Preparation and Determination of Drug-Polymer Interaction and In-vitro Release of Mefenamic Acid Microspheres Made of CelluloseAcetate Phthalate and/or Ethylcellulose Polymers

醋酸纤维素邻苯二甲酸酯和/或乙基纤维素聚合物制成的甲芬那酸微球的制备、药物-聚合物相互作用测定及体外释放

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作者:Mitra Jelvehgari, Davoud Hassanzadeh, Farhad Kiafar, Badir Delf Loveym, Sara Amiri

Abstract

The objective of this study was to formulate and evaluate the drug-polymer interaction of mefenamic acid (MA) using two polymers with different characteristics as ethylcellulose (EC) and/or cellulose acetate phthalate (CAP). Microspheres were prepared by the modified emulsion solvent evaporation (MESE). The effect of drug-polymer interaction was studied for each of microspheres. Important parameters in the evaluation of a microencapsulation technique are encapsulation efficiency, yield production, particle size, surface characteristics of microspheres, scanning electronic microscopy (SEM), powder X-ray diffraction analysis (XRD), and differential scanning calorimetry (DSC). The in-vitro release studies are performed in Tris buffer (pH 9) with Sodium lauryl sulfate (SLS). Microspheres containing CAP and EC showed 68-97% and 63-76% of entrapment efficiency, respectively. The thermogram X-ray and DSC showed stable character of MA in the microspheres and revealed an absence of drug polymer interaction. The prepared microspheres were spherical in shape and had a size range of 235-436 μm for CAP-microspheres and 358-442 μm for EC-microspheres. The results suggest that MA was successfully and efficiently encapsulated; the release rates of matrix microspheres are related to the type of polymer, only when polymers (EC and CAP combine with 1 : 1 ratio) were used to get prolonged drug release with reducing the polymers content in the microspheres. Data obtained from in-vitro release for microspheres and commercial capsule were fitted to various kinetic models and the high correlation was obtained in the peppas model. Mefenamic acid, Ethylcellulose, Cellulose acetate phthalate, Microparticles, Modified emulsion-solvent evaporation.

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