Surface stabilized atorvastatin nanocrystals with improved bioavailability, safety and antihyperlipidemic potential

Atorvastatin, a favored option for hyperlipidemia exhibits the problem of poor gastric solubility and low absolute bioavailability (12%) along with higher pre-systemic clearance (>80%). Therefore, to circumvent these limitations, atorvastatin nanocrystals were prepared using poloxamer-188 as stabilizer via high pressure homogenization technique followed by lyophilization. Various variables like drug to poloxamer-188 ratio, homogenization cycle, homogenization pressure, type and concentration of cryoprotectant were optimized to achieve uniform nanosized crystals with good dispersibility. Solid state characterization by ATR-FTIR and DSC revealed no incompatible physicochemical interaction between drug and excipients in formulation while DSC and PXRD collectively corroborated the reduced crystallinity of drug in nanocrystals. Size analysis and SEM confirmed nanometric size range of nanocrystals (225.43 ± 24.36 nm). Substantial improvement in gastric solubility (~40 folds) and dissolution rate of drug in nanocrystals was observed. Pharmacokinetic study in wistar rats revealed significant improvement in oral bioavailability (~2.66 folds) with atorvastatin nanocrystals compared to pure drug. Furthermore, reduction in serum total lipid cholesterol, LDL and triglyceride content justified the effectiveness of formulation at 50% less dose of atorvastatin along with improved plasma safety profile in comparison of pure drug. In conclusion, atorvastatin nanocrystals are safe and efficacious drug delivery system confirming potent competence in treatment of hyperlipidemic conditions with ease of scalability for commercialization.

Comparative studies on the effects of lincomycin and bacitracin on hematobiochemical and immunological parameters in broiler chickens

A total of 100 one-day-old healthy broiler chicks were used to study the effects of lincomycin and bacitracin on some hematobiochemical and immunological parameters. Chicks were divided into four equal groups, 25 each. The first group was kept as control; the 2nd group was received 0.5 g of lincomycin per liter; the 3rd group was received 100 mg bacitracin per liter and the 4th group was administered both lincomycin and bacitracin, each at the above-mentioned dose. Drugs were given in drinking water for 5 successive days from 20th to 25th day of age. Bodyweight was recorded at the beginning of the experiment and at 1st-day post administration where body performance was recorded. One day post administration, blood samples were collected for estimation of hematobiochemical and immunological alterations. The obtained results revealed that broiler chicks administered lincomycin or bacitracin or both revealed a marked increase in bodyweight, weight gain, phagocytic activity, phagocytic index, erythrocytic count, hemoglobin level, packed cell volume, total leukocytic count, serum total protein, albumin, total globulin, α, β and γ globulin. Furthermore, a significant elevation in malondialdehyde associated with a marked reduction in albumin-globulin ratio, serum total lipid, cholesterol and triglyceride and a significant decrease in catalase and superoxide dismutase, were recorded, compared with the control group. In conclusion, lincomycin and bacitracin either alone or in combination have positive impacts on growth performance, immunological and hematobiochemical parameters of broiler chickens. So, it is recommended to use both drugs as growth promoters in broiler chickens.

Changes in lipid profile of rats fed with Agaricus bisporus (white button) mushroom

Purpose White button (Agaricus bisporus) mushroom (WBM) is a good source of fiber, protein and unsaturated fatty acids and is considered an effective food for the treatment of hyperlipidemia. Design/methodology/approach Male Wistar strain rats (28) were divided into four groups, two control and two experimental, which were fed a semi-synthetic diet containing 1 per cent cholesterol and supplemented with 5 and 10 per cent dried mushroom for a period of 42 days. At the end of the experiment, the rats were anesthetized and blood samples were taken. The serum and liver were analyzed for total lipids, triglycerides and phospholipids. Findings Serum total lipid and triglyceride levels were reduced significantly in rats fed on 5 and 10 per cent WBM. However, serum phospholipid levels were decreased only in rats fed on 10 per cent WBM. The deposition of total lipids and triglycerides in liver decreased significantly in the experimental rats. However, no significant differences were observed in liver phospholipid levels in any experimental group of rats. Originality/value Hyperlipidemia is one of the leading medical problems nowadays, and it represents a major concern because of the associated death rates occurring in different communities. The study results indicate that this problem can be reduced through the consumption of A. bisporus mushrooms.

The Possible Improving Effects of γ-Irradiated and/or Extruded Soy Flour on Hypercholesterolemic Rats

Hypercholesterolemia is serious conditions that can cause fatal complications without careful management. Among the dietary supplementation with functional food, soybeans possess variety of antioxidant compounds that may lower incidence of hypercholesterolemia and degenerative cardiovascular disease. Thus, the purpose of this study is to determine the effect of gammairradiated and/or extruded soy flour on hypercholesterolemic rats. Processing of soy flour by γ-irradiation and/or extrusion reduced the amount of antinutritional factors such as tannin and trypsin inhibitor and resulted in different changes in the total amino acids and fatty acid contents. The animals maintained on the HCD showed remarkable decrease in the level of HDL-C associated with significant increase in the values of serum total lipid, total cholesterol, triglyceride, LDL-C, vLDL-C and the risk ratio in addition to serum concentration of urea, creatinine and uric acid in comparison with those of the control group. However, dietary supplementation of raw and treated soy flour resulted in reduction in the bad changes induced by HCD in the above mentioned parameters. In conclusion, treated soy flour supplementation in diet of rats pointed out to its hypocholesterolemic effect and its ability to improve lipid profile and kidney function of hypercholesterolemic rats.

The effects of dietary lipid and fibre levels on digestibility of diet and on the growth performance of sharpsnout seabream (Diplodus puntazzo)

In the present study, sharpsnout seabream (Diplodus puntazzo) were fed three experimental isonitrogenous diets composed of 45 g 100g-1 protein and varying lipid and fibre contents as follows: diet A: 45/10/1.5, B: 45/15/1.5 and C: 45/15/5. The effects of the diet composition were investigated by measuring digestibility, growth, carcass composition and haematological parameters. The apparent digestibility coefficients (ADCs) for proteins, fats and carbohydrates, measured at high (26˚C) and low (16˚C) water temperatures in laboratory conditions, were not affected by the diet or temperature treatments. Growth was evaluated in a seven-month trial using animals held in sea cages. The specific growth rate (SGR) showed no significant differences among the treatments while the feed conversion ratio (FCR) was significantly improved in the fish that were fed a low-fat diet. A significant increase in body fat was detected in the fish that were fed high-fat diets. The blood serum total lipid levels were elevated for the fish that were fed diet C. In conclusion, a diet containing a protein/fat/fibre ratio of 45/10/1.5 g 100g-1 can result in satisfactory growth and an improved FCR value when compared with diets with higher fat and/or fibre levels, demonstrating that the required fat level for sharpsnout seabream is lower than 15 g 100g-1.

Effects of 1,25 (OH)2 D3 Treatment on Lipid Levels in Uremic Hemodialysis Patients

The aim of this study was to evaluate the effect of 1,25 (OH)2D3 treatment on lipid levels in uremic hemodialysis (HD) patients. Thirty-one HD patients who had never been treated with vitamin D nor related drugs and 12 healthy subjects with normal renal functions were studied. Uremic HD patients were randomly divided into two groups. Sixteen uremic HD patients were treated with oral calcitriol (0.5 μg/day) for 8 weeks. 13 uremic HD patients and 12 healthy subjects were given placebo. In all these cases before and after 8 weeks of treatments; serum total lipid, total cholesterol, HDL-cholesterol, LDL-cholesterol and triglycerid levels were determined. After calcitriol treatment, triglycerid levels were significantly decreased. But total lipid, cholesterol, HDL-cholesterol and LDL-cholesterol levels did not significantly change. In the other two groups there were no significant changes. These results show that calcitriol treatment has a positive effect on triglycerid levels in uremic HD patients. This effect of mechanism of calcitriol treatment has not been known yet. But it could be due to regulation carbohydrates metabolism and normalization of parathormone (PTH) levels.