Physicomechanical Properties of Naproxen-Loaded Microparticles Prepared from Eudragit L100 |
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Authors: | M Maghsoodi |
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Institution: | (1) Drug Applied Research Center and School of Pharmacy, Tabriz University of Medical Sciences, Tabriz, 51664, Iran |
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Abstract: | Microparticles of naproxen with Eudragit L100 and Aerosil were prepared by the emulsion solvent diffusion method in order
to avoid local gastrointestinal irritation, one of the major side effects of nonsteroidal anti-inflammatory drugs after oral
ingestion. The process of preparation involved the use of ethanol as good solvent, dichloromethane as a bridging liquid, water
as poor solvent, Aerosil as anti-adhesion agent, and sodium dodecyl sulfate to aid in the dispersion of the drug and excipients
into the poor solvent. The obtained microparticles were evaluated for micromeritic properties, yield, encapsulation efficiency,
drug physical state, and drug release properties. The influence of formulation factors and preparation condition (polymer/naproxen
ratio, Aerosil/polymer ratio, and the initial difference of temperature between the solvent and nonsolvent) on the properties
of the microparticles were also examined. The resultant microparticles were finely spherical and uniform with high incorporation
efficiency (>79%) and yield (>71%). The incorporation efficiency was enhanced with increasing the ratio of excipients to drug
and the initial difference of temperature between the solvent and nonsolvent. The mean diameter of the microparticles was
influenced by all of the manufacturing parameters. Studies carried out to characterize the micromeritic properties of formulations,
such as flowability and packability, showed that microparticles were suitable for further pharmaceutical manipulation (e.g.,
capsule filling). Drug release studies of the microparticles confirmed the gastroresistance, and mathematical studies showed
that the drug released followed a Hixon and Crowell kinetic. These microparticles represent a simple method for the preparation
of drug-loaded enteric microparticles with desired micromeritic properties and gastroresistance release. |
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Keywords: | emulsion solvent diffusion method Eudragit L100 naproxen |
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