Department of Pharmaceutical Technology, College of Pharmacy, University of Tanta, Tanta, Egypt.
Curr Drug Deliv. 2020;17(10):861-873. doi: 10.2174/1567201817666200708113131.
Cancers are life threatening diseases and their traditional treatment strategies have numerous limitations which include poor pharmacokinetic profiles, non-specific drug distribution in the body tissues and organs and deprived tumor cells penetration. This attracted the attention of researchers to tailor efficient drug delivery system for anticancer agents to overcome these limitations. Liposomes are one of the newly developed delivery systems for anticancer agents. They are vesicular structures, which were fabricated to enhance drug targeting to tumor tissues either via active or passive targeting. They can be tailored to penetrate tumor cells membrane which is considered the main rate limiting step in antineoplastic therapy. This resulted in enhancing drug cellular uptake and internalization and increasing drug cytotoxic effect. These modifications were achieved via various approaches which included the use of cell-penetrating peptides, the use of lipid substances that can increase liposome fusogenic properties or increase the cell membrane permeability toward amphiphilic drugs, surface modification or ligand targeted liposomes and immuno-liposomes. The modified liposomes were able to enhance anticancer agent's cellular uptake and this was reflected in their ability to destroy tumor tissues. This review outlines different approaches employed for liposomes modification for enhancing anticancer agent's cellular uptake.
癌症是危及生命的疾病，其传统治疗策略存在许多局限性，包括药代动力学特性差、药物在体内组织和器官中的非特异性分布以及肿瘤细胞摄取能力不足。这引起了研究人员的关注，他们致力于开发有效的抗癌药物传递系统，以克服这些局限性。脂质体是新型抗癌药物传递系统之一。它们是囊泡结构，被设计用来通过主动或被动靶向增强药物对肿瘤组织的靶向性。它们可以穿透肿瘤细胞膜，这被认为是抗肿瘤治疗的主要限速步骤。这导致了药物细胞摄取和内化的增强，并增加了药物的细胞毒性作用。这些修饰是通过各种方法实现的，包括使用穿透细胞的肽、使用可以增加脂质体融合特性或增加亲脂性药物对细胞膜通透性的脂质物质、表面修饰或配体靶向脂质体和免疫脂质体。修饰后的脂质体能够增强抗癌药物的细胞摄取，这反映在它们破坏肿瘤组织的能力上。本文综述了为增强抗癌药物的细胞摄取而对脂质体进行修饰的不同方法。
