Improvement of the antibacterial activity of daptomycin-loaded polymeric microparticles by Eudragit RL 100: an assessment by isothermal microcalorimetry

International Journal of Pharmaceutics
Inês Santos FerreiraAntónio J Almeida

Abstract

The aim of the present study was to develop novel daptomycin-loaded acrylic microparticles with improved release profiles and antibacterial activity against two clinically relevant methicillin-susceptible and methicillin-resistant Staphylococcus aureus strains (MSSA and MRSA, respectively). Daptomycin was encapsulated into poly(methyl methacrylate) (PMMA) and PMMA-Eudragit RL 100 (EUD) microparticles by a double emulsion-solvent evaporation method. For comparison purposes similar formulations were prepared with vancomycin. Particle morphology, size distribution, encapsulation efficiency, surface charge, physicochemical properties, in vitro release and biocompatibility were assessed. Particles exhibited a micrometer size and a spherical morphology. The addition of EUD to the formulation caused a shift in the surface charge of the particles from negative zeta potential values (100% PMMA formulations) to strongly positive. It also improved daptomycin encapsulation efficiency and release, whereas vancomycin encapsulation and release were strongly hindered. Plain and antibiotic-loaded particles presented comparable biocompatibility profiles. The antibacterial activity of the particles was assessed by isothermal microcalorimetry agai...Continue Reading

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Citations

Oct 9, 2015·Nanomedicine·Inês Santos-FerreiraAntónio J Almeida
Jun 9, 2015·Applied Microbiology and Biotechnology·Weijun KongXiaohe Xiao
Oct 5, 2016·Journal of Biomaterials Science. Polymer Edition·Zhenbao LiuDongming Peng
May 11, 2018·Journal of Orthopaedic Research : Official Publication of the Orthopaedic Research Society·Christen RavnAndrej Trampuz
Apr 13, 2021·Advanced Drug Delivery Reviews·Stine Egebro BirkLine Hagner Nielsen

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