2021
DOI: 10.3390/pharmaceutics13050717
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A Safety and Tolerability Study of Thin Film Freeze-Dried Tacrolimus for Local Pulmonary Drug Delivery in Human Subjects

Abstract: Due to the low and erratic bioavailability of oral tacrolimus (TAC), the long-term survival rate following lung transplantation remained low compared to other solid organs. TAC was reformulated and developed as inhaled formulations by thin film freezing (TFF). Previous studies reported that inhaled TAC combined with 50% w/w lactose (LAC) was safe and effective for the treatment of lung transplant rejection in rodent models. In this study, we aimed to investigate the safety and tolerability of TFF TAC-LAC in hu… Show more

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Cited by 7 publications
(4 citation statements)
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“…The variable ratios of TAC and lactose at 50:50 and 95:5 show similar performance if processed using the TFF technique. The dissolution characteristics of the TFF-processed TAC formulation show a similar release pattern [20]. The rate of dissolution was also increased after combining crystalline drugs with the amorphous formulation.…”
Section: Solubility and Dissolutionmentioning
confidence: 69%
See 1 more Smart Citation
“…The variable ratios of TAC and lactose at 50:50 and 95:5 show similar performance if processed using the TFF technique. The dissolution characteristics of the TFF-processed TAC formulation show a similar release pattern [20]. The rate of dissolution was also increased after combining crystalline drugs with the amorphous formulation.…”
Section: Solubility and Dissolutionmentioning
confidence: 69%
“…After 6 months of storage at 40 • C/75% RH and 25 • C/60% RH, the amorphous state was retained, and aerosol performance did not change significantly. The authors extended this study to understand the safety and tolerability of TAC-LAC as a dry powder and suspension form in healthy human subjects [20]. This study proved the safety and tolerability of healthy human volunteers after administration (3 mg/dose) of TAC-LAC formulations.…”
Section: Tff-processed Dpi For Tacrolimus Deliverymentioning
confidence: 74%
“…Drying of the frozen thin films by lyophilization generates powders often with desirable aerosol properties, due to their low-density, large specific surface area, and brittle matrix nature [17][18][19]. TFF technology has been used to prepare aerosolizable dry powders of small molecule drugs for pulmonary delivery, such as tacrolimus, remdesivir, voriconazole, and niclosamide [20][21][22][23][24][25].…”
Section: Introductionmentioning
confidence: 99%
“…Drying of the frozen thin films by lyophilization generates powders often with desirable aerosol properties, due to their low-density, large specific surface area, and brittle matrix nature [17-19]. TFF technology has been used to prepare aerosolizable dry powders of small molecule drugs for pulmonary delivery, such as tacrolimus, remdesivir, voriconazole, and niclosamide [20-25]. Recently, it has also been applied to large molecules such as monoclonal antibodies and enzymes and particulates such as liposomes and small interfering RNA-solid lipid nanoparticles [26-32].…”
Section: Introductionmentioning
confidence: 99%