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MPEG-PCL Copolymeric Micelles for Encapsulation of Azithromycin

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Abstract

Macrolide antibiotics are lipophilic drugs with some limitations including low solubility, limited cellular permeation, patients discomfort, etc. With amphiphilic methoxy poly(ethylene glycol)-b-poly(ε-caprolactone) (MPEG-PCL) copolymer and azithromycin (AZT) as drug carrier and model drug, AZT-loaded micelles were prepared via thin-membrane hydration method in order to overcome these limitations. Encapsulation efficiency of AZT-loaded micelles was 94.40% with good storage stability for 28 days, and AZT’s water solubility was enhanced to 944 μg/mL. Fourier transform infrared spectrum and x-ray diffraction analysis indicated that AZT was enveloped into the micelles in amorphous form due to its interaction with the copolymer. AZT’s in vitro release from the AZT-loaded micelles demonstrated a slow and continuous behavior when compared with raw AZT. The release dynamics was accorded with Weibull equation, meaning that release amount of AZT lowered with time and was proportional to remaining amount of drug in the AZT-loaded micelles. Korsmeyer-Peppas fitting result suggested that drug release process was a classical Fickian diffusion-controlled manner. With Staphylococcus aureus as bacterial strain, antibacterial activity of the AZT-loaded micelles displayed was comparable with raw AZT. In conclusion, MPEG-PCL should be a promising carrier for macrolide antibiotic delivery in treatment of bacterial infections.

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Funding

This work is supported by the Natural Science Foundation of Shandong Province under grant number ZR2016BL15, and Science and Technology Project of University of Jinan under grant number XKY1732.

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Author notes

  1. Wenxiu Wei and Shida Li contributed equally to this work.

Authors and Affiliations

  1. School of Biological Science and Technology, University of Jinan, No. 336 West Road of Nanxinzhuang, Jinan, 250022, Shandong, People’s Republic of China

    Wenxiu Wei, Shida Li, Hongmei Xu, Feilong Zhou, Yi Wen, Zhimei Song & Runliang Feng

  2. School of Basic Medical Sciences, Dali University, Dali, 671000, Yunnan, People’s Republic of China

    Sijia Feng

Authors
  1. Wenxiu Wei
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  2. Shida Li
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  3. Hongmei Xu
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  4. Feilong Zhou
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  5. Yi Wen
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  6. Zhimei Song
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  7. Sijia Feng
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  8. Runliang Feng
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Correspondence to Runliang Feng.

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Wei, W., Li, S., Xu, H. et al. MPEG-PCL Copolymeric Micelles for Encapsulation of Azithromycin. AAPS PharmSciTech 19, 2041–2047 (2018). https://doi.org/10.1208/s12249-018-1009-0

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  • DOI: https://doi.org/10.1208/s12249-018-1009-0

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