Locoregional cancer chemotherapy of the esophageal cancer

我们设计了三种给药系统：硅胶吸附博莱霉素（BLM-S1）、聚乳酸（BLM-PLA）和聚乳酸/聚乙二醇酸共混微球（CDDP-MS）。结果如下：1）在食管癌的临床初步研究中，在手术前经内镜将BLm-Sl或布来霉素溶液（BLM-SOL）注射到食管壁中。BLM-S1给药组淋巴结和结缔组织中的博来霉素活性显著高于BLM-SOL给药组。36个转移淋巴结中有11个在显微镜下观察到变性或坏死改变。除发热外，未发现其他严重的全身副作用。2）在大鼠吉田肉瘤的抗肿瘤实验研究中，BLM-PLA在药物分布和抗肿瘤作用方面均上级博莱霉素溶液。3）在吉田肉瘤大鼠腹膜播散实验模型中，CDDP-MS能控制恶性腹水，与CDDP溶液相比无严重副作用。这三种药物形式可能是用于靶向化疗的有用形式。

We deviced three drug delivery systems : bleomycin adsorbed on silica particles (BLM-Sl), bleomycin incorporated into small cylinder of poly d, l-lactic acid (BLM-PLA) and cisplatin incorporated into poly lactic acid / polyethylene glycol acid blend microspheres (CDDP-MS). The results were as followes.1) In a clinical pilot study for esophageal carcinoma, BLm-Sl or blemycin solution (BLM-SOL) was endoscopically injected into the esophageal wall prior to surgery. Bleomycin activity in the lymph nodes and connective tissues was significantly higher in BLM-Sl administration that those in BLM-SOL administration. Degenerative or necrotic changes were microscopically observed in 11 of 36 metastatic lymph nodes. Serious systemic side effects except for fever were not observed.2) In the experimental study on the antitumor effect against Yoshida sarcoma in rats, BLM-PLA was superior to bleomycin solution in both drug distribution and antitumor effect.3) In the experimental model of peritoneal dissemination in rats using Yoshida sarcoma, CDDP-MS was able to control malignant ascites without serious side effect compared with CDDP solution.In conclusion, these three drug formes could be a useful modality for targeting chemotherapy.