Bile acid conjugated chitosan oligosaccharide nanoparticles for paclitaxel carrier

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• 作者：Jun-kyu Park (1)
  Tae-Hun Kim (1)
  Joung-Pyo Nam (1)
  Seong Cheol Park (1)
  YungHoon Park (1)
  Mi-Kyeong Jang (1)
  Jae-Woon Nah (1)
  
• 关键词：paclitaxel ; bile acid ; chitosan oligosaccharide ; polymeric drug carrier
• 刊名：Macromolecular Research
• 出版年：2014
• 出版时间：March 2014
• 年：2014
• 卷：22
• 期：3
• 页码：310-317
• 全文大小：706 KB
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• 作者单位：Jun-kyu Park (1)
  Tae-Hun Kim (1)
  Joung-Pyo Nam (1)
  Seong Cheol Park (1)
  YungHoon Park (1)
  Mi-Kyeong Jang (1)
  Jae-Woon Nah (1)
  
  1. Department of Polymer Science and Engineering, Sunchon National University, Jeonnam, 540-742, Korea
  
• ISSN：2092-7673

文摘

To develop a paclitaxel carrier based on chitosan, chitosan oligosaccharide (COS) was chemically modified with bile acid (deoxycholic acid and lithocholic acid) as a hydrophobic group. Paclitaxel was loaded in bile acid conjugated chitosan oligosaccharide (CBs) nanoparticles by a dialysis method. We confirmed that the paclitaxel-loaded COS (CBs-Tx) nanoparticles could be successfully prepared with a yield of 80%-0% and paclitaxel encapsulation of 54%-0%. The size of CB nanoparticles was in the range of 200-00 nm, and it increased to 300-00 nm after paclitaxel loading with the narrow size distribution maintained. Paclitaxel-loaded CBs (CBs-Tx) nanoparticles showed remarkably high anticancer activity compared with paclitaxel in cremophore EL (CrEL)-ethanol against B16F10 cells. The antitumor efficacy in vivo was shown with significant inhibition of the tumor growth in both paclitaxel-treated groups. The effect on tumor size by the paclitaxel in the CrEL-ethanol formulation appeared to be slightly larger than that in CBs-Tx. The decrease in cytotoxicity and the increase in antitumor activity may lead to the improvement in the therapeutic index in clinical use compared to commercial paclitaxel. The efficacy of CBs-Tx nanoparticles suggests that bile acid as a hydrophobic group may have a potential application of effectively loading hydrophobic drugs such as paclitaxel.