Carrier characteristics influence the kinetics of passive drug loading into lipid nanoemulsions
| العنوان: | Carrier characteristics influence the kinetics of passive drug loading into lipid nanoemulsions |
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| المؤلفون: | Katrin Göke, Heike Bunjes |
| المصدر: | European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V. 126 |
| سنة النشر: | 2017 |
| مصطلحات موضوعية: | Materials science, Carrier system, Pharmaceutical Science, 02 engineering and technology, Thermal diffusivity, 030226 pharmacology & pharmacy, Micelle, 03 medical and health sciences, 0302 clinical medicine, Fenofibrate, Dissolution testing, Solubility, Particle Size, Dissolution, Triglycerides, Drug Carriers, Chromatography, General Medicine, 021001 nanoscience & nanotechnology, Lipids, Kinetics, Chemical engineering, Nanoparticles, Emulsions, Particle size, Nanocarriers, 0210 nano-technology, Biotechnology |
| الوصف: | Passive loading as a novel screening approach is a material-saving tool for the efficient selection of a suitable colloidal lipid carrier system for poorly water soluble drug candidates. This method comprises incubation of preformed carrier systems with drug powder and subsequent determination of the resulting drug load of the carrier particles after removal of excess drug. For reliable routine use and to obtain meaningful loading results, information on the kinetics of the process is required. Passive loading proceeds via a dissolution-diffusion-based mechanism, where drug surface area and drug water solubility are key parameters for fast passive loading. While the influence of the drug characteristics is mostly understood, the influence of the carrier characteristics remains unknown. The aim of this study was to examine how the lipid nanocarriers' characteristics, i.e. the type of lipid, the lipid content and the particle size, influence the kinetics of passive loading. Fenofibrate was used as model drug and the loading progress was analyzed by UV spectroscopy. The saturation solubility in the nanocarrier particles, i.e. the lipid type, did not influence the passive loading rate constant. Low lipid content in the nanocarrier and a small nanocarrier particle size both increased passive loading speed. Both variations increase the diffusivity of the nanocarrier particles, which is the primary cause for fast loading at these conditions: The quicker the carrier particles diffuse, the higher is the speed of passive loading. The influence of the diffusivity of the lipid nanocarriers and the effect of drug dissolution rate were included in an overall mechanistic model developed for similar processes (A. Balakrishnan, B.D. Rege, G.L. Amidon, J.E. Polli, Surfactant-mediated dissolution: contributions of solubility enhancement and relatively low micelle diffusivity, J. Pharm. Sci. 93 (2004) 2064-2075). The resulting mechanistic model gave a good estimate of the speed of passive loading in nanoemulsions. Whilst the drug's characteristics - apart from drug surface area - are basically fixed, the lipid nanocarriers can be customized to improve passive loading speed, e.g. by using small nanocarrier particles. The knowledge of the loading mechanism now allows the use of passive loading for the straightforward, material-saving selection of suitable lipid drug nanocarriers. |
| تدمد: | 1873-3441 2064-2075 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ac9dd09c7ea9704af1663e115507e14d https://pubmed.ncbi.nlm.nih.gov/28807819 |
| حقوق: | CLOSED |
| رقم الأكسشن: | edsair.doi.dedup.....ac9dd09c7ea9704af1663e115507e14d |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 18733441 20642075 |
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