Gregoriadis G, Florence A T
Centre for Drug Delivery Research, School of Pharmacy, University of London, England.
Drugs. 1993 Jan;45(1):15-28. doi: 10.2165/00003495-199345010-00003.
Liposomes (phospholipid-based vesicles) have been investigated since 1970 as a system for the delivery or targeting of drugs to specific sites in the body. Because of their structural versatility in terms of size, composition, surface charge, bilayer fluidity and ability to incorporate almost any drug regardless of solubility, or to carry on their surface cell-specific ligands, liposomes have the potential to be tailored in a variety of ways to ensure the production of formulations that are optimal for clinical use. This includes controlled retention of entrapped drugs in the presence of biological fluids, controlled vesicle residence in the blood circulation or other compartments in the body, and enhanced vesicle uptake by target cells. Accumulated in vivo evidence, particularly in areas such as cancer chemotherapy, antimicrobial therapy, vaccines, diagnostic imaging and the treatment of ophthalmic disorders has indicated clearly that some liposome-entrapped drugs and vaccines exhibit superior pharmacological properties to those observed with conventional formulations. Such work has encouraged the application of liposomes in the treatment of diseases in humans. A large number of trials in patients with cancer or infections suggest that certain liposomal drug formulations are likely to prove clinically useful.
自1970年以来,脂质体(基于磷脂的囊泡)就作为一种将药物递送至体内特定部位或靶向特定部位的系统而被研究。由于脂质体在大小、组成、表面电荷、双层流动性以及几乎能够包封任何药物(无论其溶解性如何)或在其表面携带细胞特异性配体方面具有结构多样性,因此有潜力以多种方式进行定制,以确保生产出最适合临床使用的制剂。这包括在生物流体存在的情况下对包封药物的可控保留、在血液循环或体内其他隔室中对囊泡驻留的控制以及增强靶细胞对囊泡的摄取。体内积累的证据,特别是在癌症化疗、抗菌治疗、疫苗、诊断成像和眼科疾病治疗等领域的证据清楚地表明,一些脂质体包封的药物和疫苗表现出优于传统制剂的药理学特性。此类研究推动了脂质体在人类疾病治疗中的应用。针对癌症患者或感染患者进行的大量试验表明,某些脂质体药物制剂可能在临床上被证明是有用的。