title: Comparison of electrospun and extruded Soluplus®-based solid dosage forms of improved dissolution.
abstract: Electrospinning (ES) and extrusion of a poorly water-soluble active pharmaceutical ingredient were used to improve its dissolution, which is a major challenge in the field of pharmaceutical technology. Spironolactone was applied as model drug and recently developed polyvinyl caprolactame-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®) was used as carrier matrix and solubilizer. ES of the polymer matrix from ethanol solution was optimized at first without spironolactone and then the cosolution of the drug and the carrier was used for forming electrospun fibers. It resulted in real solid solution due to its very efficient amorphization effect. On the contrary, a low amount of crystalline spironolactone appeared in the extrudates according to Raman microscopy, X-ray diffraction (XRD), scanning electron microscopy (SEM) and energy-dispersive spectrometry (EDS). Raman microspectrometry had the lowest detection limit of spironolactone crystals compared with XRD and differential scanning calorimetry. Both ES and extrusion techniques resulted in significantly improved dissolution. Electrospun ultrafine fibers increased the dissolution more effectively, owing to the formed solid solution and huge surface. The developed continuous technologies demonstrate great potential to tackle the challenge of inadequate dissolution of poorly water-soluble drugs in several cases.
authors.affiliation: Organic Chemistry and Technology Department, Budapest University of Technology and Economics, H-1111 Budapest, Hungary. nagyzsomborkristof@gmail.com
authors.forename: Zsombor K
authors.initials: ZK
authors.lastname: Nagy
authors.forename: Attila
authors.initials: A
authors.lastname: Balogh
authors.forename: Balázs
authors.initials: B
authors.lastname: Vajna
authors.forename: Attila
authors.initials: A
authors.lastname: Farkas
authors.forename: Gergo
authors.initials: G
authors.lastname: Patyi
authors.forename: Aron
authors.initials: A
authors.lastname: Kramarics
authors.forename: György
authors.initials: G
authors.lastname: Marosi
mesh_terms: D002152:Calorimetry, Differential Scanning / Q000379:methods; D002209:Caprolactam / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004304:Dosage Forms; D004337:Drug Carriers / Q000737:chemistry*; D000431:Ethanol / Q000737:chemistry; D008855:Microscopy, Electron, Scanning / Q000379:methods; D011092:Polyethylene Glycols / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry; D011145:Polyvinyls / Q000737:chemistry*; D012995:Solubility; D013059:Spectrum Analysis, Raman / Q000379:methods; D013148:Spironolactone / Q000737:chemistry*; D013678:Technology, Pharmaceutical / Q000379:methods*; D014867:Water / Q000737:chemistry; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D004304:Dosage Forms; D004337:Drug Carriers; D011108:Polymers; D011145:Polyvinyls; D014867:Water; D013148:Spironolactone; C013215:polyvinyl acetate; D000431:Ethanol; D011092:Polyethylene Glycols; D002209:Caprolactam