The efficacy of inhaled nanoparticle tacrolimus in preventing rejection in an orthotopic rat lung transplant model

J Thorac Cardiovasc Surg. 2017 Dec;154(6):2144-2151.e1. doi: 10.1016/j.jtcvs.2017.07.083. Epub 2017 Sep 1.

Abstract

Objective: The immunosuppressive efficacy of inhaled nanoparticle tacrolimus was compared with systemic tacrolimus in a rodent allogeneic lung transplant model.

Methods: Sixteen rats underwent allogeneic left orthotopic lung transplantation and were divided into 3 treatment groups: (1) inhaled nanoparticle tacrolimus: 6.4 mg tacrolimus/6.4 mg lactose twice per day; (2) intramuscular tacrolimus: 1 mg/kg tacrolimus once per day; and (3) inhaled lactose: 6.4 mg of lactose twice per day. Five days after transplant, the rats were necropsied and underwent histologic rejection grading and cytokine analysis. Trough levels of tacrolimus were measured in allograft, blood, and kidney.

Results: Both intramuscular (n = 6) and nanoparticle tacrolimus (n = 6) rats displayed lower histologic grades of rejection (mean scores 3.4 ± 0.6 and 4.6 ± 0.9, respectively) when compared with lactose rats (n = 4) (mean score 11.38 ± 0.5, P = .07). Systemic tacrolimus trough levels (median) were lower in nanoparticle tacrolimus-treated rats versus intramuscular-treated rats (29.2 vs 118.6 ng/g; P < .001 in kidney, and 1.5 vs 4.8 ng/mL; P = .01 in blood).

Conclusions: Inhaled nanoparticle tacrolimus provided similar efficacy in preventing acute rejection when compared with systemic tacrolimus while maintaining lower systemic levels.

Keywords: cytokine profile in acute rejection; inhaled nanoparticle; modified pathology score for rejection in rats; orthotopic rat lung transplant; regional immunosuppression; tacrolimus.

Publication types

  • Comparative Study
  • Video-Audio Media

MeSH terms

  • Administration, Inhalation
  • Allografts
  • Animals
  • Calcineurin Inhibitors / administration & dosage*
  • Calcineurin Inhibitors / blood
  • Calcineurin Inhibitors / chemistry
  • Calcineurin Inhibitors / pharmacokinetics
  • Cytokines / blood
  • Disease Models, Animal
  • Drug Compounding
  • Graft Rejection / blood
  • Graft Rejection / immunology
  • Graft Rejection / prevention & control*
  • Immunosuppressive Agents / administration & dosage*
  • Immunosuppressive Agents / blood
  • Immunosuppressive Agents / chemistry
  • Immunosuppressive Agents / pharmacokinetics
  • Injections, Intramuscular
  • Lactose / chemistry
  • Lung Transplantation / adverse effects*
  • Male
  • Nanoparticles*
  • Rats, Inbred BN
  • Rats, Inbred Lew
  • Tacrolimus / administration & dosage*
  • Tacrolimus / blood
  • Tacrolimus / chemistry
  • Tacrolimus / pharmacokinetics

Substances

  • Calcineurin Inhibitors
  • Cytokines
  • Immunosuppressive Agents
  • Lactose
  • Tacrolimus