Glibenclamide nanosuspension inhaler: development, in vitro and in vivo assessment
Glibenclamide nanosuspension inhaler: development, in vitro and in vivo assessment
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DOI：
10.1080/03639045.2020.1753062
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发表时间：
2020-04-17
影响因子：
3.4
通讯作者：
Hassan, Abdelsabour A. A.
中科院分区：
文献类型：
--
作者：
Hashem, Fahima M.;Abd Allah, Fathy I.;Hassan, Abdelsabour A. A.
目的：研制用于格列本脲肺靶向降糖药吸入剂的纳米混悬液。方法：采用Box-Behnken设计制备格列本脲纳米混悬剂配方，考察自变量对因变量的影响，采用傅里叶变换红外光谱法、差示扫描量热法、格列本脲纳米混悬剂吸入器的评价及体内降糖效果来确定格列本脲纳米混悬剂吸入器的效果。结果：制备的纳米混悬液的平均粒径范围为0.216 ~ 0.856 μ m， zeta电位范围为+9 ~ +16 mV，溶解度范围为43% ~ 75%，空气动力学直径中值为2.34 μ m，大鼠血糖水平显著降低约60%。结论：格列本脲纳米混悬吸入剂能提高格列本脲的降糖效果，减少不良反应，为糖尿病治疗开辟了新的剂型。
Objective: The development of nanosuspension for targeted delivery of glibenclamide as hypoglycemic agent to the lung in an inhaler dosage form. Method: Glibenclamide nanosuspension formulations were prepared using Box-Behnken design to investigate the effect of independent factors on the dependent variables, Fourier-transform Infrared spectroscopy, Differential Scanning Calorimetry, evaluation of glibenclamide nanosuspension inhaler and in vivo hypoglycemic efficacy were performed to determine glibenclamide nanosuspension inhaler effect. Results: The results revealed that the mean particle sizes of the prepared nanosuspension ranged from 0.216 to 0.856 mu m, zeta potential from +9 to +16 mV, the solubility ranged from 43% to 75%, the mass median aerodynamic diameter was 2.34 mu m and the glucose level in rat was significantly reduced by about 60%. Conclusion: These results confirmed that glibenclamide nanosuspension inhaler enhance hypoglycemic effectiveness and reduce adverse effect of glibenclamide, opening up new dosage form in Diabetes mellitus treatment.