Sipos Bence, Katona Gábor, Szarvas Flóra Mária, Budai-Szűcs Mária, Ambrus Rita, Csóka Ildikó
Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös Street 6, H-6720 Szeged, Hungary.
Pharmaceuticals (Basel). 2023 Oct 12;16(10):1447. doi: 10.3390/ph16101447.
In this present formulation study, vinpocetine-loaded nano-spray-dried polymeric micelles were developed via nano-spray-drying. Three different mucoadhesive excipients were applied in the studies, namely chitosan, hyaluronic acid and hydroxypropyl methylcellulose. In all cases, the formulations had a proper particle size and drug content after drying with spherical morphology and amorphous structure. After rapid dissolution in water, the polymeric micelles had a particle size around 100-130 nm, in monodisperse size distribution. The high encapsulation efficiency (>80%) and high solubilization (approx. 300-fold increase in thermodynamic solubility) contributed to rapid drug release (>80% in the first 15 min) and fast passive diffusion at simulated nasal conditions. The formulated prototype preparations fulfilled the demands of a low-viscosity, moderately mucoadhesive nasal drug delivery system, which may be capable of increasing the overall bioavailability of drugs administered via the auspicious nasal drug delivery route.
在本制剂研究中，通过纳米喷雾干燥法制备了载有长春西汀的纳米喷雾干燥聚合物胶束。研究中使用了三种不同的粘膜粘附性辅料，即壳聚糖、透明质酸和羟丙基甲基纤维素。在所有情况下，干燥后的制剂均具有合适的粒径和药物含量，呈球形形态和无定形结构。在水中快速溶解后，聚合物胶束的粒径约为100 - 130 nm，粒径分布单分散。高包封率（>80%）和高增溶作用（热力学溶解度提高约300倍）促成了快速药物释放（前15分钟内>80%）以及在模拟鼻腔条件下的快速被动扩散。所制备的原型制剂满足了低粘度、适度粘膜粘附性鼻腔给药系统的要求，该系统可能能够提高通过理想的鼻腔给药途径给药的药物的整体生物利用度。
