RESUMO
Poorly water-soluble and unstable compounds are difficult to develop as drug products using conventional formulation techniques. The aim of the present study was to develop and evaluate a nanoformulation prepared by a hot high-pressure homogenization method, which was a scalable and solvent-free process. We successfully prepared stable nanodispersions to protect a labile antibiotic, erythromycin. The mean diameter of the dispersed droplets was approximately 150 nm, and size distribution was unimodal. Dispersion was physically stable at room temperature for over six months. Using erythromycin as a model compound, we studied its antimicrobial activity in vitro on Helicobacter pylori. Results showed that drug encapsulation improves API stability in an acidic environment and is conducive to a synergistic effect between the drug and the formulation.
Assuntos
Apoptose/efeitos dos fármacos , Preparações de Ação Retardada/administração & dosagem , Eritromicina/administração & dosagem , Helicobacter pylori/efeitos dos fármacos , Nanocápsulas/administração & dosagem , Nanocápsulas/química , Antibacterianos/administração & dosagem , Antibacterianos/química , Apoptose/fisiologia , Preparações de Ação Retardada/química , Difusão , Composição de Medicamentos/métodos , Estabilidade de Medicamentos , Emulsões/química , Eritromicina/química , Helicobacter pylori/citologia , Helicobacter pylori/fisiologia , Nanocápsulas/ultraestrutura , Tamanho da PartículaRESUMO
In the field of nanotechnologies, theranostic approaches and fixed-dose combination products require the development of innovative carriers able to co-encapsulate several entities of interest. This communication describes the preparation and characterization of lipid-based Janus compartmented nanoparticles. They were successfully prepared using a scalable process with pharmaceutically approved excipients. The analysis of the microscopic structure and supramolecular organization demonstrated the formation of two physico-chemically different compartments enabling the co-administration at once of both liposoluble and hydrosoluble active pharmaceutical ingredients.
Assuntos
Portadores de Fármacos/química , Excipientes/química , Lipídeos/química , Nanopartículas/químicaRESUMO
INTRODUCTION: The term Janus particles was used to describe particles that are the combination of two distinct sides with differences in chemical nature and/or polarity on each face. Due to the exponential growth of interest on multifunctional nanotechnologies, such anisotropic nanoparticles are promising tools in the field of drug delivery. AREAS COVERED: The main preparation processes and the materials used have been described first. Then a specific focus has been done on therapeutic and/or diagnostic applications of Janus particles. EXPERT OPINION: Janus particles are demonstrated as interesting objects with advanced properties that combine features and functionalities of different materials in one single unit. Due to their dual structure, Janus particles are promising candidates for a variety of high-quality applications dealing with drug delivery purposes. Still, the main challenges for the future lie in the development of the preparation of shape-controlled and nano-sized particles with large-scale production processes and approved pharmaceutical excipients.