Solid lipid nanoparticles with enteric coating for improving stability, palatability, and oral bioavailability of enrofloxacin
| Autor: | Yanfei Tao, Lingli Huang, Yuanhu Pan, Kuiyu Meng, Kaixiang Zhou, Dongmei Chen, Shuyu Xie, Chao Li, Muhammad Abu Bakr Shabbir, Wei Xu, Qianying Liu |
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| Rok vydání: | 2019 |
| Předmět: |
Biophysics
Pharmaceutical Science Bioengineering 02 engineering and technology 010402 general chemistry 01 natural sciences Polyvinyl alcohol Biomaterials chemistry.chemical_compound Granulation Drug Discovery Solid lipid nanoparticle Zeta potential Enrofloxacin medicine Palatability Chromatography Chemistry Organic Chemistry General Medicine 021001 nanoscience & nanotechnology Enteric coating 0104 chemical sciences Bioavailability 0210 nano-technology medicine.drug |
| Zdroj: | International Journal of Nanomedicine. 14:1619-1631 |
| ISSN: | 1178-2013 |
| Popis: | Background The poor palatability, variable oral bioavailability, stimulation to gastric mucosa, and light instability limited the application of enrofloxacin (ENR). The enteric granules combining solid lipid nanoparticles (SLNs) with enteric coating were explored to overcome these disadvantages. Materials and methods ENR-loaded SLNs were produced by a hot homogenization and ultrasonic emulsification method and the enteric granules with SLNs as inner core were prepared by wet granulation followed by coating using polyacrylic resin II (PRII). The formulation was optimized by using orthogonal or single factor test screening. Results The optimal SLNs with loading capacity (LC) and price as inspection indexes were consisted of 10 mL 3% polyvinyl alcohol per 0.8 g ENR and 2.4 g octadecanoic acid. The sizes, LC, polydispersion index, and zeta potential of the SLNs were 308.5±6.3 nm, 15.73%±0.31%, 0.352±0.015, and -22.3 mv, respectively. The best enteric granules were used 15% PRII as coating materials. The release of the enteric granules in simulated intestine fluid (SIF, pH=8) was significantly faster than in simulated gastric fluid (SGF, pH=2) and simultaneously slower than those of SLNs and native ENR. The granules showed good stability in influencing factor experiment. The granules displayed a similar daily feed intake as the control group and higher daily feed intake than ENR powder and single-coating granules. Compared to the ENR soluble powder, the area under the plasma concentration-time curve and mean retention time of the enteric granules after intragastric administration were increased from 4.26±0.85 µg h/mL and 6.80±2.28 hours to 11.24±3.33 µg h/mL and 17.97±4.01 hours, respectively. Conclusion The enteric granules combination SLNs with enteric coating significantly improved the stability, palatability, sustained-release performance and oral bioavailability of ENR. The novel technology will be a potential measure to overcome the similar disadvantages of other drugs. |
| Databáze: | OpenAIRE |
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