Glucose and Lipid Lowering Potentials of <i>Heliotropium indicum</i> L. Leaves in Alloxan-Induced Hyperglycaemic Rats

The antidiabetic potentials of Heliotropium indicum L. leaf aqueous (HILA) extract used for the management of diabetes by Traditional Medicinal Practitioners (TMPs) in Nigeria was assessed. Alloxan (ALX)-induced hyperglycaemic rats were orally administered with known folkloric dosage of 30 and 75 mg/kg b. wt. of HILA extract, once a day, for 14 days. Fasting blood glucose (FBG) levels were monitored and pancreatic histology was examined. Net hepatic glycogen (GLY) concentration and lipid profiles were also determined. Prior to treatment, ALX-induced hyperglycaemia (>250 mg/dL) was established in rats. Oral administration of 30 and 75 mg/kg b. wt. HILA extract to diabetic rats for 14 days caused significant reduction in FBG to baseline values observed in non-diabetic conditions. Treatment with HILA extract also showed improvement in lipid abnormalities observed in hyperglycaemic condition, levels of triglyceride, total cholesterol and LDL-cholesterol were significantly reduced and HDL-cholesterol increased resulting in improved artherogenic index. Hepatic GLY concentration was significantly increased in diabetic rat treated with the extract. Histological examinations showed degenerated and sparse pancreatic islets β-cells in non-treated diabetic rat, whereas microscopy of treated rats showed mild to normal architecture with enriched β-cells. Preliminary phytochemical profiling of the extract revealed the presence of alkaloids (2.54 mg/g), saponins (0.28 mg/g), phenols (0.04 mg/g) and anthraquinones (0.01 mg/g). Results from this study revealed that the aqueous leaf extract of H. indicum possesses not only antihyperglycaemic, but also antidyslipidemic activities, that may prove to be of clinical importance in the management of diabetes and associated secondary complications

Microencapsulation of eucalyptol in polyethylene glycol and polycaprolactone using particles from gas-saturated solutions

Eucalyptol is the natural cyclic ether which constitutes the bulk of terpenoids found in essential oils of Eucalyptus spp. and is used in aromatherapy for treatment of migraine, sinusitis, asthma and stress. It acts by inhibiting arachidonic acid metabolism and cytokine production. Chemical instability and volatility of eucalyptol restrict its therapeutic application and necessitate the need to develop an appropriate delivery system to achieve extended release and enhance its bioactivity. However, the synthesis method of the delivery system must be suitable to prevent loss or inactivation of the drug during processing. In this study, supercritical carbon dioxide (scCO2) was explored as an alternative solvent for encapsulation and co-precipitation of eucalyptol with polyethylene glycol (PEG) and/or polycaprolactone (PCL) using the particles from gas-saturated solution (PGSS) process. Polymers and eucalyptol were pre-mixed and then processed in a PGSS autoclave at 45 °C and 80 bar for 1 h. The mixture in scCO2 was micronized and characterized. The presence of eucalyptol in the precipitated particles was confirmed by infrared spectroscopy, gas chromatography and mass spectrometry. The weight ratios of PEG–PCL blends significantly influenced loading capacity and encapsulation efficiency with 77% of eucalyptol encapsulated in a 4 : 1 composite blend of PEG–PCL. The particle size distribution of the PGSS-micronized particles ranged from 30 to 260 μm. ScCO2 assisted microencapsulation in PEG and PCL reduced loss of the volatile drug during a two-hour vaporization study and addition of PCL extended the mean release time in simulated physiological fluids. Free radical scavenging and lipoxygenase inhibitory activities of eucalyptol formulated in the PGSS-micronized particles was sustained. Findings from this study showed that the scCO2-assisted micronization can be used for encapsulation of volatile drugs in polymeric microparticles without affecting bioactivity of the drug.National Research Fund, South Africahttp://pubs.rsc.org/en/journals/journalissues/rahj2020Zoology and Entomolog

Aqueous Leaf Extract of Heliotropium Indicum Ameliorates Hyperglycaemia-Induced Tissue Complications in Albino Rats

Background: Heliotropium indicum is used by traditional medical practitioners in North Central Nigeria for the management of ailments including diabetes. However, the folkloric use of H. indicum as antidiabetic has been asserted, but its roles on the hyperglycemia-induced organ-specific complications are not yet scientifically proven. Thus, ameliorative effect of aqueous leaf extract of H. indicum on selected toxicological parameters in hyperglycaemic rats was investigated in this study. Methods: Twenty-five rats were randomized into five groups. The study was carried out at the Animal Holding Unit, Biochemistry Department, University of Ilorin in 2013. Four groups were intraperitoneally administered singly with 150 mg/kg b.wt of alloxan to induce hyperglycemia. The normal control (NC) and hyperglycaemic control (HC) groups were administered 1 ml distilled water, while the reference group (HR) were administered 14.2 mg/kg b.wt of metformin and the test groups, H30 and H75 were administered 30 and 75 mg/kg b.wt, the extract respectively for fourteen days. Results: The significantly increased (P<0.05) serum concentrations of tissue membrane bound enzymes (ALT, AST, ACP and ALP), direct and total bilirubin, urea and creatinine in HC indicating compromised tissue structures and functions in HC were attenuated. The significantly (P<0.05) reduced serum total protein, globulin and albumin in HC were significantly increased by both doses of the extract. The ameliorative role of the extract at the test doses was supported by the histological assessment of liver and kidney of the animals. Conclusion: Aqueous leaf extract of H. indicum can be explored at the ethnobotanical dose of 30 and 75 mg/kg b.wt on the management of some of the tissue-specific disarrays associated with diabetes