Couvreur P, Fattal E, Andremont A
Laboratoire de Pharmacie Galénique et Biopharmacie, URA CNRS 1218, University of Paris XI, France.
Pharm Res. 1991 Sep;8(9):1079-86. doi: 10.1023/a:1015885814417.
The treatment of infections caused by obligate or facultative intracellular microorganisms is difficult because most of the available antibiotics have either poor intracellular diffusion and retention or reduced activity at the acidic pH of the lysosomes. The need for antibiotics with greater intracellular efficacy led to the development of endocytosable drug carriers, such as liposomes and nanoparticles, which mimic the entry path of the bacteria by penetrating the cells into phagosomes or lysosomes. This Review assesses the potential of liposomes and nanoparticles in the targeted antibiotic therapy of intracellular bacterial infections and diseases and the pharmaceutical advantages and limitations of these submicron delivery systems.
专性或兼性细胞内微生物引起的感染治疗起来很困难,因为大多数现有抗生素要么细胞内扩散和留存能力差,要么在溶酶体的酸性pH值环境下活性降低。对具有更高细胞内疗效的抗生素的需求促使了可内吞药物载体的开发,如脂质体和纳米颗粒,它们通过穿透细胞进入吞噬体或溶酶体来模拟细菌的进入途径。本综述评估了脂质体和纳米颗粒在细胞内细菌感染和疾病的靶向抗生素治疗中的潜力,以及这些亚微米递送系统的药学优势和局限性。