Abstract

Aim

The present work aimed to improve the bioavailability of terbutaline sulphate (TS) and to prolong its nasal residence time for the treatment of asthma.

Methods

Chitosan/pectin polyelectrolyte complex nanoparticles (CS/PC) were prepared by ionic gelation method and coated with phospholipid (PL) and then incorporated into optimised thermosensitive in situ gel.

Results

The optimal PL-coated nanoparticle formulation (LP1) showed the smallest particle size (345.5 nm), the highest zeta potential (32.9 mV) and the greatest percent drug released after 6 h (71%). The optimum in situ gel loaded with LP1 (NG3) showed three times greater permeation through nasal mucosa than aqueous solution of TS and revealed about 94% and 92% of the effect of IV injection of drug solution on tidal volume and peak expiratory flow in histamine treated rats, respectively.

Conclusion

The developed PL-coated CS/PC/in situ gel could be considered as a promising intranasal formulation of TS for asthma management.

中文翻译：

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新型脂质-聚合物混合纳米颗粒结合在热敏原位凝胶中，用于鼻内递送硫酸特布他林。

摘要

目的

目前的工作旨在提高硫酸特布他林 (TS) 的生物利用度并延长其用于治疗哮喘的鼻腔停留时间。

方法

采用离子凝胶法制备壳聚糖/果胶聚电解质复合纳米粒子（CS/PC）并包覆磷脂（PL），然后掺入优化的热敏原位凝胶中。

结果

最佳 PL 涂层纳米颗粒配方 (LP1) 显示出最小的粒径 (345.5 nm)、最高的 zeta 电位 (32.9 mV) 和最大的药物在 6 小时后释放百分比 (71%)。载有 LP1 (NG3) 的最佳原位凝胶显示通过鼻粘膜的渗透率是 TS 水溶液的三倍，并揭示了静脉注射药物溶液对组胺潮气量和峰值呼气流量的影响的 94% 和 92%分别处理大鼠。

结论

开发的 PL 涂层 CS / PC / 原位凝胶可以被认为是一种有前途的 TS 鼻内制剂，用于哮喘管理。