Utilize este identificador para referenciar este registo:
https://hdl.handle.net/1822/79599
Título: | Levofloxacin in nanostructured lipid carriers: preformulation and critical process parameters for a highly incorporated formulation |
Autor(es): | Araújo, Viviane Lucia Beraldo de Vicente, Ana Flávia Siqueira Lima, Marcelo van Vliet Umerska, Anita Souto, Eliana Maria Barbosa Tajber, Lidia Nascimento, Laura de Oliveira |
Palavras-chave: | Preformulation Design of experiments Levofloxacin Nanostructured lipid carrier Solid state Degradation |
Data: | 15-Out-2022 |
Editora: | Elsevier 1 |
Revista: | International Journal of Pharmaceutics |
Citação: | Araújo, Viviane; Vicente, Ana Flávia Siqueira; Lima, Marcelo van Vliet; Umerska, Anita; Souto, Eliana B.; Tajber, Lidia; Nascimento, Laura de Oliveira, Levofloxacin in nanostructured lipid carriers: preformulation and critical process parameters for a highly incorporated formulation. International Journal of Pharmaceutics, 626(122193), 2022 |
Resumo(s): | The first step of a successful nanoformulation development is preformulation studies, in which the best excipients, drug-excipient compatibility and interactions can be identified. During the formulation, the critical process parameters and their impact must be studied to establish the stable system with a high drug entrapment efficiency (EE). This work followed these steps to develop nanostructured lipid carriers (NLCs) to deliver the antibiotic levofloxacin (LV). The preformulation studies covered drug solubility in excipients and thorough characterization using thermal analysis, X-ray diffraction and spectroscopy. A design of experiment based on the process parameters identified nanoparticles with < 200 nm in size, polydispersity <=0.3, zeta potential -21 to -24 mV, high EE formulations (> 71%) and an acceptable level of LV degradation products (0.37-1.13%). To the best of our knowledge, this is the first time that a drug degradation is reported and studied in work on nanostructured lipids. LV impurities following the NLC production were detected, mainly levofloxacin N-oxide, a degradation product that has no antimicrobial activity and could interfere with LV quantification in spectrophotometric experiments. Also, the achievement of the highest EE in lipid nanoparticles than those described in the literature to date and the apparent protective action of NLC of entrapped-LV against degradation are important findings. |
Tipo: | Artigo |
Descrição: | Available online 13 September 2022 |
URI: | https://hdl.handle.net/1822/79599 |
DOI: | 10.1016/j.ijpharm.2022.122193 |
ISSN: | 0378-5173 |
Versão da editora: | http://www.elsevier.com/locate/issn/03785173 |
Arbitragem científica: | yes |
Acesso: | Acesso aberto |
Aparece nas coleções: | CEB - Publicações em Revistas/Séries Internacionais / Publications in International Journals/Series |
Ficheiros deste registo:
Ficheiro | Descrição | Tamanho | Formato | |
---|---|---|---|---|
document_55742_1.pdf | 973,73 kB | Adobe PDF | Ver/Abrir |