Enhanced Delivery of Immunosuppressive Drug Compositions for Pulmonary Delivery

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  • Robert Williams III, Ph.D. , College of Pharmacy
  • Prapasri Sinswat , College of Pharmacy
  • Keith Johnston, Ph.D. , Chemical Engineering
  • Jason McConville, Ph.D. , College of Pharmacy
  • Robert Talbert, Jr. , College of Pharmacy
  • Jay Peters, M.D. , University of Texas Health Science Center at San Antonio
  • True Rogers, Ph.D. , College of Pharmacy
  • Alan Watts , Drug Dynamics Institute - College of Pharmacy

Background/unmet need

Tacrolimus (TAC) is a potent macrolide immunosuppressant used in transplantation medicine to prevent organ rejection when cyclosporine therapy proves to be ineffective. The immunosuppressive activity of TAC is 10 to 100 times more potent than that of cyclosporine. This enhanced immunosuppressive activity of TAC is achieved without an increase in infection risk or malignancy. Additionally, it has been found that TAC has the ability to reverse ongoing rejection. Numerous studies have confirmed the effectiveness of TAC as primary therapy in a variety of solid organ transplants.

Despite the promise TAC holds as an immunosuppressive therapeutic in comparison to cyclosporine, erratic absorption from the gastrointestinal tract following oral administration has limited the clinical potential of TAC. The average oral bioavailability is approximately 25% in adult patients. The compositions of the present invention consist of porous aggregated small particles with high surface area and enhanced drug dissolution rates, enabling effective treatment of organ rejection due to improved drug bioavailability.

Invention Description

Inventors at UT Austin have developed a novel delivery means for TAC. It entails preparing nanoparticulate formulation of this immunosuppressant using biocompatible hydrophilic excipients for pulmonary administration. This composition produces inhalable nanoparticles that provide high, sustained levels of drug in the lungs, overcoming the poor oral bioavailability of TAC.


  • Enhanced efficacy in the treatment of organ rejection
  • Bypass hepatic first-pass effect for drugs which undergo extensive metabolism in oral formulations
  • Reduced total drug dose and thereby reducing non-target site toxicities

Market potential/applications

Companies currently manufacturing tacrolimus or other immunosuppressive drugs.

Development Stage

Lab/bench prototype

IP Status

  • 1 foreign patent application filed
  • 5 foreign patents issued
  • 1 U.S. patent application filed
  • 1 U.S. patent issued: 9,044,391