| Autor: |
Carvalho Feitosa R; Faculty of Pharmaceutical Sciences, University of Campinas (UNICAMP), Campinas 13083-871, SP, Brazil., Souza Ribeiro Costa J; Faculty of Pharmaceutical Sciences, University of Campinas (UNICAMP), Campinas 13083-871, SP, Brazil., van Vliet Lima M; Faculty of Pharmaceutical Sciences, University of Campinas (UNICAMP), Campinas 13083-871, SP, Brazil., Sawa Akioka Ishikawa E; Faculty of Pharmaceutical Sciences, University of Campinas (UNICAMP), Campinas 13083-871, SP, Brazil., Cogo Müller K; Faculty of Pharmaceutical Sciences, University of Campinas (UNICAMP), Campinas 13083-871, SP, Brazil., Bonin Okasaki F; Department of Physical Chemistry, Institute of Chemistry, University of Campinas (UNICAMP), Campinas 13083-970, SP, Brazil., Sabadini E; Department of Physical Chemistry, Institute of Chemistry, University of Campinas (UNICAMP), Campinas 13083-970, SP, Brazil., Garnero C; Research and Pharmaceutical Technology Development Unit (UNITEFA, CONICET-UNC) and Department of Pharmacy, Faculty of Chemical Sciences, National University of Cordoba, Cordoba X5000HUA, Argentina., Longhi MR; Research and Pharmaceutical Technology Development Unit (UNITEFA, CONICET-UNC) and Department of Pharmacy, Faculty of Chemical Sciences, National University of Cordoba, Cordoba X5000HUA, Argentina., Lavayen V; Department of Inorganic Chemistry, Institute of Chemistry, Federal University of Rio Grande do Sul (UFRGS), Porto Alegre 91501-970, RS, Brazil., da Silva-Júnior AA; Laboratory of Pharmaceutical Technology and Biotechnology, Department of Pharmacy, Federal University of Rio Grande do Norte (UFRN), Natal 59012-570, RN, Brazil., Oliveira-Nascimento L; Faculty of Pharmaceutical Sciences, University of Campinas (UNICAMP), Campinas 13083-871, SP, Brazil. |
| Abstrakt: |
Doxycycline (DX) is a well-established and broad-spectrum antimicrobial drug. However, DX has drawbacks, such as physicochemical instability in aqueous media and bacterial resistance. The inclusion of drugs in cyclodextrin complexes and their loading into nanocarriers can overcome these limitations. Thus, we studied the DX/sulfobutylether-β-CD (SBE-β-CD) inclusion complex for the first time and used it to reticulate chitosan. The resulting particles were evaluated by their physicochemical characteristics and antibacterial activity. DX/SBE-β-CD complexes were characterized by nuclear magnetic resonance, infrared spectroscopy, thermal analysis, X-ray diffraction, and scanning electron microscopy (SEM), whereas DX-loaded nanoparticles were characterized by dynamic light scattering, SEM, and drug content. The partial inclusion of the DX molecule in CD happened in a 1:1 proportion and brought increased stability to solid DX upon thermal degradation. Chitosan-complex nanoparticles measured approximately 200 nm, with a narrow polydispersity and particles with sufficient drug encapsulation for microbiological studies. Both formulations preserved the antimicrobial activity of DX against Staphylococcus aureus, whereas DX/SBE-β-CD inclusion complexes were also active against Klebsiella pneumoniae , indicating the potential use of these formulations as drug delivery systems to treat local infections. |
