Preparation and Characterization of Natamycin Loaded Bioadhesive In Situ Ophthalmic Gel for Enhanced Bioavailability

Natamycin is used in the antifungal preparation of eye drops. The eye drop needs frequent installation into the eye and also having poor bioavailability. The present study was planned to formulate and characterized in situ ophthalmic gel of Natamycin by using a blend polymer of sodium alginate, ethylcellulose, and Xanthan gum for better residence time and bioavailability of the drug. The six different formulations (F1 to F6) of Natamycin in situ gel were prepared. All the formulations were evaluated for clarity, visual appearance, pH, gelling capacity, drug content, assessment of drug release, kinetic modeling, ocular irritancy, and stability study. The results were found to have complied with the Pharmacopoeial specification. The in vitro drug releases of F3 established maximum drug release for 8 hrs compared to other formulations and showed sustained release. Further, the F3 was stable and showed non-irritant and safe to use. The studies suggested that prepared in situ ophthalmic gel of Natamycin will be an alternative for conventional eye drops and a valuable alternative to counter the precorneal loss

Ultra Flexible Nanocarrier for Enhanced the Ocular Delivery of Quercetin in Management of Macular Edema

Quercetin (Que) and its derivatives are naturally taking place phytochemicals with promising bioactive belongings. The antidiabetic, anti-inflammatory, antioxidant, antimicrobial, anti-Alzheimer’s, antiarthritic, cardiovascular, and wound-healing possessions of Que have been extensively investigated, as well as its anticancer commotion against different cancer cell lines has been newly reported. Que and its derivatives are found predominantly in the Western starve yourself, and people might benefit from their defensive effect just by taking them via diets or as a food enhancement. Bioavailability-related drug-delivery systems of Que have also been markedly exploited, and Que nanoparticles become visible as a promising proposal to enhance their bioavailability. The present review aims to make available a brief overview of the therapeutic things, new insights, and forthcoming perspectives of Que. Plants and plant parts are used for its aroma, flavor, or therapeutic properties. There are a number of recompense associated with using plants and plant phytoconstituents as contrasting to pharmaceutical merchandise

Formulation Development and Evaluation of Bilayer Tablet for Effective Treatment of Gastric Ulcer

The present study was aimed at developing Gastro retentive bilayer drug delivery systems containing esomeprazole and clarithromycin for the treatment of H. pylori induced gastric ulcer to minimize the side effect, improve the prolongation of action, to reduce the frequency of drug administration. The tablet is characterized by immediate release layer of esomeprazole and Gastroretentive layer of clarithromycin. The formulation containing Gastroretentive layer was designed using HPMC K 15, HPMC K4 and PVP K30 as floating agents, sodium bicarbonate and citric acid as gas-generating agent. Crospovidone, sodium starch glycolate and croscarmellose sodium was used as superdisintegrant for the preparation of immediate release layer. The prepared Gastroretentive layer was evaluated for their precompression parameters, physical characteristics like hardness, friability, uniformity of weight, uniformity of drug content, swelling index, In-vitro floating studies and In-vitro drug release. The release of the esomeprazole from the immediate release layer was found to be 89.98 % in 15minutes. The release of clarithromycin for the sustained release floating layer was found to be 98.89±0.47% in 12 hours. The data obtained from In-vitro release were fitted into the various kinetic models (Zero Order, Higuchi, First Order and Korsmeyer–Peppas Model). Keywords: Esomeprazole, Clarithromycin, Bilayer floating tab, Crospovidone, Superdisintegran

Furanoflavones pongapin and lanceolatin B blocks the cell cycle and induce senescence in CYP1A1-overexpressing breast cancer cells

© 2018 Elsevier Ltd Expression of cytochrome P450-1A1 (CYP1A1) is suppressed under physiologic conditions but is induced (a) by polycyclic aromatic hydrocarbons (PAHs) which can be metabolized by CYP1A1 to carcinogens, and (b) in majority of breast cancers. Hence, phytochemicals or dietary flavonoids, if identified as CYP1A1 inhibitors, may help in preventing PAH-mediated carcinogenesis and breast cancer. Herein, we have investigated the cancer chemopreventive potential of a flavonoid-rich Indian medicinal plant, Pongamia pinnata (L.) Pierre. Methanolic extract of its seeds inhibits CYP1A1 in CYP1A1-overexpressing normal human HEK293 cells, with IC50 of 0.6 µg/mL. Its secondary metabolites, the furanoflavonoids pongapin/lanceolatin B, inhibit CYP1A1 with IC50 of 20 nM. Although the furanochalcone pongamol inhibits CYP1A1 with IC50 of only 4.4 µM, a semisynthetic pyrazole-derivative P5b, has ∼10-fold improved potency (IC50, 0.49 μM). Pongapin/lanceolatin B and the methanolic extract of P. pinnata seeds protect CYP1A1-overexpressing HEK293 cells from B[a]P-mediated toxicity. Remarkably, they also block the cell cycle of CYP1A1-overexpressing MCF-7 breast cancer cells, at the G0-G1 phase, repress cyclin D1 levels and induce cellular-senescence. Molecular modeling studies demonstrate the interaction pattern of pongapin/lanceolatin B with CYP1A1. The results strongly indicate the potential of methanolic seed-extract and pongapin/lanceolatin B for further development as cancer chemopreventive agents

Modification of natural hydrocolloid as disintegrant in aceclofenac tablet formulation

The purpose of present exploration was to modify kappa (k)-Carrageenan, by crosslinking, and assessed it as a tablet disintegrant to strengthen the solubility of the drug (aceclofenac) in tablet formulation. Modified k-Carrageenan was synthesized by reacting it with epichlorhydrin at heterogenous  conditions. The swelling action of the product was investigated in order to optimize reaction circumstances for chemical cross-linking. Best modified k-Carrageenan procured by optimizing the reaction conditions and it was characterized for swelling index, particle size distribution, solubility, viscosity, gel strength and Fourier transform infrared spectroscopy (FTIR). Influence of modified k-Carrageenan on dissolution profile of therapeutic was also investigated along with other evaluation parameters. Modified k-Carrageenan exhibiting significant swelling index which is comparable to that of superdisintegrants. On comparative investigation as a tablet disintegrant by preparing anhydrous dicalcium phosphate tablet, modified k-Carrageenan showed disintegration time less than 20 seconds. Dissolution of aceclofenac (Class II) tablet formulaion utilizing modified k-Carrageenan was comparable with commercially available superdisintegrants. Faster dissolution of the accommodated drug was achieved with modified k-Carrageenan which was comparable with dissolution of the tablet formulation containing other superdisintegrants. The competent concentration of k-Carrageenan was found to be 5-15% as tablet disintegrant. Modified k-Carrageenan might be encouraging tablet disintegrant in fast dissolving formulations and can be worn in direct compression method. Keywords: k-Carageenan. Epichlorhydrin. Aceclofenac. Crosslinking. Superdisintegran

Pharmacognostical and Phytochemical Investigations on Ipomoea pes-caprae Linn R. Br.

Ipomoea pes-caprae Linn is commonly used as a first aid to treat jelly-fish stings and in ritual baths to alleviate evil spirits. The leaves were used against pain, inflammation, rheumatism and as stomachic and tonic. The present study was designed to investigate pharmacognosy and phytochemistry of Ipomoea pes-caprae its proper investigation and chemical profiling. Powdered plant extracts were subsequently soxhleted using petroleum ether (60-800C), methanol and water. Swaras was prepared from fresh plant extracts and studied for their phytochemical parameters and freshly prepared powder of I. pes-caprae was studies for its macroscopy for developing its identification parameters. Physicochemical study on I. pes-caprae herb yielded total ash (16.23%), acid insoluble ash (2.16%) and water soluble ash (13.48%) and value for loss on drying was (19.35%). Successive solvent extractive values of its powder were found to be 3.75 % w/w for petroleum ether (60-800C), 5.35 % w/w for methanol and 11.45 % w/w for aqueous extract and the value for swaras was 13.25 % w/w. Phytochemical screening on extracts and swaras revealed the presence of alkaloids, flavonoids, tannins, sterols, terpenoids and glycosides. Pharmacognostic characters, phytochemical values and macroscopic characters taken together as the outcome of this study could be used as the diagnostic tools for identification and standardization of I. pes-caprae for its purity and authencity

Study the Effect of Phytochemical Constituents of Piper betel Leaves Extracts on Liver Disorders by in vivo Model

ABSTRACT An in vivo study was conducted to evaluate the hepatoprotective activity of ethanolic extracts of Piper betel leaves. Liver damage was induced in male Wistar rats weighed 150-200 gm by administering CCl 4 (2ml/kg i.p) regularly for 10 days and tissue damage was noted by various biochemical parameters like serum glutamate oxaloacetate transaminase (SGOT), serum glutamate Pyruvate transaminase (SGPT), Alkaline Phosphatase (ALP), Acid Phosphatase (ACP), Lipid peroxidation, Level of antioxidant enzyme like catalase (CAT), Superoxide dismutase (SOD), Glutathione (GSH) in liver. Ethanolic extract of piper betel 100 mg/kg and 200 mg/kg i.p administered regularly for 10 days and compared with a control group silymarin (25 mg/kg i.p.). A significant reduction in serum SGOT, SGPT, ALP, ACP, lipid peroxidation and improvement in CAT, SOD, GSH, MDA level in the liver were observed when compared with CCl 4 administered rats. Piper betel leaves extract (PBLE) was able to protect the liver against the oxidative damage produced by CCl 4