Rogerson A, Cummings J, Willmott N, Florence A T
Department of Pharmacy, School of Pharmacy and Pharmacology, University of Strathclyde, Glasgow, UK.
J Pharm Pharmacol. 1988 May;40(5):337-42. doi: 10.1111/j.2042-7158.1988.tb05263.x.
Large multilamellar non-ionic surfactant vesicles (niosomes) with diameters of around 800-900 nm prepared from a C16 triglyceryl ether with and without cholesterol and containing doxorubicin (Adriamycin) were administered to S180 tumour-bearing NMRI mice by bolus injection. Although in-vitro drug release from cholesterol-containing niosomes is delayed, in-vivo there was little difference between the two preparations when plasma levels were compared. As previously observed, half-lives of the drug were prolonged compared with free solution profiles. Liver uptake was not significantly affected by niosome encapsulation of doxorubicin. There is minor accumulation of drug in the lung, perhaps because of aggregation of the vesicles and their physical entrapment. Tumour levels of drug were higher following administration of cholesterol-containing niosomes and this was reflected in the more effective reduction in tumour growth. Metabolism of doxorubicin is altered by niosomal administration, but more studies are required before the significance of the metabolic data can be assessed.
将由含有和不含胆固醇的C16甘油三醚制备的、直径约为800 - 900 nm的大多层非离子表面活性剂囊泡（脂质体），其中含有阿霉素（多柔比星），通过大剂量注射给予荷S180肿瘤的NMRI小鼠。尽管含胆固醇脂质体的体外药物释放延迟，但比较血浆水平时，两种制剂在体内几乎没有差异。如先前观察到的，与游离溶液曲线相比，药物的半衰期延长。阿霉素脂质体包封对肝脏摄取没有显著影响。药物在肺中有少量蓄积，这可能是由于囊泡聚集及其物理截留所致。给予含胆固醇脂质体后肿瘤中的药物水平更高，这反映在肿瘤生长的更有效降低上。阿霉素的代谢因脂质体给药而改变，但在评估代谢数据的意义之前还需要更多研究。
