文獻(xiàn)：Rehydrated Lyophilized Rifampicin-Loaded mPEG–DSPE Formulations for Nebulization

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

文獻(xiàn)鏈接：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.

使用兩種不同分子量的聚環(huán)氧乙烷嵌段二硬脂酰磷脂酰乙醇胺（mPEG2000-DSPE和mPEG5000-DSPE）聚合物制備負(fù)載利福平的納米顆粒。所有研究制劑的粒徑在162-395 nm范圍內(nèi)。

包封率（EE）不受共聚物分子量的影響，當(dāng)藥物與共聚物的比例為1:5時，獲得了最高的EE（100%）。差示掃描量熱法（DSC）熱圖顯示，負(fù)載利福平的PEG-DSPE納米顆粒的Tg降至較低值，表明利福平包埋在聚合物基質(zhì)中。傅里葉變換紅外光譜顯示，藥物與兩種共聚物之間沒有化學(xué)相互作用。

制劑的體外藥物釋放發(fā)生在3天內(nèi)，遵循一級釋放動力學(xué)和Higuchi擴(kuò)散模型。再水化凍干利福平mPEG-DSPE制劑的霧化質(zhì)量中值氣動直徑為2.6μm，細(xì)顆粒分?jǐn)?shù)為42%。制劑的空氣動力學(xué)特性不受共聚物分子量的影響。因此，建議mPEG-DSPE都是作為利福平肺部給藥載體的有前景的候選者。

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