Encapsulation of complementary model drugs in spray-dried nanostructured materials
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ORIGINAL PAPER
Encapsulation of complementary model drugs in spray-dried nanostructured materials Mohamed Fatnassi • Corine Tourne´-Pe´teilh • Pradial Peralta • Thomas Cacciaguerra • Philippe Dieudonne´ Jean-Marie Devoisselle • Bruno Alonso
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Received: 19 July 2013 / Accepted: 26 September 2013 / Published online: 2 October 2013 Springer Science+Business Media New York 2013
Abstract Two model drugs of different physico-chemical and pharmaceutical properties (ibuprofen, acetaminophen) have been incorporated together or separately in silicabased microspheres using sol–gel and spray-drying processes. A variable amount of a neutral surfactant Brij-56 has also been added. The properties of the microspheres vary significantly depending on their composition. Three kinds of texture are identified: (1) silica containing spheroid nano-domains (formed by ibuprofen; diameters between 20 and 100 nm), (2) silica containing worm-like mesophases (formed by Brij-56 and both model drugs, typical correlation distances *6 nm), (3) silica intimately mixed with the drug (acetaminophen) without visible phase-separation. The kinetics of drug release in simulated intestinal fluid strongly depend on these textures. The association of ibuprofen and acetaminophen in a single type of microsphere and without surfactant favours a concomitant release. Possible mechanisms of materials’ formation are discussed. Keywords Acetaminophen Ibuprofen Drug delivery systems Self-assembly Sol–gel materials Spray-drying
M. Fatnassi C. Tourne´-Pe´teilh P. Peralta T. Cacciaguerra J.-M. Devoisselle B. Alonso (&) Institut Charles Gerhardt de Montpellier, ICGM-MACS, UMR 5253 CNRS-ENSCM-UM2-UM1, 8 Rue de l’Ecole Normale, 34296 Montpellier Cedex 5, France e-mail: [email protected] P. Dieudonne´ Laboratoire Charles Coulomb, UMR 5221 CNRS-UM2, Universite´ Montpellier II, Place Euge`ne Bataillon, 34095 Montpellier Cedex 5, France
1 Introduction Many research efforts are devoted to the development of drug delivery systems (DDS) with optimised release properties to improve bio-disponibility according to the drug physico-chemical properties and/or the administration route. In the field of drug formulation, the spray-drying process receives a great interest in solid forms as a powerful one-step tool to generate pharmaceutical particles at the micro- to the nano-scale [1–3]. Spray-drying consists in atomizing precursors’ solutions into a spray of micro-sized droplets that possess a high surface-to-volume ratio favourable to fast solvent evaporation. The spray is dried inside a carrier gas, inducing the concentration of nonvolatile species and the solidification of the droplets. This process is low-cost and involves a limited number of preparation steps that are compatible with on-line continuous production. Some years ago, it was proposed to combine spraydying and sol–gel chemistry for DDS formulation [4]. More recently, we have proposed a synthesis procedure for the formation of DDS based on sol–gel, self-assembly and spray-drying processes
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