Narayan Prasad Yadav

Hepatoprotective activity of leaves of Kalanchoe pinnata Pers.

Kalanchoe pinnata Pers. is naturalized throughout the hot and moist parts of India. Juice of the fresh leaves is used very effectively for the treatment of jaundice in folk medicines of Bundelkhand region of India. The juice of the leaves and the ethanolic extract of the marc left after expressing the juice were studied in rats against CCl(4)-induced hepatotoxicity. The test material was found effective as hepatoprotective as evidenced by in vitro, in vivo and histopathological studies. The juice was found more effective than ethanolic extract.

Synergistic effect of silymarin and standardized extract of Phyllanthus amarus against CCl4-induced hepatotoxicity in Rattus norvegicus

In search of the effective and standardized hepatoprotective combination therapy, silymarin and standardized extract of Phyllanthus amarus has been evaluated against CCl(4)-induced hepatotoxicity in rats. Eight groups of rats were used. The animals of group A served as normal and were given only vehicle. The animals of group B served as toxin control and were administered with CCl(4) (50% solution of CCl(4) in liquid paraffin, 2 ml/kg b.w., intraperitoneally). The animals of groups C-H received silymarin (100 mg/kg b.w.), Phyllanthus amarus aqueous extract (100 mg/kg b.w.), Phyllanthus amarus ethanolic extract (100 mg/kg b.w.), silymarin (50 mg/kg b.w.)+P. amarus aq. ext. (50 mg/kg b.w.), silymarin (50 mg/kg b.w.)+P. amarus eth. ext. (50 mg/kg b.w.) and marketed formulation (M.F.) 5 ml/kg b.w. for 6 days orally as well as CCl(4) (2 ml/kg b.w.) on 4th day intraperitoneally. The test materials were found effective as hepatoprotective as evidenced by plasma and liver biochemical parameters. The combination of silymarin and Phyllanthus amarus showed synergistic effect for hepatoprotection and silymarin with ethanolic extract of P. amarus showed better activity due to the higher concentration of phyllanthin in ethanolic extract in comparison to aqueous extract of P. amarus as estimated by HPLC.

In vivo anti-diabetic activity of derivatives of isoliquiritigenin and liquiritigenin

Isoliquiritigenin (ISL), a chalcone and liquiritigenin (LTG), a flavonoid found in licorice roots and several other plants. ISL displays antioxidant, anti-inflammatory, antitumor and hepatoprotective activities whereas LTG is an estrogenic compound, acts as an agonist selective for the β-subtype of the oestrogen receptor. Both the phenolics were isolated from the rhizomes of Glycyrrhiza glabra. Five derivatives from ISL and four derivatives from LTG were synthesized. All the compounds were established by extensive spectroscopic analyses and screened through oral glucose tolerance test to gain preliminary information regarding the antihyperglycemic effect in normal Swiss albino male mice. ISL (1), ISL derivatives 3, 4, 5, 7 and LTG derivatives 9 and 10 showed significant blood glucose lowering effect. The structure-activity relationship indicated that the presence of ether and ester groups in ISL and LTG analogues are important for exhibiting the activity. Compounds 1, 4 and 10 were selected for in vivo antidiabetic activity and found to be potential candidates for treatment of diabetes. It is the first report on antidiabetic activity of ISL derivative 4 and LTG derivative 10.

Efficient Hepatic Delivery of Drugs: Novel Strategies and Their Significance

Liver is a vital organ responsible for plethora of functions including detoxification, protein synthesis, and the production of biochemicals necessary for the sustenance of life. Therefore, patients with chronic liver diseases such as viral hepatitis, liver cirrhosis, and hepatocellular carcinoma need immediate attention to sustain life and as a result are often exposed to the prolonged treatment with drugs/herbal medications. Lack of site-specific delivery of these medications to the hepatocytes/nonparenchymal cells and adverse effects associated with their off-target interactions limit their continuous use. This calls for the development and fabrication of targeted delivery systems which can deliver the drug payload at the desired site of action for defined period of time. The primary aim of drug targeting is to manipulate the whole body distribution of drugs, that is, to prevent distribution to non-target cells and concomitantly increase the drug concentration at the targeted site. Carrier molecules are designed for their selective cellular uptake, taking advantage of specific receptors or binding sites present on the surface membrane of the target cell. In this review, various aspects of liver targeting of drug molecules and herbal medications have been discussed which elucidate the importance of delivering the drugs/herbal medications at their desired site of action.

Development and characterization of cellulose-polymethacrylate mucoadhesive film for buccal delivery of carvedilol.

The aim of the present work was to develop and characterize mucoadhesive film of cellulose (methyl cellulose and hydroxy propyl methyl cellulose) and polymethacrylate (Eudragit RSPO) polymers for buccal delivery of carvedilol. Drug and polymers were found to be compatible as revealed by FTIR and DSC analysis. Mucoadhesive films were prepared by solvent casting technique. Swelling studies up to 4h did not show erosion of film, which was further confirmed by SEM analysis. New, simple and precise instrumental methods were established for the evaluation of mucoadhesive strength (33.8 ± 0.37-38.4 ± 0.24 g) and film strength (331.2 ± 0.73-369.0 ± 1.00 g) of developed films. Mucoadhesive film F5 showed 88 ± 1.15% in vitro drug release and 80 ± 2.30% ex vivo drug permeation through goat buccal mucosa in 12h. Drug release and permeation followed Higuchis model and mechanism was found to be Fickian type diffusion controlled.

Development of cellulosic polymer based gel of novel ternary mixture of miconazole nitrate for buccal delivery.

Aim of the present investigation was to develop cellulosic polymer based mucoadhesive antifungal gel comprising novel ternary mixture of miconazole nitrate (MN) for buccal delivery. Crosslinking of gel was made by adjusting pH with triethanolamine (TEA) and gel formulation was optimized on the basis of flux of MN (0.562-1.751 mg/cm(2)/h) calculated from ex vivo permeation study. Based on statistically validated polynomial equation and plotted response surfaces, B17 was found to be the optimum batch. Texture profile in terms of adhesiveness (3.24 ± 0.012 g), firmness (10.83 ± 0.067 g), spreadability (3.63 ± 0.033 mJ) and extrudability (35.6 ± 0.1 mJ) of B17 was evaluated using a novel instrumental approach. The texture parameters were found to be consistent over 90 days. Ternary mixture containing gel showed broader zone of growth inhibition (32.67-47.33 mm) in comparison to marketed formulation containing pure MN (17.50-40.33 mm) against selected strains of fungi. In conclusion, consistent and effective mucoadhesive antifungal gel of MN with extended residence time in oral mucosa was developed.

Toxic effects of oral administration of extracts of dried calyx of Hibiscus sabdariffa Linn. (Malvaceae)

The effects of a 90‐day oral administration of water and alcohol extracts of dried calyx of Hibiscus sabdariffa were evaluated in albino rats. Haematological, biochemical and histopathological changes were monitored every 30 days.

Determination of required hydrophilic–lipophilic balance of citronella oil and development of stable cream formulation

Context: Citronella oil is reported to have excellent mosquito-repellent activity. To develop a stable cream formulation (emulsion), its hydrophilic–lipophilic balance (HLB) value is important. Objective: To determine required hydrophilic–lipophilic balance (rHLB) value of citronella oil and to develop stable cream formulation. Materials and Methods: Emulsions of citronella oil were prepared by phase inversion temperature technique using water, Tween 80 and Span 80. A first series of 11 emulsions with HLB values ranging from 5.0 to 15.0 and a second series of eight emulsions with smaller interval in HLB values from 11.0 to 13.8 were prepared. Emulsions were evaluated for creaming index, droplet size and turbidity to determine rHLB. Utilizing determined rHLB, citronella oil cream was formulated and evaluated for different texture parameters. rHLB of light liquid paraffin was also determined for validation of methodology. Results: rHLB of light liquid paraffin and citronella oil was determined to be 11.80 and 12.60, respectively. Stable citronella oil cream was developed with 10% emulsifier blend. Texture parameters were found to be consistent over the entire storage period. Discussion: Creaming index, droplet diameter, percent increase in droplet diameter and turbidity are the established parameters to determine rHLB and to develop stable emulsion. Emulsions with optimum emulsifier concentration resulted in less percentage creaming index, smallest droplet, less percentage increase in droplet diameter and highest turbidity. Texture properties evaluation ensures the stability of the developed cream. Conclusion: rHLB value of citronella oil was found 12.6 and a stable cream was formulated utilizing determined rHLB.

Novel drug delivery system: an immense hope for diabetics

Abstract Context: Existing medication systems for the treatment of diabetes mellitus (DM) are inconvenient and troublesome for effective and safe delivery of drugs to the specific site. Therefore, investigations are desired to deliver antidiabetics using novel delivery approaches followed by their commercialization. Objective: The present review aims to provide a compilation on the latest development in the field of novel drug delivery systems (NDDSs) for antidiabetics with special emphasis on particulate, vesicular and miscellaneous systems. Methods: Review of literature (restricted to English language only) was done using electronic databases like Pubmed® and Scirus, i.e. published during 2005–2013. The CIMS/MIMS India Medical Drug Information eBook was used regarding available marketed formulation of antidiabetic drugs. Keywords used were “nanoparticle”, “microparticle”, “liposomes”, “niosomes”, “transdermal systems”, “insulin”, “antidiabetic drugs” and “novel drug delivery systems”. Single inclusion was made for one article. If in vivo study was not done then article was seldom included in the manuscript. Results: The curiosity to develop NDDSs of antidiabetic drugs with special attention to the nanoparticulate system followed by microparticulate and lipid-based system is found to emerge gradually to overcome the problems associated with the conventional dosage forms and to win the confidence of end users towards the higher acceptability. Conclusion: In the current scientific panorama when the area of novel drug delivery system has been recognized for its palpable benefits, unique potential of providing physical stability, sustained and site-specific drug delivery for a scheduled period of time can open new vistas for precise, safe and quality treatment of DM.

New Perspectives on Antiacne Plant Drugs: Contribution to Modern Therapeutics

Acne is a common but serious skin disease, which affects approximately 80% adolescents and young adults in 11–30 age group. 42.5% of men and 50.9% of women continue to suffer from this disease into their twenties. Bacterial resistance is now at the alarming stage due to the irrational use of antibiotics. Hence, search for new lead molecule/bioactive and rational delivery of the existing drug (for better therapeutic effect) to the site of action is the need of the hour. Plants and plant-derived products have been an integral part of health care system since time immemorial. Therefore, plants that are currently used for the treatment of acne and those with a high potential are summarized in the present review. Most active plant extracts, namely, P. granatum, M. alba, A. anomala, and M. aquifolium exhibit minimum inhibitory concentration (MIC) in the range of 4–50 µg/mL against P. acnes, while aromatic oils of C. obovoides, C. natsudaidai, C. japonica, and C. nardus possess MICs 0.005–0.6 μL/mL and phytomolecules such as rhodomyrtone, pulsaquinone, hydropulsaquinone, honokiol, magnolol, xanthohumol lupulones, chebulagic acid and rhinacanthin-C show MIC in the range of 0.5–12.5 μg/mL. Novel drug delivery strategies of important plant leads in the treatment of acne have also been discussed.