Development and validation of sensitive LC-MS/MS assays for quantifi cation of HP- β -CD in human plasma and CSF

Hui Jiang, Rohini Sidhu, Hideji Fujiwara, Marc De Meulder, Ronald De Vries, Yong Gong, Mark Kao, Forbes D. Porter, Nicole M. Yanjanin, Nuria Carillo-Carasco, Xin Xu, Elizabeth Ottinger, Myra Woolery, Daniel S. Ory, Xuntian Jiang

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20 Scopus citations

Abstract

2-Hydroxypropyl- cyclodextrin (HP- -CD), a widely used excipient for drug formulation, has emerged as an investigational new drug for the treatment of Niemann- Pick type C1 (NPC1) disease, a neurodegenerative cholesterol storage disorder. Development of a sensitive quantitative LC-MS/MS assay to monitor the pharmacokinetics (PKs) of HP- CD required for clinical trials has been challenging owing to the dispersity of the HP- -CD. To support a phase 1 clinical trial for ICV delivery of HP- -CD in NPC1 patients, novel methods for quantification of HP- CD in human plasma and cerebrospinal fl uid (CSF) using LC-MS/ MS were developed and validated: a 2D-LC-in-source fragmentation-MS/MS (2D-LC-IF-MS/MS) assay and a reversed phase ultra performance LC-MS/MS (RP-UPLC-MS/ MS) assay. In both assays, protein precipitation and "dilute and shoot" procedures were used to process plasma and CSF, respectively. The assays were fully validated and in close agreement, and allowed determination of PK parameters for HP- CD. The LC-MS/MS methods are 100- fold more sensitive than the current HPLC assay, and were successfully employed to analyze HP- CD in human plasma and CSF samples to support the phase 1 clinical trial of HP- CD in NPC1 patients. -Jiang, H., R. Sidhu, H. Fujiwara, M. De Meulder, R. de Vries, Y. Gong, M. Kao, F. D. Porter, N. M. Yanjanin, N. Carillo-Carasco, X. Xu, E. Ottinger, M. Woolery, D. S. Ory, and X. Jiang. Development and validation of sensitive LC-MS/MS assays for quantifi cation of HP- CD in human plasma and CSF. J. Lipid Res. 2014. 55: 1537 - 1548 .

Original languageEnglish
Pages (from-to)1537-1548
Number of pages12
JournalJournal of lipid research
Volume55
Issue number7
DOIs
StatePublished - Jul 2014

Keywords

  • 2-hydroxypropyl- - -cyclodextrin
  • Cerebrospinal fl uid
  • In-source fragmentation
  • Liquid chromatography-tandem mass spectrometry
  • Niemann-Pick C
  • Two-dimensional liquid chromatography
  • Ultra performance liquid chromatography

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