The major limitation with the oral administration of most of the phytochemicals is their low aqueous solubility and bioavailability. Thymoquinone (THQ) is one of the most widely used phytochemicals used to treat a variety of diseases. However, strong lipophilic characteristics limit its clinical application. Therefore, this study was aimed to design novel chitosan (C) modified polycaprolactone (PL) nanoparticles (NPs) for improved oral bioavailability of THQ. THQ-CPLNPs was optimized 33-Box–Behnken design. After that, the optimized THQ-CPLNPs was characterized by different parameters. THQ-CPLNPs showed the size, PDI, and ZP of 182.32 ± 6.46 nm, 0.179 ± 0.012, and +21.36 ± 1.22 mV, respectively. The entrapment and loading capacity were found to be 79.86 ± 4.36%, and 13.45 ± 1.38%, respectively. THQ-CPLNPs exhibited burst release in initial 2 h followed by prolonged release up to 24 h in simulated intestinal fluids. THQ-CPLNPs showed excellent mucoadhesion properties which were further confirmed with the intestinal permeation study as well as confocal microscopy. The study revealed higher permeation of THQ-CPLNPs compared to neat THQ suspension (THQ-S). Moreover, in vivo gastric irritation study revealed good compatibility of THQ-CPLNPs with the gastric mucosa. Furthermore, pharmacokinetic results depicted ∼3.53-fold improved oral bioavailability of THQ from THQ-CPLNPs than THQ-S. Therefore, from the findings, it was concluded that the prepared polymeric NPs could be an effective delivery system for improved oral bioavailability of THQ.

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Background: Putranjiva roxburghii Wall is traditionally known to cure many pathological conditions including epilepsy. Objective: The present study is aimed at determining bioactive compounds in ethanolic extract of Putranjiva roxburghii test extract (PRTE) seeds by GCMS analysis and to assess its anti-epileptic potential using various experimental models of epilepsy. Methods: The ethanolic extract of seeds of Putranjiva roxburghiiwas subjected to GC-MS analysis to detect the bioactive phytoconstituents. Acute oral toxicity of the extract was performed using OCED guideline 420. Pentylenetetrazol (PTZ) kindling model of epilepsy and Maximal electroshock epilepsy (MES) model of epilepsy were used to determine antiepileptic potential. Results: The GC-MS analysis of the extract revealed the presence of 20 phytoconstituents. The major phytoconstituents included n-Propyl heptyl ether (25.25%), 5-Ethyl hydantoin (8%), octadec-9-enoic acid (16-25%) and 1, 2-Benzene dicarboxylic acid (11.86%). The PRTE (50 mg/kg and 100 mg/kg) afforded significant and dose - dependent protection against PTZ – induced kindling epilepsy and MES induced epilepsy (p<0.001 and p<0.01). Conclusion: Based on the above finding, it is evident that Putranjiva roxburghii seeds contain biologically active compound. It can also be concluded that the extract possesses anti-epileptic potential.

Aim: The present work deals with the GC-MS-analysis of chemical constituents of hydroalcoholic extract of Cissampelos pareira leaves and thier anti-diabetic activity. Methods: GC-MS analysis of extract was performed using Shimadzu QP-2010 plus with thermal desorption system 20. Acute oral toxicity of extract was done using the Organization of Economic Co-operation and Development (OECD) guideline 423. Diabetes was induced by single dose of streptozotocin 65 mg/kg, i.p. to all the rats except in rats of control group. Following which oral glucose tolerance test was performed and the rats were divided into various experimental groups. Various treatments continued for 21 days. Parameters such as blood glucose level, body weight, liver enzymes, lipid profiles and oxidative markers were checked. Results: GC-MS analysis of the extract identified 25 compounds present in it. Based on acute oral toxicity study three doses of hydroalcoholic extract of Cissampelos pareira leaves viz 100, 200 and 400 mg/kg were selected for evaluation of anti-diabetic activity. The extracts at doses 200 and 400 mg/kg BW were able to reduce blood sugar level, liver enzymes, total cholesterol, total triglyceride, low density lipoprotein and Malondialdehyde; and enhance body weight, high density lipoprotein and Glutathione significantly when compared to rats of negative control group. The effect of extract at dose 400 mg/kg was comparable to standard Glibenclamide. Conclusion: Results conclude that the chemical constituents present in the hydroalcoholic extract of Cissampelos pareira contained some anti-diabetic compounds possessing strong anti-diabetic activity.

Background: The extensive search for a novel therapeutic agent against Alzheimer's Disease (AD) in medical and pharmaceutical research still continues. Despite a lot being explored about its therapeutics, there is still much more to learn in order to achieve promising therapeutic agents against ADAlzheimer's. Phytochemicals, especially secondary metabolites, are the major focus of the investigators for AD treatment. Objective: To describe major therapeutics targets of AD and the role of isothiocyanates (ITCs) in modulating these targets. Methods: Scientific databases, including Elsevier, Science Direct, Pub med, were explored. The explored literature was mainly journal publications on pathogenesis and targets of AD, and the effect of various ITCs in the modulation of these targets. Results: The major targets of AD include the Nrf-2/ARE signaling pathway, MAPKs pathway, GSK-3 signaling, and Ubiquitin-Protease system. ITCs, such as Sulforaphane, Allyl isothiocyanates, Moringin, 6-(methylsulfinyl) hexyl ITC, Phenethyl isothiocyanates, and Erucin, were reported to exert a protective effect against AD via modulating one of the several above mentioned targets. Conclusion: This article gives a detailed description of the therapeutic targets of AD and sheds light that phytochemicals, such as ITCs, can exert a protective effect against AD by targeting those pathways. However, properly designed research and clinical trials are required to include ITCs as a mainstream agent against AD.