Kumar Rishikesh, Sahoo Ganesh Chandra, Pandey Krishna, Das Vnr, Das Pradeep
Nanotechnology and Drug Discovery .
Drug Deliv. 2015 May;22(3):383-8. doi: 10.3109/10717544.2014.891271. Epub 2014 Mar 6.
Drug delivery systems are a promising technology to increase poor solubility and bioavailability of compounds. Therefore we have developed PLGA-PEG encapsulated amphotericin B nanoparticles (NPs) drug delivery technology to increase the solubility of amphotericin B and target the macrophage of infected tissues during visceral leishmaniasis. The structural characterization by transmission electron microscopy and dynamic light scattering revealed the nano-size of the particle (30-35 nanometers). Fourier transform infrared spectroscopy confirmed the PLGA-PEG encapsulation. The mean cytotoxic assay (0.0803 + 0.0253) of extracellular promastigote of PLGA-PEG encapsulated amphotericin B is significantly lower than that of amphotericin B (0.1134 + 0.0153) and inhibition of amastigotes in the splenic tissue was significantly more than with conventional amphotericin B (93.02 + 6.63 versus 74.42 +14.78). Amphotericin B encapsulated PLGA-PEG nanoparticles were found to be more effective than free amphotericin B in terms of therapeutic efficacy during in vitro and in vivo study.
药物递送系统是一种很有前景的技术,可提高化合物的低溶解度和生物利用度。因此,我们开发了聚乳酸-羟基乙酸共聚物-聚乙二醇(PLGA-PEG)包裹的两性霉素B纳米颗粒(NPs)药物递送技术,以提高两性霉素B的溶解度,并在治疗内脏利什曼病期间靶向感染组织的巨噬细胞。通过透射电子显微镜和动态光散射进行的结构表征揭示了颗粒的纳米尺寸(30-35纳米)。傅里叶变换红外光谱证实了PLGA-PEG的包裹。PLGA-PEG包裹的两性霉素B对细胞外前鞭毛体的平均细胞毒性测定结果(0.0803 ± 0.0253)显著低于两性霉素B(0.1134 ± 0.0153),并且对脾组织中无鞭毛体的抑制作用明显强于传统两性霉素B(93.02 ± 6.63对74.42 ± 14.78)。在体外和体内研究中,发现PLGA-PEG包裹的两性霉素B纳米颗粒在治疗效果方面比游离两性霉素B更有效。