Partheniadis Ioannis, Zarafidou Evangelia, Litinas Konstantinos E, Nikolakakis Ioannis
Department of Pharmaceutical Technology, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
Laboratory of Organic Chemistry, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
Pharmaceutics. 2020 Jun 19;12(6):571. doi: 10.3390/pharmaceutics12060571.
Oregano essential oil (EO) enteric release powder was formulated by spray drying feed emulsions stabilized with polysaccharides (PSC) and Eudragit L100 (PLM). Different modified starches were used in the PSC component. Spray-dried powders were evaluated for particle size and morphology, dynamic packing, flowability, chemical interactions, reconstitution, and gastric protection. Feed emulsions were stable, indicating the good emulsification ability of the PLM/PSC combination. The presence of polymer in the encapsulating wall neutralized electrostatic charges indicating physical attraction, and FTIR spectra showed peaks of both PLM and PSC without significant shifting. Furthermore, the presence of polymer influenced spray drying, resulting in the elimination of surface cavities and the improvement of powder packing and flowability, which was best when the surface-active, low-viscosity sodium octenyl succinate starch was used (angle of repose 42°). When a PLM/PSC ratio of 80/20 was used in the encapsulating wall, the spray-dried product showed negligible re-emulsification and less than 15% release in pH 1.2 medium for 2 h, confirming gastric protection, whereas at pH 6.8, it provided complete re-emulsification and release. In conclusion, (1) polymer-PSC physical interaction promoted the formation of a smoother particle surface and product with improved technological properties, which is important for further processing, and (2) the gastro protective function of Eudragit L100 was not impaired due to the absence of significant chemical interactions.
牛至精油(EO)肠溶释放粉末是通过喷雾干燥用多糖(PSC)和丙烯酸树脂L100(PLM)稳定的进料乳液而制成的。在PSC组分中使用了不同的变性淀粉。对喷雾干燥粉末进行了粒度和形态、动态堆积、流动性、化学相互作用、复溶和胃保护等方面的评估。进料乳液稳定,表明PLM/PSC组合具有良好的乳化能力。包封壁中聚合物的存在中和了静电荷,表明存在物理吸引力,傅里叶变换红外光谱(FTIR)显示PLM和PSC的峰均无明显位移。此外,聚合物的存在影响了喷雾干燥,导致表面空洞消除,粉末堆积和流动性得到改善,当使用表面活性、低粘度的辛烯基琥珀酸淀粉钠时效果最佳(休止角为42°)。当包封壁中PLM/PSC比例为80/20时,喷雾干燥产品在pH 1.2介质中2小时的再乳化可忽略不计,释放率低于15%,证实了其胃保护作用,而在pH 6.8时,它能实现完全再乳化和释放。总之,(1)聚合物-PSC物理相互作用促进了形成更光滑的颗粒表面和具有改善工艺性能的产品,这对进一步加工很重要;(2)由于没有明显的化学相互作用,丙烯酸树脂L100的胃保护功能未受损。