Department of Pharmacy
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Item Back Cover: Preclinical pharmacokinetics of trigonelline using ultra-performance liquid chromatography–tandem mass spectrometry and pharmacological studies targeting type 2 diabetes(Wiley, 2021-04) Taliyan, RajeevThe cover picture shows, Trigonelline (Tr) a quaternary base alkaloid, which acts by affecting β-cell regeneration and insulin secretion. Tr lowers the blood glucose and lipid levels due to which it is used in the treatment of co-morbid diseases. Herein, we have aimed to develop a bioanalytical method for estimation of Tr using UPLC-MS/MS and explore the pharmacokinetic profile. The anti-diabetic, antilipidemic efficacy studies were also conducted in the high-fat diet-induced streptozotocin-diabetic rat. The experimental results suggest that Tr follow the two compartmental pharmacokinetic model. In addition, Tr exhibited a significant anti-hyperglycemic and antihyperlipidemic efficacy in high-fat diet-induced streptozotocin induced diabetic rats.Item Preclinical pharmacokinetics of trigonelline using ultra-performance liquid chromatography–tandem mass spectrometry and pharmacological studies targeting type 2 diabetes(Wiley, 2021-03) Taliyan, RajeevTrigonelline is a quaternary base alkaloid and zwitterionic complex that acts by affecting β-cell regeneration and insulin secretion. Tr inhibits enzymatic activities, lowering the blood glucose and lipid levels due to which it is used in the treatment of co-morbid diseases such as diabetes, Alzheimer's, etc. Herein, it was aimed to develop a bioanalytical method for estimation of Tr using ultra-performance liquid chromatography–tandem mass spectrometry and explore the pharmacokinetic profile. The anti-diabetic, antilipidemic efficacy studies of Tr in the high-fat diet-induced streptozotocin-diabetic rat model was also explored. The separation of analyte was achieved with acetonitrile and 0.1% formic acid (20:80) with a flow of 0.4 mL/min. The ionization of the analyte was achieved in positive electrospray ionization mode with the precursor to product ion transitions of Tr (138.14 > 94), and Trigonelline D3 (143.19 > 97.13). The validated assay was effectively applied for the estimation of compartmental pharmacokinetic by using Phoenix WinNolin8.0 (Certera™, USA) and it was observed that the Tr follow two compartmental pharmacokinetic model. The experimental results also suggest that Tr distributed through the central compartment to the peripheral compartment and redistributed to the central compartment. In addition, Tr exhibited significant anti-hyperglycemic and antihyperlipidemic efficacy against high-fat diet-induced streptozotocin-induced type 2 diabetic rats.Item Recent advances in nanocarriers for nutrient delivery(Springer, 2022) Taliyan, Rajeev; Singhvi, GautamFor the past few years, there has been a surge in the use of nutraceuticals. The global nutraceuticals market in 2020 was USD 417.66 billion, and the market value is expected to increase by 8.9% compound annual growth rate from 2020 to 2028. This is because nutraceuticals are used to treat and prevent various diseases such as cancer, skin disorders, gastrointestinal, ophthalmic, diabetes, obesity, and central nervous system–related diseases. Nutritious food provides the required amount of nutrition to the human body through diet, whereas most of the bioactive agents present in the nutrients are highly lipophilic, with low aqueous solubility leading to poor dissolution and oral bioavailability. Also, the nutraceuticals like curcumin, carotenoids, anthocyanins, omega-3 fatty acids, vitamins C, vitamin B12, and quercetin have limitations such as poor solubility, chemical instability, bitter taste, and an unpleasant odor. Additionally, the presence of gastrointestinal (GIT) membrane barriers, varied pH, and reaction with GIT enzymes cause the degradation of some of the nutraceuticals. Nanotechnology-based nutrient delivery systems can be used to improve oral bioavailability by increasing nutraceutical stability in foods and GIT, increasing nutraceutical solubility in intestinal fluids, and decreasing first-pass metabolism in the gut and liver. This article has compiled the properties and applications of various nanocarriers such as polymeric nanoparticles, micelles, liposomes, niosomes, solid lipid nanocarriers, nanostructured lipid carrier, microemulsion, nanoemulsion, dendrimers in organic nanoparticles, and nanocomposites for effective delivery of bioactive molecules.Item Possible mechanism of protective effect of thalidomide in STZ-induced-neuropathic pain behavior in rats(Springer, 2011-12) Taliyan, RajeevDiabetes-induced neuropathic pain is recognized as one of the most difficult type of pain to treat and conventional analgesics are well known to be partially effective or associated with potential toxicity. Recently, it has been demonstrated that thalidomide, besides its teratogenic potential, reduced chronic pain in an SNL experimental pain model.Item Protective Effect and Potential Mechanism of Ginkgo biloba Extract EGb 761 on STZ-induced Neuropathic Pain in Rats(Wiley, 2012-03) Taliyan, RajeevDiabetes induced neuropathic pain is recognized as one of the most difficult types of pain to treat with conventional analgaesics. EGb 761 is a standardized extract of Ginkgo biloba that has analgaesic and antiinflammatory properties and modulatory effects on key pain-related molecules. We examined the effect of EGb 761 on streptozotocin (STZ)-induced neuropathic pain behaviours and assessed its mechanism of action. Streptozotocin (20 mg/kg i.p for 5 days) was administered to induce experimental diabetes. Pain hypersensitivity to radiant heat was measured using the Dynamic Plantar Aesthesiometer to test the pain threshold. Diabetic rats exhibited mechanical allodynia and thermal hyperanalgaesia after the third week of STZ injection and concomitantly increased thiobarbituric acid reactive substance and nitric oxide concentration. The antioxidant enzymes level of superoxide dismutase and catalase was markedly reduced in STZ-diabetic rats (p < 0.05). Systemic administration of EGb 761 (25, 50 and 100 mg/kg), starting after the third week following STZ injection, dose-dependently reversed STZ-induced thermal hyperanalgaesia and mechanical allodynia. Moreover, it reduced oxidonitrosative stress and concomitantly restored the level of antioxidant enzymes (p < 0.05) as compared with untreated diabetic rats. These results suggest that EGb 761 attenuated STZ-induced neuropathic pain behaviours by inhibiting oxidative and nitrosative stress and may constitute a new approach for treatment of painful diabetic