Gudise Venkataiah, Chowdhury Bimalendu, Manjappa Arehalli S
Department of Pharmacology, SSJ College of Pharmacy, Vattinagulapally, Gandipet, Hyderabad-500075, Telangana State, India.
Department of Pharmacology, Roland Institute of Pharmaceutical Sciences, Khodasingi, Berhampur-760010, Odisha, India.
J Tradit Complement Med. 2020 Aug 6;11(3):259-267. doi: 10.1016/j.jtcme.2020.08.001. eCollection 2021 May.
Herbal medicine combined with nanotechnology is widely proposed to improve the oral bioavailability, reduce the required dose and side effects, and improve the pharmacological efficacy of extracts. Thus, this study evaluated the antidiabetic and antihyperlipidemic activities of ethanolic leaf extracts of (AP) and (MP) plants in comparison with their micellar nanoformulations.
The mixed micelles (MMs) loaded with crude extracts (CEs) of AP and MD (AP-MMs and MD-MMs) were prepared using a film dispersion technique. Type 2 diabetes was induced in rats using high-fat diet (HFD) and low-dose (35 mg/kg) streptozotocin (STZ) injection. The pharmacological actions of CEs, AP-MMs and MD-MMs were determined in type 2 diabetic Sprague-Dawley rats.
Oral treatments with low-dose AP-MMs and MD-MMs having a mean particle size of 163 ± 10 nm and 145 ± 8 nm respectively, resulted in significantly decreased fasting blood glucose level and increased serum insulin, glucokinase levels, and normalized the elevated levels of hemoglobin A1C and glucose-6-phosphatase. Both extracts significantly decreased serum total cholesterol, triglycerides, and low-density lipoprotein, as well as elevated high-density lipoprotein levels. Additionally, improvements in antioxidant enzymes (superoxide dismutase, catalase, glutathione peroxidase) and malondialdehyde levels were evidenced clearly in tested vital organs (brain, heart, liver).
This is the first report of the antidiabetic and antihyperlipidemic activities of ethanolic leaf extracts of AP and MP plants. Our findings indicate the potential utility of nanotechnology in improving the oral therapeutic efficacy of herbal extracts.
草药与纳米技术相结合被广泛认为可提高口服生物利用度、降低所需剂量和副作用,并提高提取物的药理功效。因此,本研究评估了(AP)和(MP)植物乙醇叶提取物与其胶束纳米制剂相比的抗糖尿病和抗高脂血症活性。
采用薄膜分散技术制备负载AP和MD粗提物(CEs)的混合胶束(MMs)(AP-MMs和MD-MMs)。使用高脂饮食(HFD)和低剂量(35mg/kg)链脲佐菌素(STZ)注射诱导大鼠患2型糖尿病。在2型糖尿病Sprague-Dawley大鼠中测定CEs、AP-MMs和MD-MMs的药理作用。
口服低剂量的AP-MMs和MD-MMs,其平均粒径分别为163±10nm和145±8nm,可显著降低空腹血糖水平,提高血清胰岛素、葡萄糖激酶水平,并使升高的糖化血红蛋白A1C和葡萄糖-6-磷酸酶水平恢复正常。两种提取物均显著降低血清总胆固醇、甘油三酯和低密度脂蛋白水平,并提高高密度脂蛋白水平。此外,在受试重要器官(脑、心脏、肝脏)中,抗氧化酶(超氧化物歧化酶、过氧化氢酶、谷胱甘肽过氧化物酶)和丙二醛水平明显改善。
这是关于AP和MP植物乙醇叶提取物抗糖尿病和抗高脂血症活性的首次报道。我们的研究结果表明纳米技术在提高草药提取物口服治疗效果方面具有潜在用途。