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首页> 美国卫生研究院文献>British Journal of Cancer >Pharmacokinetic and imaging studies in patients receiving a formulation of liposome-associated adriamycin.
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Pharmacokinetic and imaging studies in patients receiving a formulation of liposome-associated adriamycin.

机译：接受脂质体相关阿霉素制剂的患者的药代动力学和影像学研究。

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Pharmacokinetic and imaging studies in 19 patients receiving liposome-entrapped adriamycin (L-ADM) were carried out within the framework of a Phase I clinical trial (Gabizon et al., 1989a). The formulation of L-ADM tested consisted of 0.2 microM-extruded multilamellar vesicles composed of egg phosphatidylcholine, egg-derived phosphatidyl-glycerol (PG), cholesterol, and ADM intercalated in the fluid lipid bilayer. Plasma clearance of total drug extracted from the plasma after L-ADM infusion followed a biexponential curve with a pattern similar to that reported for free ADM. The plasma concentration of drug circulating in liposome-associated from was also measured in a subgroup of seven patients. Liposome-associated drug was found to be rapidly cleared from plasma. Its ratio to non-liposome-associated drug appeared to correlate with liver reserve, with highest ratios in patients with normal liver function. Liposome clearance, as measured by the plasma concentration of PG in three patients was slower than the clearance of liposome-associated ADM, suggesting that liposomes lose part of their drug payload during circulation. To learn about the liposome organ distribution, imaging studies were carried out with 111Indium-deferoxamine labelled liposomes of the same composition. Liposomes were cleared predominantly by liver and spleen and to a lesser extent by bone marrow in seven out of nine patients. In two patients with active hepatitis and severe liver dysfunction, there was minimal liver uptake and increased spleen and bone marrow uptake. Except for one hepatoma patient, intrahepatic and extrahepatic tumours were not imaged by liposomes, suggesting that liposome uptake is restricted to cells of the reticulo-endothelial system (RES).(ABSTRACT TRUNCATED AT 250 WORDS)
机译：在I期临床试验的框架内，对19名接受脂质体包裹的阿霉素（L-ADM）的患者进行了药代动力学和成像研究（Gabizon等，1989a）。所测试的L-ADM配方由0.2 microM挤出的多层囊泡组成，该囊泡由卵磷脂双层，蛋衍生的磷脂酰甘油（PG），胆固醇和ADM组成。 L-ADM输注后从血浆中提取的总药物的血浆清除率遵循一条双指数曲线，其模式与报告的游离ADM相似。在七个患者的一个亚组中，也测量了与脂质体相关的血浆中循环药物的血浆浓度。发现与脂质体相关的药物可从血浆中迅速清除。与非脂质体相关药物的比例似乎与肝脏储备相关，在肝功能正常的患者中比例最高。用三名患者的血浆PG浓度测量的脂质体清除速度比脂质体相关ADM清除速度慢，这表明脂质体在循环过程中损失了部分药物有效载荷。为了了解脂质体的器官分布，使用具有相同组成的111 In-去铁胺标记的脂质体进行了成像研究。在9名患者中，有7名患者主要通过肝脏和脾脏清除了脂质体，在较小程度上通过了骨髓清除了脂质体。在两名患有活动性肝炎和严重肝功能不全的患者中，肝脏摄取最少，脾脏和骨髓摄取增加。除一名肝癌患者外，脂质体未使肝内和肝外肿瘤成像，这表明脂质体的摄取仅限于网状内皮系统（RES）的细胞。（摘要摘录于250字）

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