Singla Rajeev K, Singh Digvijay, Verma Ravinder, Kaushik Deepak, Echeverría Javier, Garg Vandana, Gupta Pankaj, Rahman Mohammad Akhlaquer, Sharma Ajay, Mittal Vineet, Shen Bairong
Joint Laboratory of Artificial Intelligence for Critical Care Medicine, Department of Critical Care Medicine and Institutes for Systems Genetics, Frontiers Science Center for Disease-related Molecular Network, West China Hospital, Sichuan University, Chengdu, Sichuan 610212, China; School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab 144411, India.
Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak 124001, India.
Phytomedicine. 2024 Feb;124:155286. doi: 10.1016/j.phymed.2023.155286. Epub 2023 Dec 16.
Fermented formulations are extensively used in Ayurveda due to several benefits like improved palatability, bioavailability, pharmacological potential, and shelf life. These formulations can also quench the heavy metals from the plant material and thus reduce the toxicity. Seeds of Silybum marianum (L.) Gaertn. are widely used for the management of many liver diseases.
In the present study, we developed a novel fermented formulation of S. marianum seeds and evaluated parameters like safety (heavy metal analysis) and effectiveness (hepatoprotective). As the developed formulation's validation is crucial, the critical process variables (time, pH, and sugar concentration) are optimized for alcohol and silybin content using the Box-Behnken design (BBD).
The response surface methodology coupled with BBD predicted the optimized conditions (fermentation time (28 days), pH 5.6, and sugar concentration (22.04%)) for the development of a fermented formulation of the selected herb. Moreover, the alcohol content (6.5 ± 0.9%) and silybin concentration (26.1 ± 2.1%) were confirmed in optimized formulation by GC-MS and HPTLC analysis. The optimized formulation was also analyzed for heavy metals (Pb, As, Hg, and Cd); their concentration is significantly less than the decoction of herbs. Further, the comparative evaluation of the developed formulation with the marketed formulation also confirmed that the fermented formulation's silybin concentration and percentage release were significantly enhanced. In addition, the developed fermented formulation's percentage recovery of HepG2 cell lines after treatment with CCl4 was significantly improved compared with the marketed formulation.
It can be summarized that the developed fermented formulation improves safety and effectiveness compared to other market formulations. Finally, it can be concluded that the developed fermented formulation could be further explored as a better alternative for developing Silybum marianum preparation.
发酵制剂在阿育吠陀医学中被广泛使用，因为它具有多种益处，如改善适口性、生物利用度、药理潜力和保质期。这些制剂还可以去除植物材料中的重金属，从而降低毒性。水飞蓟（Silybum marianum (L.) Gaertn.）的种子被广泛用于治疗多种肝脏疾病。
在本研究中，我们开发了一种新型的水飞蓟种子发酵制剂，并评估了其安全性（重金属分析）和有效性（肝脏保护作用）等参数。由于所开发制剂的验证至关重要，因此使用Box-Behnken设计（BBD）对关键工艺变量（时间、pH值和糖浓度）进行优化，以确定酒精和水飞蓟宾的含量。
响应面法结合BBD预测了所选草药发酵制剂开发的优化条件（发酵时间（28天）、pH值5.6和糖浓度（22.04%））。此外，通过气相色谱-质谱联用（GC-MS）和高效薄层色谱（HPTLC）分析，在优化制剂中确认了酒精含量（6.5±0.9%）和水飞蓟宾浓度（26.1±2.1%）。还对优化制剂中的重金属（铅、砷、汞和镉）进行了分析；其浓度明显低于草药煎剂。此外，将所开发制剂与市售制剂进行的对比评估也证实，发酵制剂的水飞蓟宾浓度和释放百分比显著提高。此外，与市售制剂相比，用四氯化碳处理后，所开发发酵制剂对HepG2细胞系的回收率百分比显著提高。
可以总结出，与其他市售制剂相比，所开发的发酵制剂提高了安全性和有效性。最后，可以得出结论，所开发的发酵制剂可作为开发水飞蓟制剂的更好替代品进行进一步探索。
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