Preparation of pegylated nano-liposomal formulation containing SN-38: In vitro characterization and in vivo biodistribution in mice
Preparation of pegylated nano-liposomal formulation containing SN-38: In vitro characterization and in vivo biodistribution in mice
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DOI：
10.2478/v10007-009-0020-0
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发表时间：
2009-06-01
影响因子：
2.8
通讯作者：
Dinarvand, Rassoul
中科院分区：
文献类型：
--
作者：
Atyabi, Fatemeh;Farkhondehfai, Anahita;Dinarvand, Rassoul
7-乙基-10-羟基-喜树碱（SN-38）是伊立替康x HCl的代谢产物，在水溶液中溶解度极差，在大多数生理相容性和药学上可接受的溶剂中几乎不溶。因此，在用于胃肠外给药的浓缩药物递送系统中配制SN-38非常困难。由于其生物相容性和低毒性，考虑使用脂质体递送SN-38。本研究制备了SN-38聚乙二醇脂质体，并对其粒径、包封率、体外释药和体内分布等进行了考察。脂质体的粒径在150-200 nm范围内。聚乙二醇化脂质体的包封率和体外释放度均高于非聚乙二醇化脂质体。正如预期的那样，聚乙二醇化脂质体在身体器官如肝、肾、脾和肺中的分布显著低于非聚乙二醇化脂质体。此外，它们的血液浓度比非聚乙二醇化脂质体高至少50%。
7-Ethyl-10-hydroxy-camptothecin (SN-38), a metabolite of irinotecan x HCl, is poorly soluble in aqueous solutions and practically insoluble in most physiologically compatible and pharmaceutically acceptable solvents. Formulation of SN-38 in concentrated pharmaceutical delivery systems for parenteral administration is thus very difficult. Due to their biocompatibility and low toxicity, liposomes were considered for the delivery of SN-38. In this study, pegylated liposomes with distearoylphosphatidylcholine, distearoylphosphatidylethanolamine containing SN-38 were prepared and their characteristics, such as particle size, encapsulation efficiency, in vitro drug release and biodistribution, were investigated. The particle size of liposomes was in the range of 150-200 nm. The encapsulation efficiency and in vitro release rate of pegylated liposomes was higher than those of non-pegylated liposomes. As expected, the distribution of pegylated liposomes in body organs such as liver, kidney, spleen and lung was considerably lower than that of non-pegylated liposomes. Also, their blood concentration was at least 50 % higher than that of non-pegylated liposomes.