抗生素脂质体的研究

Researches on the liposomal antibiotics

细菌耐药性已成为一个全球性医学难题。利用制剂学手段,通过改进抗生素的体内行为,改善其抗菌效果,是解决细菌耐药性的重要方法。脂质体是研究最广泛的纳米制剂之一,具有良好的生物相容性和可修饰性,目前已经有抗生素脂质体上市或进入临床研究。将脂质体作为抗生素药物载体,可以有效提高炎症部位抗生素的局部浓度,抑制细菌诱导耐药性的产生,并有利于减小全身给药剂量,降低毒副作用。本文较为系统地介绍了脂质体的基本结构以及几种典型的抗生素脂质体(包括两性霉素B脂质制剂、莫匹罗星脂质体、阿米卡星脂质体以及多黏菌素B脂质体),以期为抗生素脂质体的研究和发展提供参考。最后还简述了以细菌生物膜为靶点的新的抗生素脂质体的研究。

Antimicrobial resistance has been a global challenge to public health. One of the important solutions to increase antimicrobial effect of antibiotics is by the improvement of their in vivo behaviors via nanoliposome delivery system. Liposomal antibiotics have shown better therapeutics effects in infectious diseases with less doses and smaller adverse effects. The review summarized the basic properties of liposomes and the advantages of liposomal delivery system for antibiotics. Four typical nanoliposomal antibiotics under development or in the market are reviewed with the emphasis on their formulations, structures, pharmacokinetics and the therapeutic benefits. Progresses in the new liposomal antibiotics that target the biofilms are also introduced.