Pharmaceutical Research

, Volume 22, Issue 3, pp 347–355 | Cite as

Intravenous Hydrophobic Drug Delivery: A Porous Particle Formulation of Paclitaxel (AI-850)

  • Julie A. Straub
  • Donald E. Chickering
  • Jonathan C. Lovely
  • Huimin Zhang
  • Bhavdeep Shah
  • William R. Waud
  • Howard Bernstein
Research Papers

No Heading


To develop a rapidly dissolving porous particle formulation of paclitaxel without Cremophor EL that is appropriate for quick intravenous administration.


A rapidly dissolving porous particle formulation of paclitaxel (AI-850) was created using spray drying. AI-850 was compared to Taxol following intravenous administration in a rat pharmacokinetic study, a rat tissue distribution study, and a human xenograft mammary tumor (MDA-MB-435) model in nude mice.


The volume of distribution and clearance for paclitaxel following intravenous bolus administration of AI-850 were 7-fold and 4-fold greater, respectively, than following intravenous bolus administration of Taxol. There were no significant differences between AI-850 and Taxol in tissue concentrations and tissue area under the curve (AUC) for the tissues examined. Nude mice implanted with mammary tumors showed improved tolerance of AI-850, enabling higher administrable does of paclitaxel, which resulted in improved efficacy as compared to Taxol administered at its maximum tolerated dose (MTD).


The pharmacokinetic data indicate that paclitaxel in AI-850 has more rapid partitioning from the bloodstream into the tissue compartments than paclitaxel in Taxol. AI-850, administered as an intravenous injection, has been shown to have improved tolerance in rats and mice and improved efficacy in a tumor model in mice when compared to Taxol.

Key Words:

drug delivery hydrophobic drugs microparticles paclitaxel spray drying 


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Copyright information

© Springer Science+Business Media, Inc. 2005

Authors and Affiliations

  • Julie A. Straub
    • 1
  • Donald E. Chickering
    • 1
  • Jonathan C. Lovely
    • 1
  • Huimin Zhang
    • 1
  • Bhavdeep Shah
    • 1
  • William R. Waud
    • 2
  • Howard Bernstein
    • 1
  1. 1.TAcusphere, Inc.Watertown, Massachusetts
  2. 2.Southern Research InstituteBirmingham, Alabama

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