Pedroso Ligia Santos, Khalil Najeh Maissar, Mainardes Rubiana Mara
Pharmacy Department, Laboratory of Pharmaceutical Nanotechnology, Universidade Estadual do Centro-Oeste/ UNICENTRO, Simeão Camargo Varela de Sa Street 03, 85040-080 Guarapuava, PR, Brazil.
Curr Drug Deliv. 2018;15(7):1055-1063. doi: 10.2174/1567201815666180409103028.
In this study, bovine serum albumin (BSA) nanoparticles coated with polysorbate- 80 (PS-80) and containing amphotericin B (AmB) were developed using a coacervation method.
The nanoparticles were spherical, had a uniform size distribution (polydispersity < 0.25), a small mean size (185 ± 5 nm), a high zeta potential (-38.0 ± 0.7 mV), and a high AmB encapsulation efficiency (93 ± 1%). The AmB release profile was prolonged and diffusion-controlled, resulting in a low degree of AmB aggregation in solution. The physicochemical characteristics of these AmB containing nanoparticles were evaluated by X-ray diffraction, Fourier transform infrared spectroscopy, differential scanning calorimetry, and derivative thermogravimetry and showed that the nanoencapsulation process lead to AmB amorphization while maintaining its chemical integrity.
In a hemolysis assay, AmB-loaded PS-80-coated BSA nanoparticles demonstrated an absence of cytotoxicity toward erythrocytes, whereas pure and commercial AmB were highly hemolytic.
In an assay to assess antifungal activity against Cryptococcus neoformans, AmB-charged PS-80-coated BSA nanoparticles were effective, however, due to the prolonged AmB release from the nanoparticles, the MIC was higher than for pure or commercial AmB. PS-80-coated BSA nanoparticles are potential carriers for the delivery of AmB for the treatment of Cryptococcus sp infections.
在本研究中，采用凝聚法制备了包覆聚山梨酯80（PS - 80）并含有两性霉素B（AmB）的牛血清白蛋白（BSA）纳米颗粒。
纳米颗粒呈球形，粒径分布均匀（多分散性<0.25），平均粒径小（185±5 nm），zeta电位高（-38.0±0.7 mV），AmB包封效率高（93±1%）。AmB的释放曲线呈延长的扩散控制型，导致溶液中AmB的聚集程度较低。通过X射线衍射、傅里叶变换红外光谱、差示扫描量热法和导数热重分析法对这些含AmB纳米颗粒的理化特性进行了评估，结果表明纳米包封过程导致AmB非晶化，同时保持其化学完整性。
在溶血试验中，负载AmB的PS - 80包覆的BSA纳米颗粒对红细胞无细胞毒性，而纯AmB和市售AmB具有高度溶血作用。
在评估对新型隐球菌抗真菌活性的试验中，带电荷的PS - 80包覆的BSA纳米颗粒有效，然而，由于纳米颗粒中AmB的释放延长，其最低抑菌浓度（MIC）高于纯AmB或市售AmB。PS - 80包覆的BSA纳米颗粒是用于递送AmB治疗隐球菌属感染的潜在载体。
