Love W G, Amos N, Kellaway I W, Williams B D
Pharmacy Department, University of Wales College Cardiff.
Ann Rheum Dis. 1990 Aug;49(8):611-4. doi: 10.1136/ard.49.8.611.
High performance liquid chromatography has shown that after intravenous injection cholesterol-poor liposomes (100 nm) are unstable and their phospholipid is redistributed. Under identical conditions cholesterol-rich liposomes remain structurally intact within the circulation. When injected intravenously cholesterol-rich liposomes accumulate within the inflamed paws of rats with adjuvant induced arthritis to the same extent as cholesterol-poor liposomes. Uptake in inflamed tissue of three cholesterol-rich liposome preparations was always significantly greater than the uptake noted in normal tissue. The degree of accumulation in inflamed tissue was found to depend on the size of the liposome, with the greatest uptake, 7% of the injected dose, achieved by the smallest vesicle (100 nm). These results indicate that intact liposomes accumulate at inflamed joint tissue sites. Therefore the passive targeting of anti-inflammatory drugs encapsulated within these liposomes could be contemplated.
高效液相色谱法表明,静脉注射后,胆固醇含量低的脂质体(100纳米)不稳定,其磷脂会重新分布。在相同条件下,富含胆固醇的脂质体在循环中保持结构完整。静脉注射时,富含胆固醇的脂质体在佐剂诱导性关节炎大鼠的炎症爪子中积累的程度与胆固醇含量低的脂质体相同。三种富含胆固醇的脂质体制剂在炎症组织中的摄取量总是显著高于正常组织中的摄取量。发现炎症组织中的积累程度取决于脂质体的大小,最小的囊泡(100纳米)摄取量最大,达到注射剂量的7%。这些结果表明完整的脂质体在炎症关节组织部位积累。因此,可以考虑将包裹在这些脂质体内的抗炎药物进行被动靶向。