Casa Diani Meza, Carraro Talita Cristina Moreira Moraes, de Camargo Luciana Erzinger Alves, Dalmolin Luciana Facco, Khalil Najeh Maissar, Mainardes Rubiana Mara
J Nanosci Nanotechnol. 2015 Jan;15(1):848-54. doi: 10.1166/jnn.2015.9177.
In this study, poly(L-lactide) (PLA) nanoparticles containing amphotericin B (AmB) were developed, and the in vitro cytotoxicity to human erythrocytes and efficacy on strains of Candida spp. were evaluated. The nanoparticles were prepared using an emulsion/solvent evaporation method and were characterized with respect to size, size distribution, AmB encapsulation efficiency, AmB state of aggregation, and AmB in vitro release profile. The mean particle size was 225 nm, and the AmB encapsulation efficiency was over 69%. The AmB in vitro release profile revealed a burst effect within the first 24 h, which released approximately 10% of AmB, followed by a sustained release of approximately 30% of AmB over 30 days. The AmB nanoparticles presented a very low index of hemolysis compared to free AmB, which lysed more than 80% of erythrocytes in the first 2 h of incubation. The AmB-loaded PLA nanoparticles were as effective as free AmB against strains of Candida spp., considering their sustained release profile. Thus, PLA nanoparticles can deliver AmB with reduced toxicity while maintaining its antifungal activity.
在本研究中，制备了含有两性霉素B（AmB）的聚（L-丙交酯）（PLA）纳米颗粒，并评估了其对人红细胞的体外细胞毒性以及对念珠菌属菌株的疗效。采用乳液/溶剂蒸发法制备纳米颗粒，并对其尺寸、尺寸分布、AmB包封率、AmB聚集状态和AmB体外释放曲线进行了表征。平均粒径为225 nm，AmB包封率超过69%。AmB体外释放曲线显示，在前24小时内有一个突释效应，释放了约10%的AmB，随后在30天内持续释放约30%的AmB。与游离AmB相比，AmB纳米颗粒的溶血指数非常低，游离AmB在孵育的前2小时内使超过80%的红细胞裂解。考虑到其缓释特性，负载AmB的PLA纳米颗粒对念珠菌属菌株的效果与游离AmB相同。因此，PLA纳米颗粒可以在降低毒性的同时递送AmB，并保持其抗真菌活性。
