Pharmacokinetics of liposomal aerosolized cyclosporine A for pulmonary immunosuppression.
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.
Letsou
G V
GV
Department of Cardiothoracic and Vascular Surgery, University of Texas-Houston, 77030, USA.
Safi
H J
HJ
Reardon
M J
MJ
Ergenoglu
M
M
Li
Z
Z
Klonaris
C N
CN
Baldwin
J C
JC
Gilbert
B E
BE
Waldrep
J C
JC
D000336:Aerosols; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D016572:Cyclosporine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004285:Dogs; D004337:Drug Carriers; D007166:Immunosuppressive Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008081:Liposomes; D008168:Lung / Q000737:chemistry; D016040:Lung Transplantation; D010316:Particle Size; D014018:Tissue Distribution
D000336:Aerosols; D004337:Drug Carriers; D007166:Immunosuppressive Agents; D008081:Liposomes; D016572:Cyclosporine