Incorporation of drugs in an amorphous state into electrospun nanofibers composed of a water-insoluble, nonbiodegradable polymer.
Electrostatic spinning was applied to the preparation of drug-laden nonbiodegradable nanofiber for potential use in topical drug administration and wound healing. The specific aim of these studies was to assess whether these systems might be of interest as delivery systems for poorly water-soluble drugs. Itraconazole and ketanserin were selected as model compounds while a segmented polyurethane (PU) was selected as the nonbiodegradable polymer. For both itraconazole and ketanserin, an amorphous nanodispersion with PU was obtained when the drug/polymer solutions were electrospun from dimethylformide (DMF) and dimethylacetamide (DMAc), respectively. The collected nonwoven fabrics were shown to release the drugs at various rates and profiles based on the nanofiber morphology and drug content. Data were generated using a specially designed release apparatus based around a rotating cylinder. At low drug loading, itraconazole was released from the nanofibers as a linear function of the square root of time suggesting Fickian kinetics. No initial drug burst was observed. A biphasic release pattern was observed for ketanserin in which two sequential linear components were noted. These release phases may be temporally correlated with (1) drug diffusion through the polymer and (2) drug diffusion through formed aqueous pores.
Johnson & Johnson Pharmaceutical Research and Development, Pharmaceutical Sciences, Drug Evaluation, Turnhousteweg 30, 2340 Beerse, Belgium.
Geert
G
Verreck
Iksoo
I
Chun
Joel
J
Rosenblatt
Jef
J
Peeters
Alex Van
AV
Dijck
Jurgen
J
Mensch
Marc
M
Noppe
Marcus E
ME
Brewster
D002152:Calorimetry, Differential Scanning; D003692:Delayed-Action Preparations / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods*; D017964:Itraconazole / Q000008:administration & dosage / Q000493:pharmacokinetics; D007650:Ketanserin / Q000008:administration & dosage / Q000493:pharmacokinetics; D007700:Kinetics; D008855:Microscopy, Electron, Scanning; D015394:Molecular Structure; D036103:Nanotechnology / Q000379:methods*; D044367:Phase Transition; D011108:Polymers / Q000737:chemistry*; D011140:Polyurethanes / Q000737:chemistry*; D055672:Static Electricity
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D011108:Polymers; D011140:Polyurethanes; D017964:Itraconazole; D007650:Ketanserin