米氮平水包体的配制、优化和全面表征:提高抗抑郁效果的新技术

IF 2.4 4区 医学 Q3 CHEMISTRY, MEDICINAL Drug Development and Industrial Pharmacy Pub Date : 2024-03-01 Epub Date: 2024-02-28 DOI:10.1080/03639045.2024.2313538
Lamiaa Mohamed Hussein, Aya Mohamed Dawaba, Shereen Ahmed El-Adawy
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引用次数: 0

摘要

方法采用Box-Behnken设计法制备了MRT负载水生体配方,研究了超声时间(X1)、超声温度(X2)和糖浓度(X3)等独立因素对粒径和药物负载效率等因变量的影响。通过傅立叶变换红外光谱法(FTIR)、差示扫描量热法(DSC)和 X 射线粉末衍射法(XRPD)对优化配方进行了验证。此外,还利用透射电子显微镜(TEM)对配方的形态进行了评估。结果表明,优化配方的粒径小(202.7 ± 3.7 nm),负载效率高(77.65 ± 2.6%)。热 DSC 和 XRPD 研究表明,MRT 负载水苏糖具有无定形性质。体外研究表明,8 小时后 F(opt)的持续释放率为 88.16%,而普通 MRT 1 小时后的释放率为 63.06%。这些结果证实,MRT 的抗抑郁效果在配制的水囊体中得到显著增强,从而为有效递送 MRT 提供了一种前景广阔的纳米囊泡载体系统。
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Formulation, optimization and full characterization of mirtazapine loaded aquasomes: a new technique to boost antidepressant effects.

Objective: The development of Mirtazapine (MRT)-loaded aquasomes by co-precipitation sonication technique to boost the antidepressant potential of MRT.

Methodology: MRT-loaded aquasomes formulations were prepared using Box-Behnken design to investigate the effect of independent factors including sonication time (X1), sonication temperature (X2), and sugar concentration (X3) on the dependent variables as particle size and drug loading efficiency. The formulation of the optimized formula was verified by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and X-ray Powder Diffraction (XRPD). Furthermore, the morphology of the formula was evaluated by Transmission Electron Microscopy (TEM). The optimum MRT- loaded aquasomes was assessed for physiochemical properties, in vitro MRT release and in vivo antidepressant effects in mice model.

Results: The results revealed that the optimized formula showed a small particle size of 202.7 ± 3.7 nm and a high loading efficiency of 77.65 ± 2.6%. Thermal DSC and XRPD studies demonstrated the amorphous nature of MRT-loaded aquasomes. The in vitro study demonstrated sustained release of F (opt) 88.16% after 8 h, compared with plain MRT release of 63.06% after 1 h. Mice treated with MRT-loaded aquasomes demonstrated reduced immobility time in behavioral analysis to 37% with MRT-loaded aquasomes, while plain MRT reduced it to 55%.

Conclusion: These results confirmed that the antidepressant effect of MRT was significantly boosted in formulated aquasomes, and thereby they provide a promising carrier nano vesicular system for effective delivery of MRT.

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来源期刊
CiteScore
6.80
自引率
0.00%
发文量
82
审稿时长
4.5 months
期刊介绍: The aim of Drug Development and Industrial Pharmacy is to publish novel, original, peer-reviewed research manuscripts within relevant topics and research methods related to pharmaceutical research and development, and industrial pharmacy. Research papers must be hypothesis driven and emphasize innovative breakthrough topics in pharmaceutics and drug delivery. The journal will also consider timely critical review papers.
期刊最新文献
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