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Preparation, characterization, in vitro release, and pharmacokinetic studies of curcumin-loaded mPEG–PVL nanoparticles

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Abstract

Curcumin shows several pharmacological activities with low toxicity, but its low water solubility limits its usage. To overcome these drawback, methoxy poly(ethylene glycol)-b-poly (\(\delta\)-valerolactone) was synthesized through ring-opening polymerization with mPEG and \(\delta\)-valerolactone as raw materials and hydrochloride ethyl ether as catalyst. The nanoparticles were developed by thin-film hydration and used as the delivery system for curcumin. The pharmacokinetics, in vitro release and safety of curcumin-loaded nanoparticles were evaluated. The results showed that nanoparticles had high drug-loading capacity (11.70 %) and entrapment efficiency (92.66 %). The water solubility of curcumin was increased to 1.851 mg/mL, which was approximately 1.73 × 105 times higher than that of free curcumin. The plasma AUC0–∞ and V z of curcumin-loaded nanoparticles were 3.60- and 4.56-fold higher than that of curcumin control solution, respectively. The CLz of curcumin-loaded nanoparticles was decreased by 3.60-fold. The MRT0–∞ changed from 0.284 to 4.657 h. Hemolysis test results revealed that the mPEG–PVL was safe for intravenous injection. These results clearly showed that the curcumin-loaded nanoparticles were suitable to be a delivery vehicle for curcumin.

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Acknowledgments

This work is supported by the Excellent Young and Middle-aged Scientist Award Fund of Shandong Province, China (BS2011CL006) and Scientific Research Fund of University of Jinan (XKY1208).

Conflict of interest

The authors report no conflicts of interest in this work.

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Authors and Affiliations

  1. Department of Pharmaceutical Engineering, School of Biological Science and Technology, University of Jinan, 336 Nanxinzhuang Xilu, Jinan, 250022, Shandong Province, People’s Republic of China

    Zhimei Song, Fengying Yang, Na Liu & Runliang Feng

  2. Department of Pharmaceutical Engineering, School of Medicine and Life Sciences, University of Jinan, 336 Nanxinzhuang Xilu, Jinan, 250022, Shandong Province, People’s Republic of China

    Wenxia Zhu

  3. Shandong Academy of Medical Sciences, 18877 Jingshi Road, Jinan, 250062, Shandong Province, People’s Republic of China

    Wenxia Zhu

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  1. Zhimei Song
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  4. Na Liu
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Correspondence to Runliang Feng.

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Song, Z., Zhu, W., Yang, F. et al. Preparation, characterization, in vitro release, and pharmacokinetic studies of curcumin-loaded mPEG–PVL nanoparticles. Polym. Bull. 72, 75–91 (2015). https://doi.org/10.1007/s00289-014-1260-9

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