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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Improved antifungal activity of itraconazole-loaded PEG/PLA nanoparticles
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Improved antifungal activity of itraconazole-loaded PEG/PLA nanoparticles

机译：改善伊曲康唑负载的PEG / PLA纳米颗粒的抗真菌活性

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Poly(ethylene glycol)/polylactic acid (PEG/PLA) nanoparticles (NPs) containing the hydrophobic antifungal itraconazole (ITZ) were developed to provide a controlled release pattern of ITZ as well as to improve its aqueous dispersibility and hence enhance its antifungal action. Two PEG/PLA copolymers (PEGylated PLA polymers) were used in this study; branched PEGylated polymer in which PEG was grafted on PLA backbone at 7% (mol/mol of lactic acid monomer), PEG7%-g-PLA, and multiblock copolymer of PLA and PEG, (PLA-PEG-PLA)n with nearly similar PEG insertion ratio and similar PEG chain length. ITZ-loaded PLA NPs were also prepared and included in this study as a control. ITZ-NPs were prepared from a 1:1 w/w blend of PLA and each PEGylated polymer either PEG7%-g-PLA or (PLA-PEG-PLA)n using an oil-in-water emulsion evaporation method. The NPs morphology, size and size distribution, zeta potential, loading efficiency, release profile and antifungal activity were characterized. All ITZ-NPs were nearly spherical with smooth surface and showed less aggregating tendency with a size range of 185-285 nm. All ITZ-NPs measured nearly neutral zeta potential values close to 0 mV. The % LE of ITZ was -94% for PEG7%-g-PLA NPs and -83% for (PLA-PEG-PLA)r? at 15.3% w/w theoretical loading. PEG/PLA NPs were stable over time regarding size and size distribution and % ITZ loading efficiency (% LE). ITZ release showed an initial burst followed by a gradual release profile for ITZ-NPs over 5 days. (PLA-PEG-PLA)n NPs exhibited faster release rates than PEG7%-g-PLA NPs particularly at the last 2 days. Differential scanning calorimetry and powder X-ray diffractometry data confirmed that ITZ exists in an amorphous state or a solid solution state into the NPs matrix. Fourier transform infrared revealed the possibility of chemical interaction between ITZ and the NPs matrix polymer indicating the successful entrapment of ITZ inside the particles. In haemolysis test, ITZ-NPs caused mild haemolysis over the concentration range (5-20 μg/mL) compared to free ITZ, indicating better safety profile of ITZ-NPs. ITZ-loaded PEG/PLA NPs inhibited fungal growth more efficiently than either free ITZ or ITZ-loaded PLA NPs. Our results suggest that PEG/PLA-ITZ could be used efficiently as a nanocarrier to improve the aqueous dispersibility of ITZ, control its release over time and, thereby, enhance its antifungal efficacy.
机译：开发了包含疏水性抗真菌伊曲康唑（ITZ）的聚（乙二醇）/聚乳酸（PEG / PLA）纳米颗粒（NPs），以提供ITZ的控释方式，并改善其水分散性，从而增强其抗真菌作用。在这项研究中使用了两种PEG / PLA共聚物（PEG化的PLA聚合物）。支化PEG化聚合物，其中PEG以7％（摩尔/摩尔乳酸单体）接枝在PLA骨架上，PEG7％-g-PLA，以及PLA和PEG的多嵌段共聚物（PLA-PEG-PLA）n几乎相似PEG插入率和相似的PEG链长。还准备了装载ITZ的PLA NP，并将其作为对照纳入本研究。使用水包油乳液蒸发法，从PLA和每种PEG化聚合物PEG7％-g-PLA或（PLA-PEG-PLA）n的1：1 w / w混合物中制备ITZ-NP。 NPs的形态，大小和大小分布，zeta电位，加载效率，释放概况和抗真菌活性进行了表征。所有ITZ-NP均接近球形，表面光滑，并且聚集趋势较小，尺寸范围为185-285 nm。所有ITZ-NP都测得接近0 mV的接近中性的Zeta电位值。对于PEG7％-g-PLA NPs，ITZ的％LE为-94％，对于（PLA-PEG-PLA）r为-83％。理论负载为15.3％w / w。 PEG / PLA NP在尺寸，尺寸分布和％ITZ装载效率（％LE）方面随时间稳定。 ITZ释放显示出初始爆发，随后是5天内ITZ-NP的逐渐释放曲线。 （PLA-PEG-PLA）n NPs的释放速率比PEG7％-g-PLA NPs快，尤其是在最后两天。差示扫描量热法和粉末X射线衍射法数据证实，ITZ以非晶态或固溶体状态存在于NPs基质中。傅里叶变换红外光谱揭示了ITZ与NPs基质聚合物之间发生化学相互作用的可能性，表明ITZ成功地被捕获在颗粒内部。在溶血试验中，与游离ITZ相比，ITZ-NP在浓度范围（5-20​​μg/ mL）内引起轻度溶血，表明ITZ-NP的安全性更高。负载ITZ的PEG / PLA NPs比游离ITZ或负载ITZ的PLA NPs更有效地抑制真菌生长。我们的结果表明，PEG / PLA-ITZ可以有效地用作纳米载体，以改善ITZ的水分散性，控制其随时间的释放，从而增强其抗真菌功效。

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