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Sustained-release microparticle dry powders of chloramphenicol palmitate or thiamphenicol palmitate prodrugs for lung delivery as aerosols

Abstract : The purpose of this study was to design inhalable sustained-release nanoparticle-in-microparticles, i.e. nano-embedded microparticles, for the lung delivery of chloramphenicol or thiamphenicol as aerosols. The palmitate ester prodrugs of the two antibiotics were used to prepare PLGA-based nanoparticles or to form pure prodrug nanoparticles. Prodrug-loaded PLGA nanoparticles or pure prodrug nanoparticles were prepared using the emulsion-solvent evaporation method. Dry microparticle powders for inhalation were then produced by spray-drying the nanoparticle suspensions supplemented with lactose as a bulking agent and L-leucine as a dispersing enhancer. Examined under the scanning electron microscopy, the obtained microparticles appeared to be spherical and shriveled, with no crystal-like structures. Drug loading was satisfactory (14 to 34% (m/m)) and the aerodynamic properties determined with a Next Generation Impactor were appropriate for lung delivery, with mass median aerodynamic diameters close to 3 μm. The in vitro release profiles showed that sustained released was achieved with these formulations, with an almost complete release over 14 days.
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https://hal.archives-ouvertes.fr/hal-02477590
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Submitted on : Thursday, February 13, 2020 - 2:48:39 PM
Last modification on : Wednesday, October 27, 2021 - 6:15:10 AM

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Siti Nani Nurbaeti, Julien Brillault, Frédéric Tewes, Jean-Christophe Olivier. Sustained-release microparticle dry powders of chloramphenicol palmitate or thiamphenicol palmitate prodrugs for lung delivery as aerosols. European Journal of Pharmaceutical Sciences, Elsevier, 2019, 138, pp.105028. ⟨10.1016/j.ejps.2019.105028⟩. ⟨hal-02477590⟩

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