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首页> 外文期刊>Chemotherapy Research and Practice >Cisplatin Tumor Biodistribution and Efficacy after Intratumoral Injection of a Biodegradable Extended Release Implant
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Cisplatin Tumor Biodistribution and Efficacy after Intratumoral Injection of a Biodegradable Extended Release Implant

机译：瘤内注射可生物降解的缓释植入物后顺铂肿瘤的生物分布和功效。

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Local delivery of chemotherapeutic drugs has long been recognized as a potential method for reaching high drug doses at the target site while minimizing systemic exposure. Cisplatin is one of the most effective chemotherapeutic agents for the treatment of various tumors; however, its systemic toxicity remains the primary dose-limiting factor. Here we report that incorporation of cisplatin into a fatty acid-based polymer carrier followed by a local injection into the solid tumor resulted in a successful tumor growth inhibition in heterotopic mouse bladder tumor model in mice. Platinum concentration in the tumor tissue surrounding the injected implant remained above the therapeutic level up to 14 days after the injection, while the plasma levels were several orders of magnitude lower comparing to systemic delivery. The reported delivery system increased the maximum tolerated dose of cisplatin 5 times compared to systemic delivery, thus potentially improving antitumor efficacy of cisplatin in solid tumor model.
机译：长期以来，化学疗法药物的局部递送一直被认为是在靶部位达到高药物剂量同时最大程度地减少全身暴露的一种潜在方法。顺铂是治疗各种肿瘤的最有效的化学治疗剂之一。然而，其全身毒性仍然是主要的剂量限制因素。在这里我们报道顺铂加入到基于脂肪酸的聚合物载体中，然后局部注射到实体瘤中，在小鼠的异位小鼠膀胱肿瘤模型中成功地抑制了肿瘤的生长。注射后长达14天，注射的植入物周围的肿瘤组织中的铂浓度保持在治疗水平以上，而血浆水平与全身给药相比降低了几个数量级。与全身给药相比，报道的给药系统将顺铂的最大耐受剂量提高了5倍，从而潜在地提高了顺铂在实体瘤模型中的抗肿瘤功效。

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