Departamento de Bioquímica, Instituto de Química, Universidade de São Paulo, CP 26077, CEP 05513-970, São Paulo, Brazil.
J Nanobiotechnology. 2008 May 7;6:6. doi: 10.1186/1477-3155-6-6.
Particulate systems are well known to be able to deliver drugs with high efficiency and fewer adverse side effects, possibly by endocytosis of the drug carriers. On the other hand, cationic compounds and assemblies exhibit a general antimicrobial action. In this work, cationic nanoparticles built from drug, cationic lipid and polyelectrolytes are shown to be excellent and active carriers of amphotericin B against C. albicans.
Assemblies of amphotericin B and cationic lipid at extreme drug to lipid molar ratios were wrapped by polyelectrolytes forming cationic nanoparticles of high colloid stability and fungicidal activity against Candida albicans. Experimental strategy involved dynamic light scattering for particle sizing, zeta-potential analysis, colloid stability, determination of AmB aggregation state by optical spectra and determination of activity against Candida albicans in vitro from cfu countings.
Novel and effective cationic particles delivered amphotericin B to C. albicans in vitro with optimal efficiency seldom achieved from drug, cationic lipid or cationic polyelectrolyte in separate. The multiple assembly of antibiotic, cationic lipid and cationic polyelctrolyte, consecutively nanostructured in each particle produced a strategical and effective attack against the fungus cells.
颗粒系统以能够高效地传递药物且副作用较少而闻名，这可能是通过药物载体的内吞作用实现的。另一方面，阳离子化合物和组装体表现出普遍的抗菌作用。在这项工作中，由药物、阳离子脂质和聚电解质构建的阳离子纳米颗粒被证明是两性霉素 B 对抗白色念珠菌的优良且有效的载体。
在极端的药物与脂质摩尔比下，两性霉素 B 和阳离子脂质的组装物被聚电解质包裹，形成具有高胶体稳定性和杀真菌活性的阳离子纳米颗粒，对白色念珠菌具有活性。实验策略涉及动态光散射进行粒径测定、zeta 电位分析、胶体稳定性、通过光学光谱测定 AmB 聚集状态以及从 cfus 计数测定体外抗白色念珠菌活性。
新型有效的阳离子颗粒以最优的效率将两性霉素 B 递送到体外的白色念珠菌中，而单独使用药物、阳离子脂质或阳离子聚电解质很少能达到这种效果。抗生素、阳离子脂质和阳离子聚电解质的多次组装，在每个颗粒中连续进行纳米结构，对真菌细胞进行了策略性和有效的攻击。
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