Preparation and characterization of genistein containing poly(ethylene glycol) microparticles

Authors

  • Nusrat Motlekar,

    1. Department of Pharmaceutical Sciences, School of Pharmacy, Texas Tech University Health Sciences Center, Amarillo, Texas
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  • Mansoor A. Khan,

    1. Division of Product Quality Research, Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, Maryland
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  • Bi-Botti C. Youan

    Corresponding author
    1. Department of Pharmaceutical Sciences, School of Pharmacy, Texas Tech University Health Sciences Center, Amarillo, Texas
    • Department of Pharmaceutical Sciences, School of Pharmacy, Texas Tech University Health Sciences Center, Amarillo, Texas
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Abstract

The purpose of this study was to prepare, characterize, and evaluate genistein-containing microparticles with enhanced dissolution profile using poly(ethylene glycol) (PEG) as polymer matrix. Genistein loaded microparticles were prepared by a solvent evaporation process and their surface, thermal, chemical, and dissolution properties were analyzed by microscopy, differential scanning calorimetry, ATR-FTIR spectroscopy, and USP dissolution apparatus II, respectively. The wettability index was also determined. Genistein exhibited an elongated crystal habit. However, the drug containing PEG microparticles were discrete and quasispherical. The ATR-FTIR studies performed on the formulation suggested hydrogen bonding between the drug and the polymer matrix. Thermal analysis indicated a conversion of the crystalline form of the drug to an amorphous form. Genistein, exhibiting low solubility and high permeability, is a Class II drug of the Biopharmaceutical Classification Scheme. However, there was a ∼9-fold increase in the rate of dissolution of genistein in the case of all formulations as compared to native genistein. This study showed that genistein could be effectively encapsulated into PEG microparticles using an emulsion-solvent evaporation technique, therefore avoiding the potential disadvantages of other solid dispersion techniques. This approach provided a significant enhancement in the drug dissolution profile. © 2006 Wiley Periodicals, Inc. J Appl Polym Sci 101: 2070–2078, 2006

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