Characterization, lung targeting profile and therapeutic efficiency of dipyridamole liposomes
Characterization, lung targeting profile and therapeutic efficiency of dipyridamole liposomes
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DOI：
10.1080/10611860600916586
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发表时间：
2006-12-01
影响因子：
4.5
通讯作者：
Zhu Jia-Bi
中科院分区：
文献类型：
--
作者：
Cheng Ji;Wen Na;Zhu Jia-Bi
急性呼吸窘迫综合征(ARDS)是一种严重的急性肺损伤(ALI)。其发病机制与活性氧(ROS)密切相关。抗氧化剂被认为是一种有效的治疗方法。此外，脂质体作为潜在的药物载体被广泛研究，因为它们能够保护药物分子并将其携带到靶器官如肺。本研究旨在探讨脂质体双嘧达莫(DIP)对脂多糖(LPS)诱导的急性肺损伤(ALI)的影响。首先，采用薄膜水合法制备包埋DIP的脂质体，用于治疗ARDS。测定了包封率、包封率和包封率。用反相高效液相色谱法测定小鼠静脉注射DIP和DIP脂质体后组织和血浆中DIP的浓度变化，并计算肺靶向参数。为验证其治疗效果，比较了DIP脂质体和DIP注射对脂多糖诱导的ALI的影响。结果表明，DIP脂质体具有较高的包封率和较好的粒径。与DIP注射相比，脂质体能大幅度增加DIP在肺内的蓄积。此外，DIP脂质体可显著减轻内毒素所致的ALI。以上结果提示，DIP脂质体具有明显的肺靶向性，具有治疗ALI/ARDS的潜在疗效。
The acute respiratory distress syndrome (ARDS) is a severe form of acute lung injury (ALI). Its pathogenesis is closely linked with reactive oxygen species (ROS). Antioxidation has been considered as an efficient treatment. Besides, liposomes are widely investigated as potential drug carriers due to their ability to protect and carry drug molecules to the target organ such as the lung. The present study was undertaken to investigate whether dipyridamole (DIP), delivered as a liposomal preparation, can ameliorate the lipopolysaccharides (LPS)-induced ALI due to the changes of its biodistribution. First, the liposomes entrapping DIP were prepared by film hydration for treating ARDS. Subsequently, the characterizations including entrapment efficiency, size, span and micrograph of DIP liposomes were measured. The concentration change of DIP in tissues and plasma of mice after intravenous administration of DIP injection and DIP liposomes was determined by RP-HPLC and calculated to lung targeting parameters. To prove the therapeutic efficiency, the effects of DIP liposomes on LPS-induced ALI were studied compared with DIP injection. The results showed DIP liposomes have the relative high entrapment efficiency and satisfying particle size. Compared with DIP injection, the liposomes increased the accumulation of DIP in the lung on a vast scale. Furthermore, DIP liposomes alleviated the ALI induced by LPS significantly. All of the results suggested that DIP liposomes have the potential efficacy in treating ALI/ARDS due to their obvious lung targeting.