文献：Rehydrated Lyophilized Rifampicin-Loaded mPEG–DSPE Formulations for Nebulization

作者：Juma Masoud Abdulla Abdulla, Yvonne Tze-Fung Tan & Yusrida Darwis

文献链接：https://link.springer.com/article/10.1208/s12249-010-9428-6

摘要：

Rifampicin-loaded nanoparticles were prepared using two different molecular weights of poly-(ethylene oxide)-block-distearoyl phosphatidyl-ethanolamine (mPEG2000–DSPE and mPEG5000–DSPE) polymers. Particle sizes of all formulations studied were in the range of 162–395 nm. The entrapment efficiency (EE) was not affected by the copolymer’s molecular weight, and the highest EE (100%) was obtained with drug to copolymer ratio of 1:5. The differential scanning calorimetry (DSC) thermograms showed Tg of rifampicin-loaded PEG–DSPE nanoparticles that shifted to a lower value, indicating entrapment of rifampicin in polymer matrix. The Fourier transformed infrared spectra revealed no chemical interactions between the drug and both copolymers. The in vitro drug release from the formulations occurred over 3 days and followed first-order release kinetic and Higuchi diffusion model. The nebulization of rehydrated lyophilized rifampicin mPEG–DSPE formulations had mass median aerodynamic diameter of 2.6 µm and fine particle fraction of 42%. The aerodynamic characteristic of the preparations was not influenced by the molecular weight of the copolymers. Therefore, it is suggested that both mPEG–DSPE are promising candidates as rifampicin carrier for pulmonary delivery.

使用两种不同分子量的聚环氧乙烷嵌段二硬脂酰磷脂酰乙醇胺（mPEG2000-DSPE和mPEG5000-DSPE）聚合物制备负载利福平的纳米颗粒。所有研究制剂的粒径在162-395 nm范围内。

包封率（EE）不受共聚物分子量的影响，当药物与共聚物的比例为1:5时，获得了最高的EE（100%）。差示扫描量热法（DSC）热图显示，负载利福平的PEG-DSPE纳米颗粒的Tg降至较低值，表明利福平包埋在聚合物基质中。傅里叶变换红外光谱显示，药物与两种共聚物之间没有化学相互作用。

制剂的体外药物释放发生在3天内，遵循一级释放动力学和Higuchi扩散模型。再水化冻干利福平mPEG-DSPE制剂的雾化质量中值气动直径为2.6µm，细颗粒分数为42%。制剂的空气动力学特性不受共聚物分子量的影响。因此，建议mPEG-DSPE都是作为利福平肺部给药载体的有前景的候选者。

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