Linked Life Data

19782740

Source:http://linkedlifedata.com/resource/pubmed/id/19782740

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1-2
pubmed:dateCreated
2009-12-2
pubmed:abstractText
Lung transplantation animal models have been well established and enabled the investigation of a variety of new pharmacotherapeutic strategies for prevention of lung allograft rejection. Direct administration of immunosuppressive agents to the lung is a commonly investigated approach; however, can prove challenging due to the poor solubility of the drug molecule, the tortuous pathways of the lung periphery, and the limited number of excipients approved for inhalation. In this study, we aimed to evaluate a solubility enhancing formulation of tacrolimus for localized therapy in a lung transplanted rat model and determine the extent of drug absorption into systemic circulation. Characterization of the nebulized tacrolimus dispersion for nebulization showed a fine particle fraction (FPF) of 46.1% and a mass median aerodynamic diameter (MMAD) of 4.06 microm. After single dose administration to transplanted and non-transplanted rats, a mean peak transplanted lung concentration of 399.8+/-29.2 ng/g and mean peak blood concentration of 4.88+/-1.6 ng/mL were achieved. It is theorized that enhanced lung retention of tacrolimus is due to lipophilic associations with bronchial tissue and phospholipid surfactants in lung fluid. These findings indicate that tacrolimus dispersion for nebulization can achieve highly localized therapy for lung transplant recipients.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
1873-3476
pubmed:author
pubmed:issnType
Electronic
pubmed:day
15
pubmed:volume
384
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
46-52
pubmed:meshHeading
pubmed:year
2010
pubmed:articleTitle
Characterization and pharmacokinetic analysis of tacrolimus dispersion for nebulization in a lung transplanted rodent model.
pubmed:affiliation
The University of Texas at Austin, College of Pharmacy, 1 University Station A1920, Austin, TX 78712, USA.
pubmed:publicationType
Journal Article, Comparative Study