Evaluation of in vitro and in vivo antitumor activity of BCNU-Ioaded PLGA wafer against 9L gliosarcoma
Evaluation of in vitro and in vivo antitumor activity of BCNU-Ioaded PLGA wafer against 9L gliosarcoma
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DOI：
10.1016/j.ejpb.2004.06.006
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发表时间：
2005-01-01
影响因子：
4.9
通讯作者：
Khang, G
中科院分区：
文献类型：
--
作者：
Lee, JS;An, TK;Khang, G
本研究的目的是研制一种可植入的BCNU-聚（D，L-丙交酯-乙交酯）（PLGA）缓释片，用于1，3-二（2-氯乙基）-1-亚硝基脲（BCNU）的控释，并评价其体内外抗肿瘤活性。BCNU在PLGA片中的释放速率随载药量的增加而增加，并持续释放至7 d。使用对9 L胶质肉瘤细胞的体外细胞毒性和皮下（s.c.）9 L胶质肉瘤实体瘤模型。由于BCNU的半衰期较短，因此含BCNU的薄片比BCNU粉末显示出更有效的细胞毒性，并抑制9 L胶质肉瘤细胞的增殖。载BCNU的PLGA薄片显著延迟肿瘤的生长，并且增加薄片中BCNU的剂量导致肿瘤的实质性消退。载卡氮芥PLGA片的抗肿瘤活性的这些结果证明了用于临床应用的可行性。(C)2004 Elsevier B. V.保留所有权利。
The purpose of the present study was to develop implantable BCNU-Ioaded poly(D,L-lactide-co-glycolide) (PLGA) wafer for the controlled release of 1,3-bis(2-chloroethyl)-1-nitrosourea(BCNU) and to evaluate its in vitro and in vivo antitumor activity. The release rate of BCNU from PLGA wafer increased with the increase of BCNU amount loaded and the release was continued until 7 days. In vitro and in vivo antitumor activity of BCNU-Ioaded PLGA wafer was investigated using in vitro cytotoxicity against 9L gliosarcoma cells and a subcutaneous (s.c.) solid tumor model of 9L gliosarcoma, respectively. The wafers containing BCNU showed more effective cytotoxicity than BCNU powder due to its short half-life and inhibited the proliferation of 9L gliosarcoma cells. BCNU-Ioaded PLGA wafer delayed the growth of the tumors significantly and increasing the dose of BCNU in the wafer resulted in a Substantial regression of the tumor. These results of antitumor activity of BCNU-Ioaded PLGA wafer demonstrate the feasibility of the wafers for clinical application. (C) 2004 Elsevier B.V. All rights reserved.