University of Zagreb, Faculty of Pharmacy and Biochemistry, Zagreb, Croatia.
University of Split, Faculty of Science, Split, Croatia.
Eur J Pharm Biopharm. 2022 Jun;175:27-42. doi: 10.1016/j.ejpb.2022.04.009. Epub 2022 Apr 27.
In this work we present the development of in situ gelling nanosuspension as advanced form for fluticasone propionate nasal delivery. Drug nanocrystals were prepared by wet milling technique. Incorporation of drug nanocrystals into polymeric in situ gelling system with pectin and sodium hyaluronate as constitutive polymers was fine-tuned attaining appropriate formulation surface tension, viscosity and gelling ability. Drug nanonisation improved the release profile and enhanced formulation mucoadhesive properties. QbD approach combining formulation and administration parameters resulted in optimised nasal deposition profile, with 51.8% of the dose deposited in the middle meatus, the critical region in the treatment of rhinosinusitis and nasal polyposis. Results obtained in biocompatibility and physico-chemical stability studies confirmed the leading formulation potential for safe and efficient nasal corticosteroid delivery.
在这项工作中，我们提出了原位凝胶纳米混悬液作为丙酸氟替卡松鼻腔给药的先进形式。药物纳米晶通过湿磨技术制备。将药物纳米晶掺入由果胶和透明质酸钠作为组成聚合物的聚合物原位凝胶体系中，精细调整以获得适当的制剂表面张力、粘度和胶凝能力。药物纳米化改善了释放曲线，并增强了制剂的粘膜粘附特性。结合制剂和给药参数的 QbD 方法优化了鼻腔沉积分布，其中 51.8%的剂量沉积在中鼻甲，这是治疗鼻窦炎和鼻息肉的关键区域。在生物相容性和物理化学稳定性研究中获得的结果证实了该制剂具有安全有效地鼻腔皮质激素传递的潜力。
