Gauttam Vinod Kumar, Kalia Ajudhia Nath
Department of Pharmacognosy, ISF College of Pharmacy, Moga, Punjab, India.
J Adv Pharm Technol Res. 2013 Apr;4(2):108-17. doi: 10.4103/2231-4040.111527.
Multifactorial metabolic diseases, for instance diabetes develop several complications like hyperlipidemia, hepatic toxicity, immunodeficiency etc., Hence, instead of mono-drug therapy the management of the disease requires the combination of herbs. Marketed herbal drugs comprise of irrational combinations, which makes their quality control more difficult. Phytoconstituents, despite having excellent bioactivity in vitro demonstrate less or no in vivo actions due to their poor lipid solubility, resulting in high therapeutic dose regimen; phospholipids encapsulation can overcome this problem. Hence, present study was designed to develop a phospholipids encapsulated polyherbal anti-diabetic formulation. In the present study, polyherbal formulation comprises of lyophilized hydro-alcoholic (50% v/v) extracts of Momordica charantia, Trigonella foenum-graecum and Withania somnifera 2:2:1, respectively, named HA, optimized based on oral glucose tolerance test model in normal Wistar rats. The optimized formulation (HA) entrapped in the phosphatidylcholine and cholesterol (8:2) vesicle system is named HA lipids (HAL). The vesicles were characterized for shape, morphology, entrapment efficiency, polar-dispersity index and release profile in the gastric pH. The antidiabetic potential of HA, marketed polyherbal formulation (D-fit) and HAL was compared in streptozotocin-induced diabetic rat model of 21 days study. The parameters evaluated were behavioral changes, body weight, serum glucose level, lipid profile and oxidative stress. The antidiabetic potential of HA (1000 mg/kg) was at par with the D-fit (1000 mg/kg). However, the potential was enhanced by phospholipids encapsulation; as HAL (500 mg/kg) has shown more significant (P < 0.05) potential in comparison to HA (1000 mg/kg) and at par with metformin (500 mg/kg).
多因素代谢疾病,例如糖尿病会引发多种并发症,如高脂血症、肝毒性、免疫缺陷等。因此,该疾病的治疗不是采用单一药物疗法,而是需要草药组合。市售的草药药物包含不合理的组合,这使得它们的质量控制更加困难。植物成分尽管在体外具有出色的生物活性,但由于其脂溶性差,在体内的作用较小或没有作用,导致治疗剂量方案较高;磷脂包封可以克服这个问题。因此,本研究旨在开发一种磷脂包封的多草药抗糖尿病制剂。在本研究中,多草药制剂分别由苦瓜、胡芦巴和印度人参的冻干水醇(50% v/v)提取物按2:2:1组成,命名为HA,并基于正常Wistar大鼠的口服葡萄糖耐量试验模型进行了优化。包裹在磷脂酰胆碱和胆固醇(8:2)囊泡系统中的优化制剂(HA)命名为HA脂质(HAL)。对囊泡的形状、形态、包封效率、极性分散指数和在胃pH值下的释放曲线进行了表征。在链脲佐菌素诱导的糖尿病大鼠模型中进行了为期21天的研究,比较了HA、市售多草药制剂(D-fit)和HAL的抗糖尿病潜力。评估的参数包括行为变化、体重、血糖水平、血脂谱和氧化应激。HA(1000 mg/kg)的抗糖尿病潜力与D-fit(1000 mg/kg)相当。然而,磷脂包封增强了其潜力;因为HAL(500 mg/kg)与HA(1000 mg/kg)相比显示出更显著(P < 0.05)的潜力,并且与二甲双胍(500 mg/kg)相当。