Absorption of ipratropium and L-carnitine into the pulmonary circulation of the ex-vivo rat lung is driven by passive processes rather than active uptake by OCT/OCTN transporters.

08:00 EDT 14th October 2015 | BioPortfolio

Summary of "Absorption of ipratropium and L-carnitine into the pulmonary circulation of the ex-vivo rat lung is driven by passive processes rather than active uptake by OCT/OCTN transporters."

The organic cation transporters OCT and OCTN have been reported to play a significant role in the cellular uptake of substrates within in vitro lung cells. However, no studies to date have investigated the effect of these transporters upon transepithelial absorption of substrates into the pulmonary circulation. We investigated the contribution of OCT and OCTN transporters to total pulmonary absorption of L-carnitine and the anti-muscarinic drug, ipratropium, across an intact isolated perfused rat lung (IPRL). The results obtained from the IPRL were contrasted with active transport in vitro using three human pulmonary cell lines and primary rat alveolar epithelial cells. Ex-vivo studies showed that OCT/OCTN transporters do not play a role in the overall pulmonary absorption of L-carnitine or ipratropium, as evidenced by the effect of chemical inhibition of these transporters upon pulmonary absorption. In contrast, in-vitro studies showed that OCT/OCTN transporters play a significant role in cellular accumulation of substrates with preferential uptake of ipratropium by OCTs, and of L-carnitine uptake by OCTNs. The results show that in-vitro uptake studies cannot be predictive of airway to blood absorption in-vivo. Nevertheless, localised submucosal pulmonary concentrations of inhaled drugs and their pulmonary pharmacodynamic profiles may be influenced by OCT/OCTN transport activity.


Journal Details

This article was published in the following journal.

Name: International journal of pharmaceutics
ISSN: 1873-3476


DeepDyve research library

PubMed Articles [13583 Associated PubMed Articles listed on BioPortfolio]

Safety and effectiveness of sodium colistimethate-loaded nanostructured lipid carriers (SCM-NLC) against P. aeruginosa: in vitro and in vivo studies following pulmonary and intramuscular administration.

The usefulness of nanotechnology to increase the bioavailability of drugs and decrease their toxicity may be a tool to deal with multiresistant P. aeruginosa (Mr-Pa) respiratory infections. We describ...

EXPRESS: Improvement of Lung Function and Pulmonary Hypertension After Pulmonary Aneurysm Repair: Case Series.

Grape seed proanthocyanidin inhibits monocrotaline-induced pulmonary arterial hypertension via attenuating inflammation: in vivo and in vitro studies.

Inflammation in pulmonary arterioles initiates and maintains pathological processes in pulmonary arterial hypertension (PAH), and inhibition of it attenuates PAH development. Grape seed proanthocyanid...

Phosphodiesterase-4 Inhibitor Roflumilast Attenuates Pulmonary Air Emboli-Induced Lung Injury.

Pulmonary air embolism (PAE)-induced acute lung injury (ALI) can be caused by massive air entry into the lung circulation. PAE can occur during diving, aviation, and some iatrogenic invasive procedure...

Hybrid Three-Dimensional Lung Tissue Cultures to Improve Ex Vivo Models of Chronic Obstructive Pulmonary Disease.

Continued reliance on preclinical animal models and traditional human cell culture experiments conducted on supraphysiologically stiff surfaces in two dimensions often limits the translation of cellul...

Clinical Trials [10399 Associated Clinical Trials listed on BioPortfolio]

Duration of Protective Effect From Inhaled Ipratropium Bromide on Methacholine Airway Hyperresponsiveness

Certain lung disease medications can influence diagnostic tests and research investigations. This study will investigate how long ipratropium bromide must be withheld before a methacholin...

Ipratropium Bromide in Peri-Operative COPD

This is a randomized, double-blind, placebo-controlled, parallel-group, multi-centre trial.The trial aims to evaluate efficacy of nebulized ipratropium bromide in Chinese peri-operative pa...

Protein Ingestion and Muscle Carnitine Uptake

The purpose of this study is to assess the effects of a protein-carbohydrate beverage on the absorption of an orally ingested bolus of L-carnitine, compared to flavoured water and carbohyd...

Study to Assess the Effect of Salbutamol and Ipratropium Bromide in Chronic Obstructive Pulmonary Disease (COPD) Patients

The objectives of this study are to assess the effect of salbutamol in comparison with ipratropium bromide on the geometry of central and peripheral airways and to correlate spirometric in...

The Effects of RPL554 on Top of Standard COPD Reliever Medications

This study evaluates the addition of RPL554 to standard reliever medications for chronic obstructive pulmonary disorder (COPD). All patients will receive the same six treatments in a rando...

Medical and Biotech [MESH] Definitions

A combined pharmaceutical preparation of Ipratropium Bromide and Albuterol Sulfate that is used to treat the symptoms of ASTHMA and CHRONIC OBSTRUCTIVE PULMONARY DISEASE.


Absence of air in the entire or part of a lung, such as an incompletely inflated neonate lung or a collapsed adult lung. Pulmonary atelectasis can be caused by airway obstruction, lung compression, fibrotic contraction, or other factors.

A diverse group of lung diseases that affect the lung parenchyma. They are characterized by an initial inflammation of PULMONARY ALVEOLI that extends to the interstitium and beyond leading to diffuse PULMONARY FIBROSIS. Interstitial lung diseases are classified by their etiology (known or unknown causes), and radiological-pathological features.

A condition associated with VENTRICULAR SEPTAL DEFECT and other congenital heart defects that allow the mixing of pulmonary and systemic circulation, increase blood flow into the lung, and subsequent responses to low oxygen in blood. This complex is characterized by progressive PULMONARY HYPERTENSION; HYPERTROPHY of the RIGHT VENTRICLE; CYANOSIS; and ERYTHROCYTOSIS.

Quick Search


DeepDyve research library

Relevant Topics

Pulmonary relating to or associated with the lungs eg Asthma, chronic bronchitis, emphysema, COPD, Cystic Fibrosis, Influenza,  Lung Cancer, Pneumonia, Pulmonary Arterial Hypertension, Sleep Disorders etc Follow and track Lung Cancer News ...

Drug Discovery
Clinical Approvals Clinical Trials Drug Approvals Drug Delivery Drug Discovery Generics Drugs Prescription Drugs In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which drugs are dis...

Searches Linking to this Article