A novel dense CO2 supercritical fluid technology for the development of microparticulate delivery systems containing ketoprofen |
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| Institution: | 1. Laboratory of Pharmaceutical Nanomaterials Science, Department of Materials Science and Engineering, Technion-Israel Institute of Technology, Technion City, Haifa, Israel;2. Institute of Nanobiotechnology, National Science Research Council (CONICET), Buenos Aires, Argentina;3. Department of Pharmaceutical Technology, Faculty of Pharmacy and Biochemistry, University of Buenos Aires, Buenos Aires, Argentina;4. Department of Basic and Applied Sciences, National University of the Chaco Austral, Pcia. R. Sáenz Peña, Chaco, Argentina;1. Nutrition Research Center, School of Nutrition and Food Sciences, Shiraz University of Medical Sciences, Shiraz, Iran;2. Department of Food Science and Technology, School of Agriculture, Shiraz University, Shiraz, Iran;3. Food and Markets Department, Natural Resources Institute, University of Greenwich, Medway, UK;4. Social Determinants of Health Research Center, Department of Public Health, School of Health, Birjand University of Medical Sciences, Birjand, Iran;5. Research Center for Traditional Medicine and History of Medicine, Department of Persian Medicine, School of Medicine, Shiraz University of Medical Sciences, Shiraz, Iran |
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| Abstract: | VarioSol® is an innovative, solvent-free technology able to produce microparticles exploiting near-critical CO2 properties as spraying and cooling agent. The aim of the present work was to evaluate the feasibility to produce in a single processing step by VarioSol® technology, oral ketoprofen-loaded microparticles with gastro-protective properties. The obtained products were powders composed of regular in shape and small in diameter microparticles, characterized by high drug content (40%) and good flow properties. Microparticles were composed by anionic lipids scarcely soluble at acidic pH, blended with gastro-resistant polymers of the methacrylate type. In vitro drug release results indicated that the drug was rapidly delivered from the microparticulate systems in phosphate buffer at pH 6.8, while in acidic medium, the microparticles were able to retard the drug release process but without reaching complete gastro-resistance.However, the results obtained in this study, although non optimal, are not far from the specifications required for gastro-resistant release products (i.e., no more than 10% drug released after 1 h at pH 1.0) according to EMA guidelines and represent a good starting point for future formulation development. |
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