脂质体包封率的研究进展

Research Progress on Encapsulation Efficiency of Liposomes

脂质体是由脂质双分子层包裹水相形成的囊泡结构。它既可以在内水相包裹亲水性药物,又可以在脂质双分子层中包裹亲脂性药物。由于脂质双分子层结构和天然细胞形态相似,所以常被报道为人体理想的药物载体。它的应用对神经系统疾病、恶性肿瘤、遗传性疾病等的诊断和治疗都有重要意义。控制脂质体的包封率对于设计和开发脂质体制剂很重要。高的包封率是一个很重要的特性,此外,包封率也是对脂质体制剂的监管要求。该文通过查阅相关文献,对脂质体包封率的测定方法进行综述,并讨论脂质膜组成、磷脂链长度、电位和不同制备方法对脂质体包封率的影响。

Liposomes are vesicles composed of phospholipid bilayers surrounding an aqueous compartment. It is possible to encapsulate not only hydrophilic drugs in the inner aqueous compartment, but also lipophilic compounds in the lipidic double layer. Lipidic double layer is ideal for drug delivery to the human body, due to the similarity with natural cells. Its application is important to the diagnosis and treatment of nervous system diseases, malignant tumors, hereditary diseases and so on. When designing and developing a liposome formulation, it is important to control the encapsulation efficiency. High drug encapsulation is a very important characteristic. Furthermore, evaluation of EE is a regulatory requirement. Herein, our aim is to review the relevant papers in the literature on method for determination of entrapment efficiency and discuss the effect of the lipid membrane composition, phospholipid chain length, charge, and different liposome preparation methods on the encapsulation efficiency.