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

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• 作者：Zhimei Song ; Wenxia Zhu ; Fengying Yang ; Na Liu ; Runliang Feng
• 关键词：In vitro release ; Pharmacokinetic studies ; Curcumin ; Methoxy poly(ethylene glycol) ; block ; poly( $$\delta$$ δ ; valerolactone) ; Nanoparticles
• 刊名：Polymer Bulletin
• 出版年：2015
• 出版时间：January 2015
• 年：2015
• 卷：72
• 期：1
• 页码：75-91
• 全文大小：874 KB
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  14. Yin HT, Zhang DG, Wu XL,
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Chemistry
  Polymer Sciences
  Characterization and Evaluation Materials
  Soft Matter and Complex Fluids
  Physical Chemistry
  
• 出版者：Springer Berlin / Heidelberg
• ISSN：1436-2449

文摘

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.