[博来霉素聚 DL-乳酸微球在大鼠体内的药物分布及抗肿瘤作用]

[Drug distribution and antitumor effect of bleomycin incorporated in poly DL-lactic acid in rats].

作者信息

Kumanohoso T, Natsugoe S, Tokuda K, Shimada M, Sagara M, Shinkawa T, Nakamura K, Yamada K, Fukuzaki H, Aikou T

机构信息

First Dept. of Surgery, Kagoshima University School of Medicine.

出版信息

Gan To Kagaku Ryoho. 1994 Sep;21(13):2248-50.

PMID:7524449

Abstract

Two bleomycin (BLM)-containing agents (BLM-PLA, BLM-SOL) were prepared, and the drug distribution and antitumor effect were studied. BLM-PLA is an agent in which BLM is incorporated into biodegradable low-molecular-weight polylactic acid, and BLM-SOL is an aqueous solution of BLM. BLM-PLA or BLM-SOL was subcutaneously administered in the back of rats. When BLM-PLA was implanted, high BLM activity of the connective tissues near the implants was maintained for 2 weeks. On the other hand, BLM activity was very low when BLM-SOL was administered. The effects of BLM-PLA, BLM-SOL and nontreatment on tumor growth and survival time were compared using subcutaneous tumor of Yoshida sarcoma in 21 rats each. The survivors and mean survival time in BLM-PLA group, BLM-SOL group and nontreatment group was 14 and 44.6 days, 5 and 23.7 days, and 0 and 11.3 days, respectively. BLM-PLA was superior to BLM-SOL in both drug distribution and antitumor effect, and consequently BLM-PLA could be a useful tool in loco-regional chemotherapy.

摘要

制备了两种含博来霉素（BLM）的制剂（BLM-PLA、BLM-SOL），并研究了药物分布和抗肿瘤效果。BLM-PLA是将BLM掺入可生物降解的低分子量聚乳酸中的制剂，而BLM-SOL是BLM的水溶液。将BLM-PLA或BLM-SOL皮下注射到大鼠背部。植入BLM-PLA时，植入物附近结缔组织的高BLM活性维持了2周。另一方面，给予BLM-SOL时BLM活性非常低。使用吉田肉瘤皮下肿瘤对21只大鼠分别比较了BLM-PLA、BLM-SOL和不治疗对肿瘤生长和存活时间的影响。BLM-PLA组、BLM-SOL组和不治疗组的存活大鼠数和平均存活时间分别为14只和44.6天、5只和23.7天、0只和11.3天。BLM-PLA在药物分布和抗肿瘤效果方面均优于BLM-SOL，因此BLM-PLA可能是局部区域化疗的有用工具。