Sautereau A M, Cros S, Tocanne J F
Biopharm Drug Dispos. 1986 Jul-Aug;7(4):357-71. doi: 10.1002/bdd.2510070406.
Encapsulation in liposomes of the antitumoral drug 2-methyl 9-hydroxyellipticinium and the consequences of its cytotoxicity in vitro on L1210 leukemia cells and on its antitumoral activity in vivo on leukemic mice inoculated with L1210 cells are described. Provided the drugs is dissolved in the buffer below its critical micelle concentration (10(-4) M), it can be encapsulated in lipid vesicles with a very good yield in the form of a very stable combination with the lipids. The in vitro experiments show that 2-CH3 9-OH-ellipticinium is less cytotoxic against L1210 cells when entrapped than when free in solution. The in vivo experiments on tumor-bearing mice show that encapsulation of the drug reduces its toxicity. Encapsulation maintains the antitumoral activity of the drug or increases it if the leukemia is delayed (10(4) cells injected per mouse instead of 10(5) cells per mouse).
描述了抗肿瘤药物2-甲基-9-羟基玫瑰树碱脂质体包封及其体外对L1210白血病细胞的细胞毒性后果，以及其对接种L1210细胞的白血病小鼠体内抗肿瘤活性的影响。若药物溶解于低于其临界胶束浓度（10⁻⁴ M）的缓冲液中，它能以与脂质非常稳定的组合形式，高收率地包封于脂质囊泡中。体外实验表明，与游离于溶液中相比，包封后的2-CH₃ 9-OH-玫瑰树碱对L1210细胞的细胞毒性较小。对荷瘤小鼠的体内实验表明，药物包封可降低其毒性。如果白血病延迟（每只小鼠注射10⁴个细胞而非10⁵个细胞），包封可维持药物的抗肿瘤活性或增强其活性。
