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Rehydrated Lyophilized Rifampicin-Loaded mPEG–DSPE Formulations for Nebulization

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Abstract

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.

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Acknowledgment

The authors would like to thank Universiti Sains Malaysia, Penang, Malaysia, for providing the research grant to support this work.

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Authors and Affiliations

  1. Institute of Health, Sebha University, Sebha, Libya

    Juma Masoud Abdulla Abdulla

  2. School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800, Penang, Malaysia

    Yvonne Tze-Fung Tan & Yusrida Darwis

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  1. Juma Masoud Abdulla Abdulla
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  2. Yvonne Tze-Fung Tan
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  3. Yusrida Darwis
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Correspondence to Yusrida Darwis.

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Abdulla, J.M.A., Tan, Y.TF. & Darwis, Y. Rehydrated Lyophilized Rifampicin-Loaded mPEG–DSPE Formulations for Nebulization. AAPS PharmSciTech 11, 663–671 (2010). https://doi.org/10.1208/s12249-010-9428-6

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