Tc-LAI is suitable for tracing LAI. The ACI study demonstrated that the aerosol droplet size distribution determined gravimetrically was similar to that determined by radioactivity. The liposome surface labeling method using SnCl₂ in 0.91 mM ascorbic acid produced (99m)Tc-LAI with a high labeling efficiency and stability that are adequate to evaluate the deposition and clearance of inhaled LAI in the lung by gamma scintigraphy.

译文

:脂质体表面的放射性标记可能是体内追踪治疗性载药脂质体的有用工具。我们研究了带有(99m)Tc的放射性标记治疗药物(即抗生素,丁胺卡那霉素)负载的脂质体,(99m)Tc标记的脂质体丁胺卡那霉素吸入剂((99m)Tc-LAI)的雾化特性,以及通过尺寸排阻法的稳定性高压液相色谱(LPLC)。在室温下,使用溶解在抗坏血酸中的SnCl2作为还原剂,使LAI与(99m)Tc反应10分钟。然后通过阴离子交换树脂纯化标记的产物。将纯化的(99m)Tc-LAI溶于1.5%NaCl溶液,于4°C孵育,以通过LPLC评估其稳定性。纯化的(99m)Tc-LAI用临床使用的雾化器(PARIeFlow®)和Anderson级联撞击器(ACI)进行了研究。 0.91 mM的抗坏血酸的使用导致定量标记效率。 LPLC图谱表明,由UV监测仪在200 nm和254 nm处检测到的LAI脂质体峰与(99m)Tc-LAI的放射性峰重叠,表明(99m)Tc-LAI适合于追踪LAI。 ACI研究表明,通过重量分析确定的气溶胶液滴尺寸分布与通过放射性确定的液滴尺寸分布相似。使用SnCl 2在0.91 mM抗坏血酸中制备的脂质体表面标记法(99m)Tc-LAI具有很高的标记效率和稳定性,足以评估γ闪烁显像法在肺中吸入的LAI的沉积和清除。

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