Formulation of spray-dried phenytoin loaded poly(epsilon-caprolactone) microcarrier intended for brain delivery to treat epilepsy.

Abstract

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.

• Authors: Zhuzhu Li, Qingxiu Li, Sindee Simon, Necip Guven, Karin Borges, Bi-Botti C Youan
• Journal: Journal of pharmaceutical sciences (J Pharm Sci) Vol. 96 Issue 5 Pg. 1018-30 (May 2007) ISSN: 0022-3549 [Print] United States
• PMID: 17455322 (Publication Type: Evaluation Study, Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: (c) 2007 Wiley-Liss, Inc. and the American Pharmacists Association.

Chemical References

• Anticonvulsants
• Delayed-Action Preparations
• Drug Carriers
• Emulsifying Agents
• Polyesters
• Powders
• Water
• polycaprolactone
• Phenytoin

Topics

• Anticonvulsants (chemistry)
• Brain (metabolism)
• Calorimetry, Differential Scanning
• Chemistry, Pharmaceutical
• Chromatography, High Pressure Liquid
• Crystallography, X-Ray
• Delayed-Action Preparations
• Desiccation
• Drug Carriers
• Drug Compounding
• Emulsifying Agents (chemistry)
• Microscopy, Electron, Scanning
• Microscopy, Electron, Transmission
• Microspheres
• Models, Chemical
• Particle Size
• Phenytoin (chemistry, metabolism)
• Polyesters (chemistry)
• Powder Diffraction
• Powders
• Solubility
• Surface Properties
• Technology, Pharmaceutical (methods)
• Time Factors
• Water (chemistry)