RESUMEN
Oral delivery of insulin provides a good alternative because it is non-invasive and patient-friendly. However, multiple challenges affected this route. To overcome barriers for oral delivery of insulin, we aimed to develop a novel insulin-loaded microemulsion system based on snail mucin for oral administration. The strategy in the novel system of using mucin loading insulin into the inner core of prepared water in oil microemulsion to provide sustained released, increased in vivo stability and enhanced drug absorption in the gastrointestinal tract. We report how microemulsion composed of varying ratios of snail mucin and Tween® 80 (1:9-9:1) using oil/water emulsion preparation method influenced insulin performance after oral administration. The results obtained include an encapsulation efficiency of above 70 %; in vitro release was sustained over 10 h and in vivo evaluations in diabetic rat model shows that insulin-loaded microencapsulation effectively reduced blood glucose levels over a period >8 h after oral administration. Therefore, we suggest that the developed formulation for oral insulin can be a promising alternative dosage form for oral protein delivery.
RESUMEN
AIM/BACKGROUND: Given the prevalence of toxicants in foods, beauty products, etc., and the increasing demand for "green" products, there is a need for the development of "nutri-drinks" with hepatoprotective properties. The usefulness of tigernut milk (TNM) in preventing acetaminophen (APAP)-induced liver injury was, therefore, investigated. MATERIALS AND METHODS: A total of 25 rats were randomized into five equal groups. Four groups were treated with 0, 500, 1000, and 2000 kg/mg body weight (bw) TNM, respectively, per os for 2 weeks before they were challenged with 2500 mg/kg bw APAP. Biochemical markers of hepatotoxicity and oxidative stress were determined in the sera of the rats at the end of the study. RESULTS: Serum alanine aminotransferase concentrations decreased significantly (P < 0.001) and dose-dependently from 334.3 ± 16.1 in the negative control group to 65.4 ± 8.3 in the 2000 mg/kg bw TNM group. Other studied liver enzymes were similarly dose-dependently reduced. These data are corroborated by histological findings. Superoxide dismutase activity (U/mg protein) was increased significantly (P < 0.001) from 108.0 ± 7.4 in the negative control group to 291.0 ± 11.3 in the 2000 mg/kg bw TNM group, and indeed all the test groups. The malondialdehyde concentrations in the test rats were slightly lower than that of the negative control group. CONCLUSION: TNM at the tested concentrations significantly prevented liver injury. Phytochemicals in TNM, working directly as antioxidants or indirectly by inducing the synthesis of glutathione, may be responsible for the observed effect.
RESUMEN
BACKGROUND: The fruit extract of Dacryodes edulis (D. edulis), the African pear or plum, a tree indigenous to the humid tropics has been used for managing wounds, skin diseases, sickle cell anaemia, dysentery and fever in some African nations. In South Eastern Nigeria, 'herbal doctors' include its marshed fruit in decoctions administered to diabetic patients. However no scientific substantiation of their claim and use exist in literature. Hence, the need to evaluate the antidiabetic and hypolipidaemic activity of hexane extracts of D. edulis fruit in alloxanised animal model. MATERIALS AND METHODS: Sub-toxic doses between 400 and 1600mg/kg were orally administered sub-chronically to alloxan-induced diabetic rats for 15 days and compared to glibenclamide (2.5mg/kg). The glycaemia levels, body weights, lipid profile, blood urea, creatinine and liver enzyme levels were measured. Basic histology of the pancreatic tissue was also performed to examine the effects on the pancreas as possible mechanistic lead. RESULTS: Oral acute dosing of D. edulis hexane extract decreased blood glucose levels, while sub-chronic treatment of the extract down-regulated significantly hyperglycaemia, total cholesterol, triglycerides, LDL-C, ALT and ALP levels. However, the HDL-C levels increased significantly. Histopathological examination of the pancreatic tissues after sub-chronic treatment showed that glibenclamide and the highest dose of the extract 1600mg/kg restored the afore-damaged pancreatic ß-cell architecture. CONCLUSION: Our findings portend that D. edulis hexane fruit extract possesses hypoglycaemic and hypolipidaemic activities as well as restoration of the pancreatic architecture without any obvious untoward hepatic damages, suggesting that its use in the management of the diabetes may be valid. List of Non-standard abbreviations:D. edulis = dacryode edulis, DEnH = Dacryodes edulis n-hexane fruit extract, B.wt. = Body weight, Per os = Oral administration, NC = normal control, DC =Diabetic control, SC = Standard control, LDL-C = low density lipoprotein cholesterol, HDL-C = High density lipoprotein cholesterol, TG = Triglyceride, TC = Total cholesterol.
