Youssef M, Fattal E, Alonso M J, Roblot-Treupel L, Sauzières J, Tancrède C, Omnès A, Couvreur P, Andremont A
Laboratoire d'Ecologie Microbienne, Institut Gustave-Roussy, Villejuif, France.
Antimicrob Agents Chemother. 1988 Aug;32(8):1204-7. doi: 10.1128/AAC.32.8.1204.
The effectiveness of nanoparticle-bound ampicillin was tested in the treatment of experimental Listeria monocytogenes infection in congenitally athymic nude mice. Nanoparticles of polyisohexylcyanoacrylate (PIHCA) 187 +/- 13 nm in diameter were bound to ampicillin at an ampicillin/PIHCA ratio of 0.2:1. The proportion of ampicillin bound was 90% +/- 3%. After adsorption onto nanoparticles, the therapeutic activity of ampicillin increased dramatically over that in the free state. Thus, 2.4 mg of nanoparticle-bound ampicillin (three doses of 0.8 mg each) had a greater therapeutic effect than 48 mg of free ampicillin (three doses of 16 mg each). These results might provide an incentive for further development of intracellular targeting of antibiotics on biodegradable polymeric carriers.
在先天性无胸腺裸鼠实验性单核细胞增生李斯特菌感染的治疗中,测试了纳米颗粒结合氨苄青霉素的有效性。直径为187±13纳米的聚异己基氰基丙烯酸酯(PIHCA)纳米颗粒以氨苄青霉素/PIHCA比例0.2:1与氨苄青霉素结合。结合的氨苄青霉素比例为90%±3%。吸附到纳米颗粒上后,氨苄青霉素的治疗活性比游离状态下显著增加。因此,2.4毫克纳米颗粒结合的氨苄青霉素(每次0.8毫克,共三剂)比48毫克游离氨苄青霉素(每次16毫克,共三剂)具有更大的治疗效果。这些结果可能会激励人们进一步开发可生物降解聚合物载体上抗生素的细胞内靶向应用。