包裹[3H]甲氨蝶呤的脂质体注入正常或关节炎兔关节后的滞留与分布情况。
Retention and distribution of liposome-entrapped [3H]methotrexate injected into normal or arthritic rabbit joints.
作者信息
Foong W C, Green K L
机构信息
School of Pharmacy and Biomedical Sciences, Portsmouth Polytechnic, UK.
出版信息
J Pharm Pharmacol. 1988 Jul;40(7):464-8. doi: 10.1111/j.2042-7158.1988.tb05278.x.
Normal or arthritic rabbits were injected intra-articularly (i.a.) with free [3H]methotrexate ([3H]MTX) or liposomes containing [3H]MTX with [14C]cholesteryl oleate as a lipid marker. The distribution of 3H and 14C in the injected joint and other tissues was determined. Free [3H]MTX was rapidly cleared from the joint, 79% being excreted in the urine within 24 h of injection. Liposome-entrapment retarded [3H]MTX clearance from the joint (P less than 0.001), 45.5% being recovered from the joint 24 h after injection. Uptake of liposomes by the inflamed synovium was lower than expected, 4% liposomal [3H]MTX injected being associated with the synovium after 24 h. Nevertheless, this was 40-fold greater than when free [3H]MTX was injected. Liposome entrapment should improve the efficacy and reduce the side effects of drugs injected directly into the joint cavity.
将游离的[³H]甲氨蝶呤（[³H]MTX）或含有[³H]MTX且以[¹⁴C]油酰胆固醇为脂质标记物的脂质体关节内注射（i.a.）到正常或患有关节炎的兔子体内。测定³H和¹⁴C在注射关节及其他组织中的分布。游离的[³H]MTX迅速从关节清除，注射后24小时内79%经尿液排出。脂质体包封延缓了[³H]MTX从关节的清除（P小于0.001），注射后24小时从关节回收45.5%。炎症滑膜对脂质体的摄取低于预期，注射后24小时，滑膜中与脂质体结合的[³H]MTX占注射量的4%。然而，这比注射游离[³H]MTX时高40倍。脂质体包封应能提高直接注射到关节腔内药物的疗效并减少其副作用。
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