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Inhalable Tacrolimus for Lung Transplant Patients to be a Reality Soon

Inhalable Tacrolimus for Lung Transplant Patients to be a Reality Soon

healthcare

Saksham Charan, Padmakshi Agarwal

Nov 17, 20223 min read

Transplant rejection can be prevented with the use of Tacrolimus and other medications. Tacrolimus belongs to a class of drugs known as immunosuppressants. According to Joshua Diamond, MD, Associate Medical Director of Penn Medicine's Lung Transplant Program, Tacrolimus is a primary calcineurin inhibitor that has been commonly prescribed to lung transplant recipients for more than 15 years now.

Tacrolimus is currently available for administration in two forms-intravenous and oral. Having tacrolimus orally, however, has a few setbacks including limited and erratic bioavailability; multiple drug interactions; and adverse effects such as nephrotoxicity, neurotoxicity, hypertension, and onset of diabetes mellitus.

Recently established pulmonary route of drug delivery addresses these issues and provides a more viable and safer route of administration. Pulmonary drug delivery introduces the drug in higher concentration within the lungs while reducing systemic adsorption, thereby resulting in a potentially lower incidence of adverse effects.

A team at the University of Texas, Austin headed by Sawittree Sahakijpijarn has developed a novel formulation of Tacrolimus for pulmonary route of administration employing thin film freezing (TFF). TFF is a particle engineering technology that can alter the physiochemical properties of a drug such as particle size, surface characteristics, morphology and crystallinity. According to previous studies Tacrolimus combined with 50% w/w lactose was found to be safe and effective for treatment of lung transplant rejection in rodent models. Sahakijpijarn et al therefore used the combination of tacrolimus and lactose along with the TFF technology to develop a lyophilized powder that can be delivered to the lung using both a nebulizer and a dry powder inhaler. A pilot study was then performed by the group in human subjects to determine the efficacy and safety of this formulation.

20 healthy volunteers were enrolled for the study. All the enrolled subjects were given a dose of the novel formulation comprising of 3 mg tacrolimus and 3 mg lactose through a nebulizer in stage 1 of the study. In stage 2, 10 out of the 20 enrolled subjects were randomly selected to take the drug of the same dosage through an inhaler.

Symptoms recorded over a 24-hour period included cough, abnormal taste, shortness of breath, abnormal throat sensations and chest discomfort, with abnormal taste being the most common symptom reported during both the stages of the study. A majority of subjects enrolled for stage 2 also reported cough as a common symptom, which patients who were nebulized did not experience. This study therefore demonstrated that both the nebulization of TFF-TAC-LAC colloidal dispersion and dry powder inhalation of TFF-TAC-LAC powder were well-tolerated and safe methods for targeted drug delivery to the lung.

According to this study, inhaled Tacrolimus has similar pharmacological effects in humans as it does in animal models. The inhalation route offers the opportunity of delivering an immunosuppressant directly to the target site. Therefore, inhaled tacrolimus should be considered as the preferred future therapeutic option for patients with lung conditions requiring immunosuppression.


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