Combination therapy with Hordeum vulgare, Elettaria cardamomum, and Cicer arietinum exhibited anti-diabetic potential through modulation of oxidative stress and proinflammatory cytokines.

Poly-herbal therapies for chronic diseases like diabetes mellitus (DM) have been practiced in south Asia for centuries. One of such therapies comprises of Hordeum vulgare, Elettaria cardamomum and Cicer arietinum that have shown encouraging therapeutic potential in the treatment of diabetes and obesity. Therefore, poly-herbal granules (PHGs) of this formula were developed and investigated for their anti-diabetic and anti-obesity potential in obese-diabetic rats. The developed PHGs were chemical characterized and the virtual molecular docking was performed by Discovery studio visualizer (DSV) software. For in-vivo experiment, obesity in rats was induced with high-fat high-sugar diet. After that, diabetes was induced by alloxan monohydrate 150 mg/kg i.p. injection. The diseased rats were treated with PHGs at 250, 500 and 750 mg/kg/day for four weeks. GC-MS analysis of PHGs demonstrated the presence of 1,3-Benzenedicarboxylic acid bis(2-ethylhexyl) ester and 1,2-Benzenedicarboxylic acid di-isooctyl ester and phenol, 2,4-bis(1,1-dimethylethyl). Molecular docking of these compounds demonstrated higher binding energies with receptor than metformin against α-amylase and α-glucosidase. PHGs exhibited a decline in body weight, HbA1c, hyperlipidemia, hyperglycemia, and insulin resistance in diseased rats. The histopathological examination revealed that PHGs improved the alloxan-induced damage to the pancreas. Furthermore, PHGs increased the SOD, CAT and GSH while and the decreased the level of MDA in the liver, kidney and pancreas of diseased rats. Additionally, the PHGs had significantly downregulated the TNF-α and NF-κB while upregulated the expression of NrF-2. The current study demonstrated that the PHGs exhibited anti-diabetic and anti-obesity potential through amelioration of oxidative stress, NF-κB, TNF-α, and NrF-2 due to the presence of different phytochemicals.

Development and Pharmacokinetic Evaluation of Novasomes for the Trans-nasal Delivery of Fluvoxamine Using Arachidonic Acid-Carboxymethyl Chitosan Conjugate.

Depression is the major mental illness which causes along with loss of interest in daily life, a feeling of hopelessness, appetite or weight changes, anger and irritability. Due to the hepatic first-pass metabolism, the absolute bioavailability of fluvoxamine (FVM) after oral administration is about 50%. By avoiding the pre-systemic metabolism, nasal delivery would boost bioavailability of FVM. Additionally, the absorption is anticipated to occur more quickly than it would via the oral route because of the existence of microvilli and high vasculature. A nonionic surfactant, cholesterol and an arachidonic acid-carboxymethyl chitosan (AA-CMCS) conjugate were used to develop FVM-loaded novasomes. To investigate the effects of surfactant concentration, AA-CMCS conjugate concentration and stirring speed on the novasomes' characteristics, a Box-Behnken design was used. The dependent variables chosen were zeta potential, polydispersity index and particle size. The AA-CMCS conjugate was confirmed by 1H-NMR and FTIR. Using Design Expert software (version 7; Stat-Ease Inc., Minneapolis, MN, USA), novasomes were further optimized. The chosen optimal formulation (NAC8) was made up of AA-CMCS conjugate, Span 60 and cholesterol. Particle size, zeta potential and PDI values for NAC8 formulation were 101 nm, -35 mV and 0.263, respectively. The NAC8 formulation's DSC and TGA analysis demonstrated that the medication had been uniformly and amorphously distributed throughout the novasomes. The NAC8 formulation showed 99% and 90% FVM release and permeation, respectively, and the novasome adherence time was 24 h. An improved antidepressant effect along with five-fold increase in bioavailability of FVM was observed after trans-nasal administration of NAC8 formulation compared to the reference commercially available Flumin® tablets. FVM-loaded novasomes administered via the nasal route may therefore constitute an advancement in the management of depression.

Optimization of ranitidine hydrochloride based on stability performance in directly compressible immediate and sustained release formulations.

Ranitidine hydrochloride (RTD), a moisture-sensitive drug, has issues of stability during shelf life especially when formulated through wet granulation method. In current study, RTD was blended with non-hygroscopic excipient like ethyl cellulose and compressed using direct compression method. The physical and physicochemical characteristics were evaluated including hardness, thickness, diameter, friability, weight variation, disintegration, dissolution and accelerated stability study to optimize findings. Subsequently, the optimized formulation was characterized for Fourier Transform Infrared (FTIR) analysis and in vitro drug release kinetics. The physical characterization was unaffected by polymer variation while the friability and weight variation were within the USP limits. In vitro drug release depicted that the release rate was sustained by increasing the amount of ethyl cellulose, with a 10% increase of ethyl cellulose 99.09% drug was released. FTIR analysis exhibited no interaction among the ingredients of the optimized formulation (E2). The optimized formulation followed Hixson-Crowell release kinetics. Formulation A5 displayed immediate release characters as plain uncoated formulation. Accelerated studies showed no significant change in the drug content. The RTD was successfully sustained to be released up to 6 h and accelerated stability showed that the optimized formulation (E2) containing 4% starch 1500 and 10% of ethyl cellulose, respectively, was stable up to 6 months.

Development and validation of RP-HPLC method for determination of Lornoxicam in rabbit's plasma.

A simple, rapid and accurate reverse phase high performance liquid chromatographic (RP- HPLC) method was developed for the quantification of lornoxicam in oral disintegrating tablets (ODTs) and in rabbit's plasma. C18 Hypersil™ column was used as stationary phase to separate the drug. Mobile phase methanol: acetonitrile: water (60:30:10) was run isocratically at flow rate of 1 mL/min at room temperature. Mean retention time was 4.23 minutes and minimum amount of lornoxicam that can be measured was 7 ng/mL in rabbit's plasma. Good linearity was observed in concentration range of 10-100 ng/mL with regression coefficient R2 value of 0.9989 and slope value 23773. As per ICH norms, developed method was validated in terms of interday, intraday precision, accuracy, specificity, limit of detection (LOD), limit of quantification (LOQ) and drug plasma stability studies. All the data obtained revealed that this method can be used for in-vitro and in-vivo determination of lornoxicam in various pharmaceutical preparations.

Evaluation of in vitro antioxidant capacity and reducing potential of polyherbal Coded capsules Arthitec 1 and Arthitec 2.

Free radicals are partially reduced form of metabolites of Nitrogen and Oxygen. These are highly reactive and potentially toxic compounds which are contributing factors in different chronic disease. The present study was aimed to determine antioxidant capability and reducing ability of coded polyherbal capsules (Arthitec 1 & Arthitec 2). DPPH (2,2'-diphenyl-1-picryl hydrazyl) assay is most commonly used method for gauging antioxidant capability of natural compounds. In this assay DPPH act as stable free radical which react with an antioxidant. For measuring reducing ability suspected antioxidant react with ferric tripyridyltriazine (Fe3± TPTZ) complex and convert ferric into ferrous. Results are evident that both capsule formulations Arthitec 1 & Arthitec 2 have promising antioxidant activity and reducing potential. Antioxidant potential of both coded capsules with varied concentrations (10, 50 and 100 µg/ml) were compared and in both cases scavenging activity and as well as reducing ability raised in a dose dependent manner just like standard Butylated hydroxyanisole (BHA).