Mixed micelles containing lipophilic gadolinium complexes as MRA contrast agents
Mixed micelles containing lipophilic gadolinium complexes as MRA contrast agents
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DOI：
10.1007/bf02668092
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发表时间：
2001-05-01
影响因子：
2.3
通讯作者：
Uggeri, F
中科院分区：
文献类型：
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作者：
Anelli, PL;Lattuada, L;Uggeri, F
混合胶束;用于MRA的是多组分系统，其包含磷脂、生物相容性非离子表面活性剂（例如Synperonic（R）F-108）和亲脂性钆。复杂.设计了多种亲脂性钆络合物，考虑到诸如以下的特征：（i）配体的性质（环状与非环状）;（ii）亲脂性部分;（iii）络合物的全局电荷;和（iv）将络合物连接至亲脂性部分的键的性质。配制成混合胶束后，所有亲脂性钆络合物在水中和血液（大鼠）中均显示出高弛豫率。混合胶束含有钆配合物轴承，只有一个脂肪族。链不能用作MRA造影剂，因为它们具有高溶血作用。此外，在大鼠中，它们很快从血液中消除。使用带有两个脂族链的钆络合物完全避免了这些缺点。混合胶束，含有这样的复合物显示高松弛性，没有溶血作用和长的血液持久性。这使得它们成为MRA造影剂的有希望的候选者。然而，仅通过肝脏发生的消除即使在7天后也不完全。在亲脂性部分和螯合物亚基之间含有不稳定（例如酯）键的复合物通过肝脏和肾脏消除。然而，7天后消除仍不完全。(C)2001 Elsevier Science B. V.保留所有权利。
Mixed micelles; for MRA are multicomponent systems containing a phospholipid, a biocompatible non-ionic surfactant (e.g. Synperonic (R) F-108), and a lipophilic gadolinium. complex. A variety of lipophilic gadolinium complexes were designed taking, into account features such as: (i) nature of ligand (cyclic versus acyclic); (ii) lipophilic moiety; (iii) global charge of the complex; and (iv), nature of bond connecting the complex to the lipophilic moiety. All the lipophilic gadolinium complexes after formulation as mixed micelles show high relaxivities in water and in blood (rat). Mixed micelles containing gadolinium complexes bearing only, one aliphatic. chain cannot be used as, MRA contrast agents because they have a high haemolytic effect. Furthermore, in rats they are quickly, eliminated from the blood stream. These drawbacks are completely circumvented using gadolinium complexes bearing two aliphatic chains. Mixed micelles, containing such complexes show high relaxivities, no haemolytic effect and long blood permanence. This, makes them promising candidates as, MRA contrast agents. However, elimination, which occurs exclusively through the liver, is not complete, even after 7 days. Complexes containing labile (e.g. ester) bonds between the lipophilic moieties and the chelate, subunit are eliminated through both the liver and the kidneys. However, elimination is still not complete after 7 days. (C) 2001 Elsevier Science B.V. All rights reserved.