Development of an HPLC-FLD Method for Determination of Rhodamine-123 in Caco-2 Cell-Based Permeability Studies

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• 作者：Zhonglian Cao ; Xiaoxia Li ; Xueling Liao ; Ping Yang
• 关键词：P ; glycoprotein ; Inhibitor ; HPLC ; Caco ; 2
• 刊名：Chromatographia
• 出版年：2016
• 出版时间：February 2016
• 年：2016
• 卷：79
• 期：3-4
• 页码：261-266
• 全文大小：620 KB
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• 作者单位：Zhonglian Cao (1)
  Xiaoxia Li (2)
  Xueling Liao (1)
  Ping Yang (1)
  
  1. School of Pharmacy, Fudan University, No. 826 Zhangheng Road, Pudong, 201203, Shanghai, People’s Republic of China
  2. Children’s Hospital of Fudan University, Minhang, 201102, Shanghai, People’s Republic of China
  
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Chemistry
  Analytical Chemistry
  Organic Chemistry
  Pharmacy
  Biochemistry
  Plant Sciences
  Measurement Science and Instrumentation
  
• 出版者：Vieweg Verlag
• ISSN：1612-1112

文摘

P-glycoprotein (P-gp) overexpression and its efflux pump function have been associated with chemotherapy failure in many cancers. Many cytotoxic agents have been P-gp substrates. Thus, it was essential to develop a simple and validated method to determine the P-gp substrate in the presence of P-gp inhibitors. In this study, the HPLC-FLD method was developed combined with Caco-2 cell-based permeability studies. First, we developed the HPLC method to quantify Rhodamine-123 (Rho-123) in transport media. It was validated to be sensitive, precise, accurate, linear and specific. Then, the method was employed to determine the Rho-123 concentration in the presence or absence of two known P-gp inhibitors, verapamil and tetrandrine, in a Caco-2 transepithelial transport experiment. The results showed that the two P-gp inhibitors decreased the secretory and increased the absorptive transport of Rho-123. It illustrated that the HPLC-FLD method for determination of Rho-123 in the presence of two P-gp inhibitors in Caco-2 cell-based permeability studies was accurate and reliable. Keywords P-glycoprotein Inhibitor HPLC Caco-2