Solid Lipid Nanoparticles as Formulative Strategy to Increase Oral Permeation of a Molecule Active in Multidrug-Resistant Tuberculosis Management
| Autor: | Elisabetta Gavini, Giovanna Rassu, Sandra Piras, Roberta Ibba, Paola Molicotti, Antonio Carta, Rossana Migheli, Elena Piera Porcu, Alessandro Dalpiaz, Antonella Obinu, Luca Ferraro, Paolo Giunchedi |
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| Rok vydání: | 2020 |
| Předmět: |
Antitubercular activity
Drug-resistant tuberculosis Gelucire@ Oral permeation Solid lipid nanoparticles Witepsol@ lcsh:RS1-441 Pharmaceutical Science antitubercular activity 02 engineering and technology Absorption (skin) Pharmacology 030226 pharmacology & pharmacy Intestinal absorption Article NO lcsh:Pharmacy and materia medica oral permeation 03 medical and health sciences 0302 clinical medicine Intestinal mucosa Oral administration Solid lipid nanoparticle Chemistry drug-resistant tuberculosis Permeation 021001 nanoscience & nanotechnology solid lipid nanoparticles Efflux Nanocarriers 0210 nano-technology |
| Zdroj: | Pharmaceutics Pharmaceutics, Vol 12, Iss 1132, p 1132 (2020) Volume 12 Issue 12 |
| ISSN: | 1999-4923 |
| Popis: | The role of mycobacterial efflux pumps in drug-resistant tuberculosis has been widely reported. Recently, a new compound, named SS13, has been synthesized, and its activity as a potential efflux inhibitor has been demonstrated. In this work, the chemical&ndash physical properties of the SS13 were investigated furthermore, a formulative study aimed to develop a formulation suitable for oral administration was performed. SS13 shows nonintrinsic antitubercular activity, but it increases the antitubercular activity of all the tested drugs on several strains. SS13 is insoluble in different simulated gastrointestinal media thus, its oral absorption could be limited. Solid lipid nanoparticles (SLNs) were, therefore, developed by using two different lipids, Witepsol and/or Gelucire. Nanoparticles, having a particle size (range of 200&ndash 450 nm with regards to the formulation composition) suitable for intestinal absorption, are able to load SS13 and to improve its permeation through the intestinal mucosa compared to the pure compound. The cytotoxicity is influenced by the concentration of nanoparticles administered. These promising results support the potential application of these nanocarriers for increasing the oral permeation of SS13 in multidrug-resistant tuberculosis management. |
| Databáze: | OpenAIRE |
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