Browsing by Author "Azad, Md. Abul Kalam"

Traditionally P. macrocarpa fruits have been used as an herbal anti diabetic remedy for a long time in South-East Asia. The purpose of this study was to evaluate the cytotoxicity, acute oral toxicity and antidiabetic effects of Phaleria macrocarpa (EEPM) fruits in streptozotocin-induced Sprague-Dawley rat model. The plant fruits were extracted using 70% ethanol followed by cold maceration. Brine shrimp lethality bioassay, using sea water was prepared by dissolving 38 g sea salt in 1 liter distilled water for two days, this is allowed to hatch the shrimp to nauplii and potassium dichromate was used as a positive control. In an acute oral toxicity study, twelve male adult Sprague-Dawley rats (10 weeks) weighing 180-200 g were divided into Group-I (Control- 10% normal saline) and Group-II (extract), n=6. The fruit extract (5000 mg/kg/b.w) was given orally to each rat and observation carefully at 4 and 6 hr intervals for any physical changes. In antidiabetic study, a total of thirty-six healthy adult male rats were divided into six groups (n=6). Diabetes was induced under light ether anesthesia by a single dose (65 mg/kg/b.w) of intraperitoneally injected streptozotocin. Their glycemic status (Oral glucose Tolerance Test) was re-evaluated intermittently at 0, 30, 60, 90 and 120 min, respectively. Blood sugar level (mg/dl) and body weight of each rat in the respective groups were repeatedly measured on day 0, 7, 14, 21, 28 and 35 of the experiment. The findings of the present toxicity study suggest that the ethanol extract of EEPM fruits is non-toxic. It was found that the EEPM at 50, 100 and 200 mg/kg and glibenclamide (0.5 mg/kg) reduced the blood glucose level (hyperglycemia due to glucose load 2 g/kg p.o.) significantly after 2 hr of oral administration, when compared to the diabetic control group. The repeated oral administration of EEPM daily up to 35 days exhibited significant (p˂0.01) blood glucose activity in STZ-induced diabetic rats compared with diabetic control. At the end of 35 days of treatment, the blood glucose level of normal control, drug control and diabetic control was 132.16±5.79, 134.33±7.18 (p˂0.01) and 514.83±7.96 respectively. In the treatment groups, the dose of EEPM 200 mg/kg (392.66±3.2 to 174.33±4.3 mg/dl, p˂0.01) was shown to be more effective than EEPM 100 mg/kg (392.5±3.9 to 240.5±9.2, p?0.05) and EEPM 50 mg/kg 395.66±4.4 to 284.66±4.8 (p˂0.05). However, all selected doses showed antidiabetic activity gradually in STZ-induced diabetic rats. In histopathological examination results showed the pancreas of diabetic control were degranulated and dilated islet cells, whereas the drug control group showed granulated, nonappearance of dilation and hyperplasticity of islets. In treatment groups (EEPM at 100 and 200 mg/kg) also showed granulated pancreatic islets and prominent hyper plasticity islets. Light micrographs of rat kidney tissue in treatment groups showed various regions of the kidneys of treated animals with absence of matrix expansion and glomerular basement membrane thickening suggesting normal histoarchitecture of pancreas and renal. Biochemical aspects of the treated animal group were almost similar to the drug control group except the EEPM 50mg/kg group. In conclusion, EEPM may also serve as a good alternative in the present armamentarium of antidiabetic drugs. Keywords: P. macrocarpa, Toxicity, Antidiabetic, Histopathology, Kidney, Pancreas, Streptozotocin.

Black seed oil (BSO) have traditional claims and scientific evidences for therapeutic and pharmacological values. Similarly, peppermint oil (PO) has been used for a long time as a therapeutic agent for stomach related diseases. In conjunction with their therapeutic benefit, they have become an interest in utilization in pharmaceutical use. The key objective and major challenge of this study was to develop a pH sensitive BSO and PO loaded alginate bead as an intestinal release matrix system designed to release in the intestine without releasing the drug in the gastric fluid. To overcome these challenges, organic-solvent-free, green, and environmentally friendly electrohydrodynamic atomization (EHDA) technique was employed to prepare BSO and PO loaded alginate beads. This process enabled the formulation of small size and uniform beads with suitable diffusion, and swelling characteristic resulting in process performance enhancement. The current study deals with the development, optimization, and in vitro characterization of BSO and PO beads in different aspects like emulsion stability (ES), particle size distribution, zeta potential, yield percentage (Y%), physical appearance i.e. scanning electron microscopy (SEM), encapsulation efficiency (EE%), quantification of thymoquinone and menthol, shape, weight uniformity, ex vivo mucoadhesive properties, in vitro drug release profile, and gastrointestinal tract (GIT) beads distribution. Prior to that, the compatibility was tested using attenuated total reflectance-Fourier-transform infrared spectroscopy (ATR-FTIR) and differential scanning calorimetry (DSC). Then the optimized formulation was administered to evaluate the therapeutic efficacy as an anti-inflammatory effect of BSO and PO loaded beads in irritable bowel syndrome (IBS) in mustard oil (MO)-induced Sprague-Dawley rats. The results indicate that the voltage and flow rate have significant influenced on beads size and sphericity factor as well as on encapsulation efficiency. All prepared formulations (F1-F9) exhibited low release rate in simulated gastric fluid (SGF) (pH 1.2) within 2 h. However, all these beads (F1-F9) showed better drug release profile in simulated intestinal fluid (SIF) (pH 6.8) at the next 2 h. The optimized formulation (F8) has shown excellent ex-vivo mucoadhesive properties, well distributed in various parts of the intestine, well swelling behaviour and release in the SIF. BSO and PO-loaded alginate beads exhibited potential improvement of IBS on MO-induced rat compare to non-treatment group. These formulations were significantly suppressed proinflammatory cytokines like interleukin- IL-1β, IL-6, and TNF-α expression upregulated of anti-inflammatory cytokine (IL-10) expression in MO-induced intestinal inflammation. However, within the treatment groups, BSO-loaded alginate beads potentially upregulated the anti-inflammatory cytokine (IL-10) expression compared to other treatment groups. The combination of BSO (75 mg) and PO (25 mg) treatment group showed synergistic therapeutic effect by improving disease symptoms and suppressing IL-1β, IL-6, and TNF-α expression. The technique for the preparation of beads was found to be simple, reproducible, easily controllable, economical, and appeared to be a promising approach to control the bead’s nature and to ensure release into targeted site after oral administration. This formulation is considered as an anti-inflammatory drug candidate with possible synergistic effect for IBS treatment. Keywords: black seed oil, Peppermint oil, electrohydrodynamic technique, microencapsulation, inflammation, IBS.