Luppi Barbara, Bigucci Federica, Mercolini Laura, Musenga Alessandro, Sorrenti Milena, Catenacci Laura, Zecchi Vittorio
Department of Pharmaceutical Sciences, Bologna University, Bologna, Italy.
J Pharm Pharmacol. 2009 Feb;61(2):151-7. doi: 10.1211/jpp/61.02.0003.
The purpose of this study was the preparation and characterisation of mucoadhesive nasal inserts based on chitosan/hyaluronate polyelectrolyte complexes prepared at various pHs and at different molar ratios.
A suspension of chitosan/hyaluronate complexes with or without the model drugs (vancomycin or insulin) was lyophilised into small inserts. Complexation yield, FT-IR spectra and thermogravimetric analysis were used to study the degree of interactive strength between polyions. In-vitro swelling, mucoadhesion and release tests were performed in order to investigate delivery of vancomycin and insulin in the nasal cavity.
The results indicated that the selection of complex preparative conditions allows modulation of insert swelling and mucoadhesion ability. Nasal inserts containing vancomycin or insulin had showed completely different drug release behaviour.
Chitosan/hyaluronate polyelectrolyte complexes can be used for the formulation of mucoadhesive nasal inserts for the delivery of peptide and protein drugs.
本研究的目的是制备并表征基于壳聚糖/透明质酸盐聚电解质复合物的粘膜粘附性鼻腔插入剂,这些复合物在不同pH值和不同摩尔比下制备。
将含有或不含有模型药物(万古霉素或胰岛素)的壳聚糖/透明质酸盐复合物悬浮液冻干成小插入剂。采用络合产率、傅里叶变换红外光谱和热重分析来研究聚离子之间的相互作用强度。进行体外溶胀、粘膜粘附和释放试验,以研究万古霉素和胰岛素在鼻腔中的递送情况。
结果表明,复合物制备条件的选择可调节插入剂的溶胀和粘膜粘附能力。含有万古霉素或胰岛素的鼻腔插入剂表现出完全不同的药物释放行为。
壳聚糖/透明质酸盐聚电解质复合物可用于制备用于递送肽和蛋白质药物的粘膜粘附性鼻腔插入剂。