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Design and Optimization of Nanophytosomes Containing Mucuna prureins Hydroalcoholic Extract for Enhancement of Antidepressant Activity
Journal of Pharmaceutical Innovation ( IF 2.6 ) Pub Date : 2022-04-11 , DOI: 10.1007/s12247-022-09646-w
Poonam Karekar 1, 2 , Sudhanshu Kulkarni 2 , Amir Shaikh 2 , Suresh Killedar 3 , Poournima Patil 4
Affiliation  

Purpose

In this study, the herbal formulation containing nanophytosomes of Mucuna prureins extract (MPE) was engineered to ameliorate its rate of drug release, in vivo antidepressant profile, and stability.

Method

The Mucuna prureins nanophytosomes (MPP) were designed by using a full factorial design approach, taking into consideration various variables that could give optimized formulation. Then, pure extract and optimized formulation showing higher entrapment efficiency were studied for in vitro dissolution and in vivo antidepressant activity in depression models like forced swimming test (FST) and tail suspension test (TST) in Swiss albino mice. The physicochemical characterization was carried out using particle size analysis and zeta potential, Fourier transformation infrared spectroscopy, differential scanning calorimetry, proton nuclear magnetic resonance, powder X-ray diffractometer, scanning electron microscopy, and solubility studies. Moreover, the stability of nanophytosomes was assessed by subjecting optimized formulation to freeze–thaw cycle stability testing and calculating entrapment efficiency at the end of the cycle.

Results

PXRD and SEM revealed a decrease in the crystalline nature of nanophytosomes. 1H NMR, DSC, and FTIR asserted the formation of the phyto-phospholipids complex. The rate and extent of dissolution were also found enhanced and sustained in nanophytosomes as compared to pure extract. In vivo antidepressant activity depicted a significant reduction of immobility in mice treated with nanophytosomes as compared to those treated with the pure extract. Moreover, optimized formulation was found stable as entrapment efficiency values were not reduced significantly.

Conclusion

Thus, nanophytosomes drug delivery could be the best strategy to improve physicochemical properties of extract and thus could be exploited for the extracts having poor solubility, poor permeability, and poor stability.

Graphical Abstract



中文翻译:

含有黧豆素水醇提取物的纳米植物体的设计和优化以增强抗抑郁活性

目的

在这项研究中,含有黧豆素提取物 (MPE) 纳米植物体的草药制剂经过工程改造,可改善其药物释放速率、体内抗抑郁特性和稳定性。

方法

纳米植物体 (MPP) 是通过使用全因子设计方法设计的,同时考虑了可以提供优化配方的各种变量。然后,在瑞士白化病小鼠的强迫游泳试验 (FST) 和悬尾试验 (TST) 等抑郁症模型中,研究了显示更高包封率的纯提取物和优化制剂的体外溶出和体内抗抑郁活性。使用粒度分析和zeta电位、傅里叶变换红外光谱、差示扫描量热法、质子核磁共振、粉末X射线衍射仪、扫描电子显微镜和溶解度研究进行物理化学表征。而且,

结果

PXRD 和 SEM 揭示了纳米植物体的结晶性质降低。1 H NMR、DSC 和 FTIR 断言植物-磷脂复合物的形成。与纯提取物相比,纳米植物体的溶解速率和程度也被发现增强和持续。与用纯提取物处理的小鼠相比,用纳米植物体处理的小鼠体内抗抑郁活性显着降低。此外,发现优化的配方是稳定的,因为包封效率值没有显着降低。

结论

因此,纳米植物体药物递送可能是改善提取物理化性质的最佳策略,因此可用于溶解性差、渗透性差和稳定性差的提取物。

图形概要

更新日期:2022-04-11
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