Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Preparation and Characterization of Tributyrin Sub-micron Emulsion as Carrier for Paclitaxel

  • Fei, Xiang (Department of Pharmaceutical Engineering, Woosuk University) ;
  • Xu, Wenting (Department of Pharmaceutical Engineering, Woosuk University) ;
  • Yue, Yuan (Department of Pharmaceutical Engineering, Woosuk University) ;
  • Lee, Mi-Kyung (College of Pharmacy, Woosuk University)
  • Received : 2011.08.04
  • Accepted : 2011.10.19
  • Published : 2011.10.20
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Abstract

Paclitaxel is a well known anticancer agent and has been a pharmaceutical challenge because of its extremely poor water-solubility and susceptibility to the p-glycoprotein (p-gp)-mediated efflux in multi-drug resistant (MDR) cancer cells. Tributyrin (TB), a triglyceride with relatively short fatty acid chains, was chosen as solubilizing vehicle for paclitaxel based on the solubility study (26.6 mg/mL). Tributyrin (10%) o/w emulsion containing paclitaxel (5%), egg phosphatidylcholine (5%) and pegylated phospholipid (0.5%) was prepared by high pressure homogenization to obtain submicron-sized emulsion. The mean particle size of the resultant TB emulsion was 395.5 nm. Paclitaxel in TB emulsion showed higher anticancer activity against human breast cancer cell line, MCF-7, than free form delivered in DMSO solution. On the other hand, its anticancer activity was significantly reduced in MCF-7/ADR, a MDR variant cancer cell line of MCF-7, and recovered by the presence of verapamil, suggesting of the susceptibility to the p-gp mediated efflux even though paclitaxel was encapsulated into emulsion. The TB emulsion showed great potential as a promising vehicle for water-insoluble anticancer agent, paclitaxel.

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References

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