[3H]-메토트렉세이트-락토오스아미노화한 소 혈청 알부민 공유결합체의 간표적성 및 체내동태

• 영문명: Liver Targetability and Pharmacokinetics of [3H]-Methotrexate-Lactosaminated Bovine Serum Albumin Conjugates
• 발행기관: 대한약학회
• 저자명: 김종국(Chong Kook Kim) 이응두(Woong Doo Lee) 박호군(Ho Koon Park)
• 간행물 정보: 『약학회지』제36권 제6호 (1992년), 591~597쪽, 전체 7쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1992.12.29

영문 초록

The organ distribution of [3H]-methotrexate-lactosaminated bovine serum albumin conjugates ([3H]-MTX-LBSA) was investigated to examine their role as a liver-specific anticancer drug. Synthesis of lactosaminated bovine serum albumin(LBSA) with BSA, lactose and sodium cyanoborohydride through reductive animation was followed by its conjugation with methotrexate (MTX) and 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC), thereby synthesizing [3H]-MTX-LBSA conjugates. Organ distribution and plasma elimination profiles were studied in male Wistar rats after intravenous injection of [3H]-MTX-LBSA conjugates. The fates of [3H]-MTX and the [3H]-MTX-BSA conjugates fates were also investigated for comparison. The results showed that the plasma level of [3H]-MTX-LBSA conjugates declined more rapidly than those of [3H]-MTX-BSA and their liver concentration was significantly higher than those of other treatment (p<0.01). In addition, their uptake compared to the amount taken up by the liver (1 : 33.1 at 10min, 1 : 24.1 at 120min). All these suggested that MTX-LBSA conjugate is one of the drug delivery system (DDS) that is advanced in concentrating MTX in the liver and minimizing the renal toxicity of MTX.

키워드

Methotrexate lactosaminated bovine serum albumin methotrexate-lactosaminated bovine serum albumin conjugates pharmacokinetics organ distribution liver targetability drug targeting.