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通过动脉注射脂质造影剂实现抗癌药物在实体瘤中的选择性靶向及同步图像增强。

Selective targeting of anti-cancer drug and simultaneous image enhancement in solid tumors by arterially administered lipid contrast medium.

作者信息

Konno T, Maeda H, Iwai K, Maki S, Tashiro S, Uchida M, Miyauchi Y

出版信息

Cancer. 1984 Dec 1;54(11):2367-74. doi: 10.1002/1097-0142(19841201)54:11<2367::aid-cncr2820541111>3.0.co;2-f.

Abstract

Twenty-four patients with various solid tumors including metastatic liver cancer and cancer of the lung, gallbladder, and pancreas were treated with a lipophilic macromolecular drug, copoly(styrene-maleic acid) conjugated neocarzinostatin (SMANCS). The drug was dissolved in a lipid contrast medium Lipiodol and administered by catheterizing the respective feeding arteries under x-ray monitoring. The advantages of this therapy include: (1) selective deposition of Lipiodol with the anti-cancer drug in the target tumor, (2) a pronounced and long-lasting anti-cancer effect, (3) enhanced visualization of the tumor on x-ray examinations for a prolonged period which also facilitated the long-term follow-up, (4) semiquantitative evaluation of the dosage regimen by x-ray examination before further administration, (5) general applicability due to procedural simplicity, and (6) little side effect. Since the amount of Lipiodol and SMANCS used per administration for a patient (1.0-5.0 ml; 1.0-5.0 mg) was far less than the anticipated toxicity (LD50 of Lipiodol = 95 ml/60 kg, dog, intravenously; and that of SMANCS = 3.4 mg/kg, mouse, IV), no deleterious effects to such critical organs as the brain, heart, lung, liver, or kidneys were observed upon radiologic and general clinical examination.

摘要

24例患有包括转移性肝癌以及肺癌、胆囊癌和胰腺癌等各种实体瘤的患者接受了亲脂性大分子药物——聚苯乙烯-马来酸共聚物结合新制癌菌素(SMANCS)的治疗。该药物溶解于脂质造影剂碘油中,并在X线监测下通过导管插入相应的供血动脉给药。这种治疗方法的优点包括:(1)碘油与抗癌药物在靶肿瘤中选择性沉积;(2)具有显著且持久的抗癌效果;(3)在X线检查中肿瘤的显影增强且持续时间延长,这也便于长期随访;(4)在进一步给药前通过X线检查对给药方案进行半定量评估;(5)由于操作简单而具有普遍适用性;(6)副作用小。由于每位患者每次给药时使用的碘油和SMANCS的量(1.0 - 5.0 ml;1.0 - 5.0 mg)远低于预期毒性(碘油的半数致死量=95 ml/60 kg,犬,静脉注射;SMANCS的半数致死量=3.4 mg/kg,小鼠,静脉注射),在放射学和一般临床检查中未观察到对脑、心、肺、肝或肾等重要器官的有害影响。

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