Pharmacokinetics of liposomal aerosolized cyclosporine A for pulmonary immunosuppression

Ann Thorac Surg. 1999 Dec;68(6):2044-8. doi: 10.1016/s0003-4975(99)01183-2.

Abstract

Background: The results of pulmonary transplantation are compromised by acute and chronic rejection. We hypothesized that a liposomal form of aerosolized cyclosporine A (CsA) would be selectively deposited and concentrated in the lungs. The theoretical advantage of this therapy is selective pulmonary immunosuppression with prolonged utilization.

Methods: Eighteen dogs were endotracheally intubated; aerosolized liposomal CsA was administered for 15 min. CsA levels were measured in whole blood, lung, trachea, heart, kidney, liver, and spleen at various times after treatment.

Results: The lung rapidly absorbs aerosolized liposomal CsA; other organs have much lower concentrations. The retention of pulmonary CsA delivered by liposome aerosol is approximately 120 min in this model.

Conclusions: Aerosolized liposomal CsA is selectively deposited and concentrated in the lungs; other organs absorb less CsA.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aerosols
  • Animals
  • Chromatography, High Pressure Liquid
  • Cyclosporine / administration & dosage
  • Cyclosporine / pharmacokinetics*
  • Dogs
  • Drug Carriers
  • Immunosuppressive Agents / administration & dosage
  • Immunosuppressive Agents / pharmacokinetics*
  • Liposomes
  • Lung / chemistry
  • Lung Transplantation*
  • Particle Size
  • Tissue Distribution

Substances

  • Aerosols
  • Drug Carriers
  • Immunosuppressive Agents
  • Liposomes
  • Cyclosporine