Design and Optimization of Nanophytosomes Containing Mucuna prureins Hydroalcoholic Extract for Enhancement of Antidepressant Activity

IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Poonam Karekar, Suresh Killedar, Sudhanshu Kulkarni, Amir Shaikh, Poournima Patil
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Abstract

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

Abstract Image

含粘虫醇提取物纳米植物体抗抑郁活性的设计与优化
目的:通过对含粘虫提取物(MPE)纳米植物体的中药制剂进行改造,改善其药物释放速度、体内抗抑郁特性和稳定性。方法采用全因子设计方法,综合考虑多种因素,优选优选的Mucuna prureins纳米植物体(MPP)。然后,研究了具有较高包封效率的纯提取物和优化配方在瑞士白化病小鼠强迫游泳试验(FST)和悬尾试验(TST)抑郁模型中的体外溶出度和体内抗抑郁活性。采用粒度分析、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、扫描电镜和溶解度研究等方法进行了理化表征。此外,通过冻融循环稳定性测试和循环结束时的包封效率来评估优化后的纳米植物体的稳定性。结果spxrd和SEM分析显示纳米植物体的结晶性降低。1H NMR、DSC和FTIR证实了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度和程度也得到了增强和维持。体内抗抑郁活性表明,与用纯提取物治疗的小鼠相比,用纳米植物体治疗的小鼠的不动能力显著减少。优化后的配方稳定,捕集效率值没有显著降低。结论纳米植物体给药是改善提取液理化性质的最佳途径,可用于改善溶解度差、渗透性差、稳定性差的提取液。图形抽象
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来源期刊
Journal of Pharmaceutical Innovation
Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-
CiteScore
3.70
自引率
3.80%
发文量
90
审稿时长
>12 weeks
期刊介绍: The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.
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