Accelerated fenofibrate release from spray-dried microparticles based on polymer blends |
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| Institution: | 1. University of Lille, College of Pharmacy, 3, rue du Professeur-Laguesse, 59006 Lille, France;2. INSERM U 1008, Controlled Drug Delivery Systems and Biomaterials, 3, rue du Professeur-Laguesse, 59006 Lille, France;3. University of Lille, Department of Physics, UMR CNRS 8024, 59655 Villeneuve-d’Ascq, France;4. University of Lille, School of dentistry, 1, place de Verdun, 59000 Lille, France;1. Macromolecules and Interfaces Institute, Department of Sustainable Biomaterials, College of Natural Resources and Environment, Virginia Tech, Blacksburg, Virginia 24061;2. Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, West Lafayette, Indiana 47907;1. Physicochemical and Preformulation, Applied Chemistry for Drug Discovery, Innovative Drug Discovery Research Laboratories, Shionogi & Company, Ltd., Toyonaka-shi, Osaka 561-0825, Japan;2. Laboratory of Formulation Design and Pharmaceutical Technology, Osaka University of Pharmaceutical Sciences, Takatsuki-shi, Osaka 569-1094, Japan;3. Oral Formulation Department, Formulation Development Center, CMC Development Laboratories, Shionogi & Company, Ltd., Amagasaki-shi, Hyogo 660-0813, Japan;1. Institute of Pharma Technology, University of Applied Sciences and Arts Northwestern Switzerland Muttenz 4132 Switzerland;2. Department of Pharmaceutical Sciences, University of Basel Basel 4056 Switzerland;3. Tillotts Pharma AG Rheinfelden 4310 Switzerland |
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| Abstract: | Fenofibrate-loaded microparticles based on PVP/Eudragit E or HPMC/Eudragit E blends were prepared by spray-drying. The composition of the systems (in particular the polymer/polymer blend ratio and the drug loading) was varied and the resulting key properties were determined (including drug release measurements in 0.1 M HCl, X-ray diffraction studies, solubility measurements and particle size analysis). For reasons of comparison, also the respective physical drug/polymer/polymer mixtures, microparticles based on binary drug/PVP and drug/HPMC blends, the fenofibrate powder as received and a commercially available drug product were investigated. Importantly, highly supersaturated fenofibrate solutions were created upon exposure of the different types of microparticles to the release medium, in contrast to any reference formulation. Also, the presence of co-dissolved Eudragit E led to a significant increase in fenofibrate solubility. At 10 % drug loading, all microparticles were amorphous and drug release stable during one month open storage. However, at 30 % loading, HPMC containing microparticles showed storage instability, due to drug re-crystallization. |
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