Faculty of Pharmacy, Pharmaceutics Department, Helwan University, Cairo, Egypt.
Faculty of Pharmacy, Pharmaceutics and Industrial Pharmacy, Al-Azhar university, Cairo, Egypt.
J Liposome Res. 2021 Sep;31(3):291-303. doi: 10.1080/08982104.2020.1806874.
The aim of this research was the development and optimization of nanoniosomes for delivery of glibenclamide (Gbn) as hypoglycaemic agent to the lung in an inhaler dosage form. Fifteen formulae of niosomal dispersions were prepared according to Box-Behnken design. The effect of drug amount, Cholesterol molar ratio, and Hydrophilic lipophilic balance (HLB) values of the surfactant on the mean vesicle size, Zeta potential (ZP), polydispersity index (PDI), entrapment efficiency, and released of Gbn were investigated. A quality control check was performed on an inhaler filled with the optimum nanoniosomal formula. The hypoglycaemic effect of nanoniosomal inhalation was also evaluated. The vesicle size observed of the optimized formula was 172 ± 4.6 nm, PDI was 0.304 ± 0.06 and ZP was -49.9 ± 1.5 mv with 69 ± 9.3% drug release after 2 h. The Cholesterol molar ratio and the HLB value showed a statistically significant effect on dependent variables. results proved that nanoniosomes were efficiently delivered from the inhalation canister showing a mass median aerodynamic diameter of 1.4 micron. The inhaled nanoniosomal dispersion loaded with Gbn showed a decrease in blood glucose level of hyperglycaemic rats by 51.42 ± 5.2%± after 180 min which was nearly two folds compared to oral Gbn. Gibenclamide nanoniosomes inhaler could be suggested as a novel effective dosage form for the treatment of Diabetes mellitus.
本研究旨在开发和优化用于将格列本脲（Gbn）作为降血糖剂递送至肺部的纳米囊泡，制成吸入剂型。根据 Box-Behnken 设计，制备了 15 种纳米囊泡分散体配方。考察了药物剂量、胆固醇摩尔比和表面活性剂的亲水亲油平衡值（HLB）对平均囊泡粒径、Zeta 电位（ZP）、多分散指数（PDI）、包封效率和 Gbn 释放的影响。对装有最佳纳米囊泡配方的吸入器进行了质量控制检查。还评估了纳米囊泡吸入的降血糖作用。优化配方观察到的囊泡大小为 172±4.6nm，PDI 为 0.304±0.06，ZP 为-49.9±1.5mv，2h 后药物释放 69±9.3%。胆固醇摩尔比和 HLB 值对因变量显示出统计学上的显著影响。结果证明，纳米囊泡从吸入罐中有效递送至肺部，显示出 1.4 微米的质量中值空气动力学直径。负载 Gbn 的吸入纳米囊泡分散体可使高血糖大鼠的血糖水平降低 51.42±5.2%±，180min 后，与口服 Gbn 相比，降低了近两倍。格列本脲纳米囊泡吸入器可作为治疗糖尿病的新型有效剂型。
