Biodistribution of dual radiolabeled lipidic nanocapsules in the rat using scintigraphy and γ counting
Biodistribution of dual radiolabeled lipidic nanocapsules in the rat using scintigraphy and γ counting
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DOI：
10.1016/s0378-5173(02)00218-1
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发表时间：
2002-08-21
影响因子：
5.8
通讯作者：
Benoît, JP
中科院分区：
文献类型：
--
作者：
Cahouet, A;Denizot, B;Benoît, JP
本工作的目的是研究放射性标记的脂质纳米胶囊制剂在大鼠静脉注射后的生物分布。该制剂有望用作抗癌剂递送装置和转染络合物。为此，将~(99m)Tc-oxine掺入到脂核中，而I-125标记的是纳米囊的张力壳。首先，通过对蒸馏水的透析法和尺寸测量来评价放射性标记纳米胶囊的体外稳定性。其次，静脉给药3h后，通过动态核素扫描技术跟踪纳米胶囊的生物分布，并通过测定血液和组织中的伽马活性来跟踪纳米胶囊的生物分布。放射性标记在体外是有效和稳定的。静脉注射后，两种放射性核素的血放射性均降低，早期半衰期约为45min。肝脏和肠道的放射性在24小时内升高，示踪剂在血液中的残留相对较长，这可能是由于纳米载体表面存在聚乙二醇酯，因此这些无溶剂的脂类纳米胶囊作为亲脂药物的载体似乎很有希望。(C)2002 Elsevier Science B.V.保留所有权利。
The aim of the present work was to study the biodistribution of a radiolabeled lipidic nanocapsule formulation after intravenous administration in rat by scintigraphy and gamma counting. This formulation is expected to be used as anticancer agent delivery devices and as transfection complexes. For this purpose, Tc-99m-oxine was incorporated in the lipidic core, while I-125 labeled tensioactive shell of the nanocapsule. First, in vitro stability of radiolabeled nanocapsules was evaluated by dialysis against distilled water and size measurements. Second, the nanocapsule biodistribution was followed after intravenous administration for 3 h by dynamic scintigraphic acquisition and up to 24 h by determining the gamma activity in blood and tissues. Radiolabeling was efficient and stable in vitro. After intravenous injection blood radioactivity decreased with an early half disappearance time of about 45 min for both radioisotopes. Liver and intestine radioactivities raised up to 24 h. The relatively long remanence in blood of the tracers which is probably due to the presence of PEG at the nanocarrier surface seems promising for the use of these solvent free lipidic nanocapsules as carrier of lipophilic drugs. (C) 2002 Elsevier Science B.V. All rights reserved.