新型脂质-聚合物杂化纳米粒嵌入温敏原位凝胶中用于硫酸特布他林的经鼻给药。
Novel lipid-polymer hybrid nanoparticles incorporated in thermosensitive in situ gel for intranasal delivery of terbutaline sulphate.
机构信息
College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology (MUST), Giza, Egypt.
Faculty of Pharmacy, Helwan University, Helwan, Egypt.
出版信息
J Microencapsul. 2020 Dec;37(8):577-594. doi: 10.1080/02652048.2020.1826590. Epub 2020 Oct 2.
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.
目的
本研究旨在提高硫酸特布他林（TS）的生物利用度，并延长其在鼻腔中的驻留时间，以治疗哮喘。
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（CS/PC），并用磷脂（PL）进行包覆，然后将其包埋于优化的温敏原位凝胶中。
结果
最优的 PL 包覆纳米粒制剂（LP1）具有最小的粒径（345.5nm）、最高的 Zeta 电位（32.9mV）和最大的 6h 药物累积释放率（71%）。载有 LP1 的最优原位凝胶（NG3）显示出比 TS 水溶液高 3 倍的鼻腔黏膜透过性，并且在组胺处理的大鼠中分别显示出约 94%和 92%的 IV 注射药物溶液对潮气量和呼气峰流速的作用。
结论
所开发的 PL 包覆 CS/PC/原位凝胶可被视为一种有前途的 TS 鼻腔给药制剂，用于哮喘管理。
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