Nano Spray Drying of Pharmaceuticals Dr. Cordin Arpagaus NTB Interstate University of Applied Sciences of Technology Buchs, Switzerland IDS’2018 – 21st International Drying Symposium València, Spain, 11-14 September 2018 Paper #7356 INSTITUTE FOR ENERGY SYSTEMS
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Nano Spray Drying of Pharmaceuticals · Introduction to nano spray drying technology Concept of nano spray drying & equipment components (e.g. nozzle, particle collector) Main process
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Nano Spray Drying of Pharmaceuticals
Dr. Cordin Arpagaus
NTB Interstate University of Applied Sciences of Technology Buchs, Switzerland
IDS’2018 – 21st International Drying Symposium València, Spain, 11-14 September 2018Paper #7356
dichloromethane (Beck-Broichsitter et al. 2012, Bege et al. 2013, Dahili et al. 2015, Dahili and Feczkó 2015, Draheim et al. 2015, Panda et al. 2014, Schafroth et al. 2012),
acetone (Beber et al. 2014, Beck-Broichsitter et al. 2015b, Draheim et al. 2015, Durli et al. 2014, Fontana et al. 2014, Gu et al. 2015, Li et al. 2010, Perecin et al. 2015),
ethanol (Baba and Nishida 2013, 2012, Bürki et al. 2011, Maged et al. 2017, Zellnitz et al. 2015a),
methanol (Basran 2017, Öztürk et al. 2017, 2015, Schmid 2011, Suryaprakash et al. 2014),
acetonitrile (Amsalem et al. 2017, Denora et al. 2016),
ethylacetate (Draheim et al. 2015) and mixtures thereof with water (Aquino et al. 2014, Dimer et al. 2015a, Kaewjan and Srichana 2016, Martena et al. 2012a, Schoubben et al. 2015, 2013a; Son et al., 2013b).
Applications of nano spray dried pharmaceuticals
The selection of the organic solvent is based on drugsolubilization and the encapsulating wall materials. Typical solvents applied are:
asthma (e.g. salbutamol, terbutaline, or fluticasone), inflammation (e.g. dexamethasone and azithromycin, or pain and fever reducer
indomethacin and nimesulide), cystic fibrosis (e.g. antibacterial dexketoprofen in Kollidon and Eudragit nanoparticles, or
azithromycin in leucine), diabetes (e.g. sitagliptin, vildagliptin, and metformin in mucoadhesive Carbopol and gelatin), pulmonary arterial hypertension (e.g. resveratrol in poly(caprolactone), or sildenafil in
PLGA), tuberculosis (e.g. capreomycin or pyrazinamide in L-leucine, or ethambutol mixed with
chitosan carrier particles), Alzheimer's and Parkinson's diseases (e.g. nanocrystals of calpain inhibitor steroids), breast cancer (e.g. simvastatin loaded PLGA particles), or lung cancer (e.g. methotrexate,
carboplatin in gelatine, or paclitaxel), bacterial infections (e.g. amoxicillin, ciprofloxacin, gatifloxacin, clarithromycin, or
levofloxacin), fungal infections (e.g. antifungal griseovulfin) ophthalmic disorders (e.g. calpain inhibitor nanocrystals or dirithromycin incorporated in
Kollidon), high blood pressure (e.g. nimodipine in PLGA or pure nicergoline nanoparticles), congestive heart failure and edema (e.g. diuretic furosemide).
It is a versatile technology with a wide range of applications.
Main application trends are in the areas of pulmonary drug delivery, nanotherapeutics, the encapsulation of nanoemulsions with poorly water-soluble active ingredients and the formulation of nanocrystals for a higher bioavailability.
Submicron particles formed with diluted solutions of 0.1 to 1% (w/v).
Encapsulation efficiencies of over 95%, adjustable drug loadings, stability, protection, dry powder form.
High yields enable an economical use of valuable drugs.
Literature on nano spray drying of pharmaceuticals
Arpagaus C., Collenberg A., Rütti D., Assadpour E., Jafari S.M.: Nano Spray Drying forEncapsulation of Pharmaceuticals, International Journal of Pharmaceutics, 2018, 546, 1–2, 194-214.
Arpagaus, C., John, Ph., Collenberg, A., Rütti, D.: Chapter 10: Nanocapsules formation bynano spray drying, in: Nanoencapsulation Technologies for the Food and NeutraceuticalIndustries, edited by Seid Mahdi Jafari, ISBN: 978-0-12-809426-5, London, ElsevierAcademic Press, 2017, 346-401.
Arpagaus C., Rütti D., Meuri M.: Chapter 17: Enhanced solubility of poorly soluble drugsvia spray drying, in: Drug delivery strategies for Poorly Water-Soluble Drugs, edited byDouroumis D. and Fahr A., ISBN: 978-0-470-71197-2, Chichester, West Sussex, John Wiley & Sons, 2012, 551-586.
Arpagaus C.: A Novel Laboratory-Scale Spray Dryer to Produce Nanoparticles, DryingTechnology, 2012, 30, 10, 1113-1121.