Khan Amjad Ali, Allemailem Khaled S, Almatroodi Saleh A, Almatroudi Ahmed, Rahmani Arshad Husain
1Department of Basic Health Science, College of Applied Medical Sciences, Qassim University, P.O. Box 6699, Buraidah, 51452 Saudi Arabia.
2Department of Medical Laboratories, College of Applied Medical Sciences, Qassim University, P.O. Box 6699, Buraidah, 51452 Saudi Arabia.
3 Biotech. 2020 Apr;10(4):163. doi: 10.1007/s13205-020-2144-3. Epub 2020 Mar 10.
Liposomes are very useful biocompatible tools used in diverse scientific disciplines, employed for the vehiculation and delivery of lipophilic, ampiphilic or hydrophilic compounds. Liposomes have gained the importance as drug carriers, as the drugs alone have limited targets, higher toxicity and develop resistance when used in higher doses. Conventional liposomes suffer from several drawbacks like encapsulation inefficiencies and partially controlled particle size. The surface chemistry of liposome technology started from simple conventional vesicles to second generation liposomes by modulating their lipid composition and surface with different ligands. Introduction of polyethylene glycol to lipid anchor was the first innovative strategy which increased circulation time, delayed clearance and opsonin resistance. PEGylated liposomes have been found to possess higher drug loading capacity up to 90% or more and some drugs like CPX-1 encapsuled in such liposomes have increased the disease control up to 73% patients suffering from colorectal cancer. The surface of liposomes have been further liganded with small molecules, vitamins, carbohydrates, peptides, proteins, antibodies, aptamers and enzymes. These advanced liposomes exhibit greater solubility, higher stability, long-circulating time and specific drug targeting properties. The immense utility and demand of surface modified liposomes in different areas have led their way to the modern market. In addition to this, the multi-drug carrier approach of targeted liposomes is an innovative method to overcome drug resistance while treating ceratin tumors. Presently, several second-generation liposomal formulations of different anticancer drugs are at various stages of clinical trials. This review article summarizes briefly the preparation of liposomes, strategies of disease targeting and exclusively the surface modifications with different entities and their clinical applications especially as drug delivery system.
脂质体是非常有用的生物相容性工具，应用于多种科学学科，用于运载和亲脂性、两亲性或亲水性化合物的递送。脂质体作为药物载体已变得至关重要，因为单独使用药物时靶点有限、毒性较高，且高剂量使用时会产生耐药性。传统脂质体存在一些缺点，如包封效率低和粒径控制不完全。脂质体技术的表面化学从简单的传统囊泡发展到第二代脂质体，通过调节其脂质组成和用不同配体修饰表面来实现。将聚乙二醇引入脂质锚定是第一个创新策略，它增加了循环时间、延迟了清除并具有抗调理素作用。已发现聚乙二醇化脂质体具有高达90%或更高的药物负载能力，一些包裹在这种脂质体中的药物（如CPX-1）使患有结直肠癌的患者疾病控制率提高到了73%。脂质体表面已进一步与小分子、维生素、碳水化合物、肽、蛋白质、抗体、适体和酶进行配体结合。这些先进的脂质体表现出更大的溶解度、更高的稳定性、更长的循环时间和特定的药物靶向特性。表面修饰脂质体在不同领域的巨大实用性和需求使其进入了现代市场。除此之外，靶向脂质体的多药载体方法是在治疗某些肿瘤时克服耐药性的一种创新方法。目前，几种不同抗癌药物的第二代脂质体制剂正处于临床试验的不同阶段。这篇综述文章简要总结了脂质体的制备、疾病靶向策略，特别是用不同实体进行的表面修饰及其临床应用，尤其是作为药物递送系统的应用。
