顺铂-白蛋白微球舌动脉导向治疗舌鳞癌的药物释放研究

目的　研究顺铂-白蛋白微球(CDDP-AMS)舌动脉导向治疗舌癌时,顺铂(DDP)在体内和肿瘤局部的释放情况。方法　采用自行研制的平均粒径为56·3μm的CDDP-AMS 100 mg(含CDDP 13·6 mg),经舌动脉推注治疗舌部鳞癌患者7例,分别测定患者外周静脉血和肿瘤切除标本组织匀浆中的铂含量,并与单纯CDDP给药组患者相比较,分析 CDDP-AMS药物释放的特点。结果　CDDP-AMS舌动脉推注治疗舌部鳞癌组,患者外周静脉血平均血药浓度在90 min时达峰值,10 d时血药浓度尚可测到;肿瘤局部药物浓度可较长时间维持恒定,到第17天时尚可测到。结论　CDDP-AMS 具有很强的缓释作用,起到了药物“贮存站”作用,达到肿瘤局部长时间高浓度、全身外周血低浓度的效果,消除了CDDP 全身大剂量用药时的毒副作用,值得推广应用。

Study on Drug Release after Arterial Embolism with Cisplain-loaded Albumin Microspheres in Treating Carcinoma of Tongue

Objective　The purpose of this study was to investigate the cisplatin release in peripheral blood and tumor tissue after cisplatin-loaded albumin microspheres (CDDP-AMS) were infused through lingual artery for treating carcinoma of tongue.Methods 　Anticancer agent cisplatin was encapsulated with biodegradable and non-antigenic albumin. The cisplatin-loaded albumin microsph- eres, which were 56·3μm in diameter, were used for treating 7 patients with squamous carcinoma of tongue by infusing through lingual artery. The cisplatin in peripheral venous blood and carcinoma tissue were measured for analyzing the drug releasein vivo.Results　 Concentration of the drug in peripheral venous blood increased to the highest level in 90 minutes after CDDP-AMS was infused through lingual arterial and still could be detected until 10th day. The cisplatin concentration in tumor tissue kept considerably stable and could be detected until 17 days.Conclusion　CDDP-AMS had the effect of controlled releaseinvive. Effective and steady local drug concen- tration played the role of killing tumor cells, the low concentration in peripheral blood reduced the side effects of cisplatin tominimum as well. It is concluded that CDDP-AMS is a useful and recommendable method for treating the carcinoma of tongue.