Formulation of spray-dried phenytoin loaded poly(epsilon-caprolactone) microcarrier intended for brain delivery to treat epilepsy.
This study evaluates the efficacy of the spray-drying technique in the bioengineering of phenytoin (PHT) containing poly(epsilon-caprolactone) (PCL) microcarrier intended for brain delivery for long-term treatment of epilepsy. Through orthogonally designed experiments, the optimal formulation and process variables for the preparation of PCL-microcarriers containing PHT were obtained. The produced microcarriers were characterized by coulter counter, scanning electron, scanning transmission electron microscopies, differential scanning calorimetry, powder X-ray diffraction, and in vitro release. The results showed that the produced microcarriers have a spherical structure, uniform size distribution, and a particle mean diameter of about 4.0 microm, which is suitable for brain delivery. The PHT was loaded as dispersed microcrystals within the PCL-microcarriers. From this system, PHT was released slowly into a buffer solution for approximately 14 days without any burst effect. These data suggested that PHT containing spray-dried PCL-microcarrier may be a promising drug delivery system for local brain delivery and long-term treatment of pharmacoresistant epilepsy.
Li
Zhuzhu
Z
Division of Pharmaceutical Sciences, University of Missouri-Kansas City, 5005 Rockhill Road, Kansas City, Missouri 64110-2499, USA.
Li
Qingxiu
Q
Simon
Sindee
S
Guven
Necip
N
Borges
Karin
K
Youan
Bi-Botti C
BB
D000927:Anticonvulsants / Q000737:chemistry*; D001921:Brain / Q000378:metabolism*; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D018360:Crystallography, X-Ray; D003692:Delayed-Action Preparations; D003890:Desiccation; D004337:Drug Carriers; D004339:Drug Compounding; D045703:Emulsifying Agents / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D046529:Microscopy, Electron, Transmission; D008863:Microspheres; D008956:Models, Chemical; D010316:Particle Size; D010672:Phenytoin / Q000737:chemistry* / Q000378:metabolism; D011091:Polyesters / Q000737:chemistry*; D033362:Powder Diffraction; D011208:Powders; D012995:Solubility; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods*; D013997:Time Factors; D014867:Water / Q000737:chemistry
D000927:Anticonvulsants; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D045703:Emulsifying Agents; D011091:Polyesters; D011208:Powders; D014867:Water; C016240:polycaprolactone; D010672:Phenytoin