리포좀에 봉입된 아클라루비신의 약물동태, 세포독성, 항암효과 및 비장/혈구 세포독성

• 영문명: Pharmacokinetics, Cell Toxicity, Antitumor Activity and Spleen/Blood Cell Toxicity of Aclarubicin-entrapped Liposomes
• 발행기관: 대한약학회
• 저자명: 박목순(Mork Soon Park) 박진규(Jin Kyu Park) 이계원(Gye Won Lee) 명평근(Pyung Keun Myung) 석대은(Dai Eun Sok) 황성주(Sung Joo Hwang) 지웅길(Ung Kil Lee)
• 간행물 정보: 『약학회지』제42권 제3호 (1998년), 275~283쪽, 전체 9쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1998.06.30

영문 초록

Aclarubicin(ACL)-entrapped freeze dried liposomes were prepared using Microfludizer to attain a sustained release at targeted organs in a prolonged time so that it can reduce the side effect and maximize the therapeutic effect. The freeze-dried liposomes were evaluated for pharmacokinetics, antitumor activity against Sarcoma 180, cytotoxicity against L1210 and A549 tumor cells, spleen toxicity and myelosuppressive action. The AUC0->8hr values were 122+/-42, 382+/-140, 419+/-171, 835+/-206 and 443+/-309mcg min/ml for free ACL. ACL-liposome formulation I, II, III and IV, respectively. Cytotoidcity of ACL-entrapped liposomes against L1210 and A549 tumor cells was 2-4 times higher than that of free aclarubicin. ACL-liposome formulation I(PC/CHOL/TA) showed the most potent antitumor activity against Sarcoma 180 in mice. The loss of body weight was much smaller with ACL-entrapped liposomes than free ACL after I.p. injection at a dose of 2 mg/kg/day. Compared to free ACL, ACL-entrapped liposomes expressed a lower and delayed spleen toxicity up to 5th day after I.v. administration. Myelosupperssion seemed to be lower with ACL-entrapped liposome of PC/PC-hydrate/CHOL/TA (formulation III) than free aclarubicin.

키워드

Aclarubicin microfluidizer pharmacokinetics cytotoxicity freeze dried liposome antitumor activity myelosuppression.