Matryoshka-type gastro-resistant microparticles for the oral treatment of Mycobacterium tuberculosis

Vanesa Andreu, Ane Larrea, Pablo Rodriguez-Fernandez, Salvador Alfaro, Begonã Gracia, Ainhoa Luciá, Laura Usón, Andromeda Celeste Gomez, Gracia Mendoza, Alicia Lacoma, Jose Dominguez, Cristina Prat, Victor Sebastian, José Antonio Ainsa, Manuel Arruebo

Research output: Contribution to journalArticleResearch

4 Citations (Scopus)

Abstract

© 2019 Future Medicine Ltd. Aim: Production of Matryoshka-type gastroresistant microparticles containing antibiotic-loaded poly lactic-co-glycolic acid (PLGA) nanoparticles (NP) against Mycobacterium tuberculosis. Materials & methods: The emulsification and evaporation methods were followed for the synthesis of PLGA-NPs and methacrylic acid-ethyl acrylate-based coatings to protect rifampicin from degradation under simulated gastric conditions. Results & conclusion: The inner antibiotic-loaded NPs here reported can be released under simulated intestinal conditions whereas their coating protects them from degradation under simulated gastric conditions. The encapsulation does not hinder the antituberculosis action of the encapsulated antibiotic rifampicin. A sustained antibiotic release could be obtained when using the drug-loaded encapsulated NPs. Compared with the administration of the free drug, a more effective elimination of M. tuberculosis was observed when applying the NPs against infected macrophages. The antibiotic-loaded PLGA-NPs were also able to cross an in vitro model of intestinal barrier. Matryoshka-type gastroresistant microparticles containing antibiotic-loaded poly lactic-co-glycolic acid nanoparticles against M. tuberculosis were produced to protect the antibiotic from degradation under simulated gastric conditions. The antibiotic-loaded poly lactic-co-glycolic acid nanoparticles were able to cross an in vitro model of intestinal barrier, being more effective in the elimination of M. tuberculosis when applied against infected macrophages compared with the use of the free drug. </inline-graphic.
Original languageEnglish
Pages (from-to)707-726
JournalNanomedicine
Volume14
DOIs
Publication statusPublished - 1 Mar 2019

Keywords

  • enteric coating
  • eudragit
  • gastroresistant
  • microparticles
  • Mycobacterium tuberculosis
  • oral delivery
  • PLGA
  • rifampicin
  • TEER
  • tuberculosis

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