Bioavailability enhancement of a COX-2 inhibitor, BMS-347070, from a nanocrystalline dispersion prepared by spray-drying

Shawn X. Yin, Miriam Franchini, Jinling Chen, Alice Hsieh, Sandy Jen, Tu Lee, Munir Hussain, Ronald Smith

Research output: Contribution to journalArticlepeer-review

53 Scopus citations

Abstract

Spray drying drug with excipients is usually associated with the preparation of microcrystalline or amorphous drug in order to improve bioavailability. It was found that BMS-347070, when spray-dried with Pluronic F127 from acetone or methylene chloride, was dispersed as nanosized crystalline drug within the water-soluble Pluronic matrix. The reduction in drug particle/crystallite size, coupled with wetting by the Pluronic, resulted in a fast-onset formulation with bioavailability comparable to that of a solubilized and a NanoCrystal® formulation. For this system, it is theorized that the polyethylene oxide segments of Pluronic crystallize and that the polypropylene oxide segments remain amorphous, providing a size-restricted domain in which the COX-2 drug crystallizes. This results in improved bioavailability while limiting the potential risk of conversion of an amorphous drug to its crystalline state.

Original languageEnglish
Pages (from-to)1598-1607
Number of pages10
JournalJournal of Pharmaceutical Sciences
Volume94
Issue number7
DOIs
StatePublished - Jul 2005

Keywords

  • Bioavailability
  • COX-2
  • Nanocrystallite
  • Pluronic
  • Spray-drying

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