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Design and physicochemical characterization of advanced spray-dried tacrolimus multifunctional particles for inhalation.
Drug Des Devel Ther. 2013; 7:59-72.DD

Abstract

The aim of this study was to design, develop, and optimize respirable tacrolimus microparticles and nanoparticles and multifunctional tacrolimus lung surfactant mimic particles for targeted dry powder inhalation delivery as a pulmonary nanomedicine. Particles were rationally designed and produced at different pump rates by advanced spray-drying particle engineering design from organic solution in closed mode. In addition, multifunctional tacrolimus lung surfactant mimic dry powder particles were prepared by co-dissolving tacrolimus and lung surfactant mimic phospholipids in methanol, followed by advanced co-spray-drying particle engineering design technology in closed mode. The lung surfactant mimic phospholipids were 1,2-dipalmitoyl-sn-glycero-3-phosphocholine and 1,2-dipalmitoyl-sn-glycero-3-[phosphor-rac-1-glycerol]. Laser diffraction particle sizing indicated that the particle size distributions were suitable for pulmonary delivery, whereas scanning electron microscopy imaging indicated that these particles had both optimal particle morphology and surface morphology. Increasing the pump rate percent of tacrolimus solution resulted in a larger particle size. X-ray powder diffraction patterns and differential scanning calorimetry thermograms indicated that spray drying produced particles with higher amounts of amorphous phase. X-ray powder diffraction and differential scanning calorimetry also confirmed the preservation of the phospholipid bilayer structure in the solid state for all engineered respirable particles. Furthermore, it was observed in hot-stage micrographs that raw tacrolimus displayed a liquid crystal transition following the main phase transition, which is consistent with its interfacial properties. Water vapor uptake and lyotropic phase transitions in the solid state at varying levels of relative humidity were determined by gravimetric vapor sorption technique. Water content in the various powders was very low and well within the levels necessary for dry powder inhalation, as quantified by Karl Fisher coulometric titration. Conclusively, advanced spray-drying particle engineering design from organic solution in closed mode was successfully used to design and optimize solid-state particles in the respirable size range necessary for targeted pulmonary delivery, particularly for the deep lung. These particles were dry, stable, and had optimal properties for dry powder inhalation as a novel pulmonary nanomedicine.

Authors+Show Affiliations

University of Kentucky, College of Pharmacy, Department of Pharmaceutical Sciences-Drug Development Division, Lexington, KY 40536-0596 , USA.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

23403805

Citation

Wu, Xiao, et al. "Design and Physicochemical Characterization of Advanced Spray-dried Tacrolimus Multifunctional Particles for Inhalation." Drug Design, Development and Therapy, vol. 7, 2013, pp. 59-72.
Wu X, Hayes D, Zwischenberger JB, et al. Design and physicochemical characterization of advanced spray-dried tacrolimus multifunctional particles for inhalation. Drug Des Devel Ther. 2013;7:59-72.
Wu, X., Hayes, D., Zwischenberger, J. B., Kuhn, R. J., & Mansour, H. M. (2013). Design and physicochemical characterization of advanced spray-dried tacrolimus multifunctional particles for inhalation. Drug Design, Development and Therapy, 7, 59-72. https://doi.org/10.2147/DDDT.S40166
Wu X, et al. Design and Physicochemical Characterization of Advanced Spray-dried Tacrolimus Multifunctional Particles for Inhalation. Drug Des Devel Ther. 2013;7:59-72. PubMed PMID: 23403805.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Design and physicochemical characterization of advanced spray-dried tacrolimus multifunctional particles for inhalation. AU - Wu,Xiao, AU - Hayes,Don,Jr AU - Zwischenberger,Joseph B, AU - Kuhn,Robert J, AU - Mansour,Heidi M, Y1 - 2013/02/04/ PY - 2013/2/14/entrez PY - 2013/2/14/pubmed PY - 2013/6/14/medline KW - dry powder inhaler (DPI) KW - immunosuppression KW - lung surfactant KW - lung transplant KW - organic solution advanced spray drying KW - phospholipid colloidal self-assemblies KW - pulmonary nanomedicine KW - solid-state particle engineering design SP - 59 EP - 72 JF - Drug design, development and therapy JO - Drug Des Devel Ther VL - 7 N2 - The aim of this study was to design, develop, and optimize respirable tacrolimus microparticles and nanoparticles and multifunctional tacrolimus lung surfactant mimic particles for targeted dry powder inhalation delivery as a pulmonary nanomedicine. Particles were rationally designed and produced at different pump rates by advanced spray-drying particle engineering design from organic solution in closed mode. In addition, multifunctional tacrolimus lung surfactant mimic dry powder particles were prepared by co-dissolving tacrolimus and lung surfactant mimic phospholipids in methanol, followed by advanced co-spray-drying particle engineering design technology in closed mode. The lung surfactant mimic phospholipids were 1,2-dipalmitoyl-sn-glycero-3-phosphocholine and 1,2-dipalmitoyl-sn-glycero-3-[phosphor-rac-1-glycerol]. Laser diffraction particle sizing indicated that the particle size distributions were suitable for pulmonary delivery, whereas scanning electron microscopy imaging indicated that these particles had both optimal particle morphology and surface morphology. Increasing the pump rate percent of tacrolimus solution resulted in a larger particle size. X-ray powder diffraction patterns and differential scanning calorimetry thermograms indicated that spray drying produced particles with higher amounts of amorphous phase. X-ray powder diffraction and differential scanning calorimetry also confirmed the preservation of the phospholipid bilayer structure in the solid state for all engineered respirable particles. Furthermore, it was observed in hot-stage micrographs that raw tacrolimus displayed a liquid crystal transition following the main phase transition, which is consistent with its interfacial properties. Water vapor uptake and lyotropic phase transitions in the solid state at varying levels of relative humidity were determined by gravimetric vapor sorption technique. Water content in the various powders was very low and well within the levels necessary for dry powder inhalation, as quantified by Karl Fisher coulometric titration. Conclusively, advanced spray-drying particle engineering design from organic solution in closed mode was successfully used to design and optimize solid-state particles in the respirable size range necessary for targeted pulmonary delivery, particularly for the deep lung. These particles were dry, stable, and had optimal properties for dry powder inhalation as a novel pulmonary nanomedicine. SN - 1177-8881 UR - https://www.unboundmedicine.com/medline/citation/23403805/Design_and_physicochemical_characterization_of_advanced_spray_dried_tacrolimus_multifunctional_particles_for_inhalation_ L2 - https://dx.doi.org/10.2147/DDDT.S40166 DB - PRIME DP - Unbound Medicine ER -