International Journal of Pharmaceutical Sciences and Drug Research

278-283

Authors: Rajesh Nagar*, Rakesh Patel

The traditional system of medicine is so ingrained in our culture that, about 75% of the Indian population depends on this indigenous system for relief. With such a huge section of an ever increasing population relying on herbal remedies, it is imperative that the plant products which have been in use for such a long time be scientifically supported for their efficacy. Diabetes a metabolic disorders is most frequent occurring disease in India. The present paper reports with the investigation of antidiabetic potential of Eugenia jambolana (Bark), Phyllanthus niruri (Whole plant), Momordica charantia Linn. (Seeds) and Nyctanthes arbor-tristis (Leaves).

289-298

Authors: Jyotsna Begani1, Jyoti Lakhani2, Dharmesh Harwani1*

The efficacy of an actinomycete strain JB66 recovered from a sand dune soil from the Bikaner district of the Thar desert in inhibiting the growth of various bacterial pathogens was studied. The type strains Staphylococcus aureus, Shigella flexneri, Klebsiella pneumoniae and the clinical isolates Escherichia coli, multidrug-resistant S. aureus and P. vulgaris were included in the antimicrobial assays. Polyphasic characterization of JB66 isolate revealed its identity as Streptomyces (MH762010). It showed 88.99-89.24% sequence similarity with the other members of this genus and share the maximum (88.89%) similarity with Streptomyces sp. ATSC13. The strain JB66 was found to produce a high amount of extracellular L-asparaginase, catalase, gelatinase, protease, tyrosinase and urease enzymes. The partial chemical categorization of the methanolic crude extract of the JB66 strain led to the preliminary identification of various metabolic compounds. The thin-layer chromatography fractionation revealed the presence of prodigiosin pigment or chandramycin, cephalosporin or zeatin, daidzein, demethoxy rapamycin, 4,6-dihydroxy-7-methoxyisoflavone, munumbicins and amiclenomycin like compounds. Bio-autography revealed that the metabolites localized at the Rf values of 0.40, 0.46 and 0.53 in TLC profile had the actual bioactive fractions. UV-VIS spectrum absorbance maxima at 288 nm revealed the presence of an aromatic nucleus.

305-317

Authors: Chandani Makvana*, Satyajit Sahoo

The present study was aimed to formulate, comparatively evaluate and optimize multiple lipid drug carriers of valsartan for oral controlled release to overcome the problems associated with the drug such as bioavailability, to reduce the dosage regimen, half life and to determine the appropriateness of niosomal formulation as a drug carrier. Ether injection method was chosen for the formulation of physically and chemically stable niosomes of valsartan. The formulation and process parameters were optimized by manufacturing placebo niosomes. Than drug loaded niosome was prepared by varying the concentration of span 60. The prepared nine formulations were evaluated for various parameters. Placebo niosomes were evaluated for appearance, odour, texture, creaming volume, pH and changes after 15 days. The medicated nine formulations were evaluated for organoleptic properties (appearance/color, odour), pH, total drug content, entrapment efficiency, mean particle size and polydispersibility index, zeta potential and In-vitro drug release. All formulations were off-white in color, odourless, and fluid in nature. It was stable and did not show sedimentation. The pH was found to be in the range of 4.6-5.4. Drug content was found in the range of 89.13 to 99.52. The Entrapment efficiency was found in range of 79.05 to 98.24. The mean vesicle size of drug loaded niosomes of the different batches ranged between 2.52-3.42μm. The polydispersvity index was in the range of 0.325 to 0.420 which indicates a narrow vesicle size distribution. The values of zeta potential were in the range of -20.29 mV to -30.55 mV which indicates that niosome had sufficient charge and mobility to inhibit aggregation of vesicles. All the nine formulations shows constant drug release in controlled manner up to 24 h. Formulation V7 was considered to be the best formulation as the % drug content (99.52 ± 0.97), % entrapment efficiency (98.24 ± 1.50) and % drug release at the end of 24th h (98.55) were high for V7. The optimized formulation V7 showed higher degree of correlation coefficient (r2) 0.9805 which indicates process of constant drug release from dosage form. The present study concludes that the prepared niosome is a convenient and efficiency carrier for the delivery of antihypertensive drug. Besides this, it provided controlled delivery of drug.

325-329

Authors: Raghavender Chenna*, Y. Padmanabha Reddy

Chronotherapy has been emerging as a novel technology in the field of pharmaceutical research. Delivery of drugs with respect to the circadian rhythm has gained greater importance in the diseases such as diabetes, asthma and hypertension in producing maximum therapeutic action. Present study focus on the formulation and evaluation of Nimodipine pulsatile release tablets with the incorporation of Eudragit pH sensitive polymers used for the chronotherapy of hypertension. Pharmacologically Nimodipine is an anti-hypertensive agent that acts by blocking the L and N-type calcium channels. Evaluation parameters for Nimodipine tablets included friability, drug content, bulk and tapped density, angle of repose and Carr’s index and drug release in vitro and in vivo.

337-342

Authors: S. Srikanth Reddy1, G. Suresh2*

The current research is aimed at developing liquid self-nanoemulsifying drug delivery system (liquid-SNEDDS) of Manidipine for enhanced solubility and oral bioavailability. The Manidipine SNEDDS are formulated with excipients comprising of Capmul MCM (oil phase), Transcutol P (surfactant) Lutrol L 300 as co-surfactant. The prepared fifteen formulations of Manidipine SNEDDS analysed for emulsification time, percentage transmittance, particle size, in vitro drug release, and stability studies. In vivo pharmacokinetic studies of the optimized formulation were carried out in Wistar rats in comparison with control (pure drug). The morphology of Manidipine SNEDDS indicates spherical shape with uniform particle distribution. The percentage drug release from optimized formulation F14 is 98.24 ± 5.14%. The particle size F14 formulation was 22.4 nm and Z-Average 23.3 nm. The PDI and zeta potential of Manidipine SNEDDS optimized formulation (F14) were 0.313 and-5.1mV respectively. From in vivo bioavailability data the optimized formulation exhibited a significantly greater Cmax and Tmax of the SNEDDS was found to be 3.42 ± 0.46ng/ml & 2.00 ± 0.05 h respectively. AUC0-∞ infinity for formulation was significantly higher (11.25 ± 3.45 ng.h/ml) than pure drug (7.45 ± 2.24ng. h/ml). Hence a potential SNEDDS formulation of Manidipine developed with enhanced solubility and bioavailability.

347-353

Authors: Mohini Bajaj, Sanju Nanda*

This study was conducted to develop, an High Performance Liquid Chromatography using photodiode array detector (HPLC-PDA) method to analyse the samples generated by the stress testing of antifilarial combination (albendazole and diethylcarbamazine citrate) in the solution state. The concept of Quality by Design (Design of Experiment, DoE) approach was used for the development. For the separation of the drugs and its degradation products (DPs), DoE was applied in two stages, i.e., primary parameter stage where factors having major effect were selected. This stage gives us CQA (Critical Quality Attribute) which along with minor factors affecting were varied to get the secondary design. For each of the stage a different design was selected; for primary stage IV optimal design (Response Surface Method) was selected whereas for secondary stage, Taguchi orthogonal array design was selected. The major primary parameters affecting the HPLC method as screened by preliminary studies were the buffer pH, organic modifier (methanol or acetonitrile), initial hold time (start of gradient) and gradient time. The primary stage was completed successfully. The results were compiled in form of resolution of peak from next peak and analysed by DoE. The process fixed the values for buffer pH (4.38), organic modifier (acetonitrile) and gradient time (30 min). The CQA from primary run was initial hold time. This parameter along with other parameters: initial and final concentration of organic modifier, buffer type (phosphate or acetate), buffer strength (mM) and oven temperature were further varied and samples withdrawn were analysed. The data of secondary design was compiled in the form of resolution (R), analysed by Design Expert and final value for secondary parameter for HPLC method were fixed. The resolution of the peaks for some secondary runs was sufficient reflecting some type of interaction between the drugs and/or degradation products.

358-369

Authors: Sandeep Dilip Kadam*, M. S. Kondawar

In the world cancer is the major cause of death. Adansonia digitata L is commonly called as baobab belongs to Family Bombacaceae. Due to the high cost and toxic side effects like Bone marrow suppression, hepatotoxicity, nephrotoxicity, Immunosuppression, teratogenicity etc. of chemotherapeutic agents. So, for the proper controlling on cancer the trends of people are moving towards natural therapies. In light to above, in present research A. digitata L is selected for evaluation of in-vitro anticancer activity based on its reported phytoconstituents of fruit and quantitation of active principle of it. The extracts of fruit pulp, seed, and its combination were obtained using solvents like water, ethanol and n-hexane by maceration technique (Aqueous) and Soxhlet extraction method (organic). This extracts were used for further research possesses phytochemical constituents like Carbohydrates, tannins, Saponins, vitamins, alkaloids, terpenoids, phenol, glycoside flavonoids, steroids, etc. in-vitro antioxidant activity were evaluated via free scavenging assay by using DPPH assay method. Further in-vitro anticancer activity was evaluated against three human cancer cell lines MCF-7 (breast cancer cell line), Hep-G2 (liver cancer cell line) and COLO-205 (colon cancer cell line) using Brine Shrimp Lethality Assay (BSLA), Tryphan Blue Dye Cell Exclusion Assay (TBDCEA) and MTT assay. The quantitation of active ingredients Vit. C and Squalene from extracts was done by using titration method and HPLC method respectively. Formulation possesses highest percent antioxidant capacity (49.36). In BSLA formulation possesses highest rate of percent mortality than other extracts. In TBCE assay and in MTT assay formulation gives more significant effect in Hep-G2 liver cancer cell line than remaining cell lines. These findings introduce A. digitata L as potentially useful as anti-cancer agent. Further research is required to elucidate its specific mechanism of action and exact active principle responsible for action.

376-381

Authors: Arti Kumari1*, Jainendra Kumar2

Glycyrrhiza glabra, commonly known as licorice, has traditionally been used in various medicinal preparations as expectorant, antimicrobial, antiviral, anticancer, anti allergic agent. It has also prominent role in skin whitening and has anti-inflammatory and esterogenic properties. This study aims to the characterization of the bioactive constituent glabridin in plant extract of Glycyrrhiza glabra in ethanol, methanol and ethyl acetate using UV-VIS and FTIR and HPLC. A wavelength scan (200-600 nm) by UV-Vis spectrophotometer was performed and the characteristic peaks were recorded. The scan confirmed presence of glabridin with λmax at 281 nm with a small number of additional phytochemicals indicated by the extra peaks. FTIR spectrum of 62% pure glabridin was compared to the spectra shown by the three extracts. Presence of glabridin in all the three extracts was corroborated by HPLC analysis with the retention time of 4.05 minute. Glabridin was also evaluated for its antibacterial activity against Propionibacterium acne, causative agent of Acne vulgaris and found to have the detrimental effect at concentration 500, 1000 and 1500 ppm.

387-392

Authors: G. C. Madhu1, Jaianand Kannaiyan2, Balaji Paulraj2, Veeramanikandan Veeramani1*

In regenerative medicine, nanotechnology plays a vital role in the diagnosis, the delivery of therapeutic drugs and the treatment of many diseases and disorders. Due to the growing need to develop environmentally friendly technologies in material synthesis, the biosynthesis of Iron Oxide Nanoparticles (IOP) has received considerable attention over the past decades. Therefore, the community is now looking back for traditional medicines for various diseases after the practice of allopathic drugs with tremendous side effects. There are an increasing number of biomedical applications for iron oxide nanoparticles; as such uses are essential for in-vitro characterisation and in-vivo to ensure the bio-safety of these particles. The main complication of diabetes due to frequent lipid peroxidation is liver damage and renal dysfunction, but treatment with Leucas aspera has a pronounced effect on these indicators, which protects the organs from further damage. The current research supports the traditional use of Leucas aspera against diabetes mellitus and cancer, as well as the safety, effectiveness and potency of Leucas aspera leaf extract's anti-diabetic and anti-cancer effect in the in-vivo model. The overall results reveal that Leucas aspera has the potential and can be a candidate of choice without side effect.

399-404

Authors: Bhupendra Vyas*, Y. S. Sarangdevot

The objective of the present investigation was to study the antidiabetic and diuretic potential of Anogeissus latifolia (A. latifolia) bark in experimental rats. The A. latifolia bark was extracted with hydro-alcoholic solvent by cold extraction method. Acute toxicity study was performed according to OECD 425 guidelines for hydro-alcoholic extracts of A. latifolia bark (ALBE). The dose of 150 mg/kg p.o. and 300 mg/kg, p.o. of ALBE was selected for further studies. Animals were prepared diabetic by administration of alloxan (120 mg/kg, i.p.). The albino rats were divided in to five groups for oral glucose tolerance test (OGTT) and alloxan induced anti diabetic model with six animals in each group. Diabetic animals were treated with hydro-alcoholic extract of A. latifolia bark for 20 days. The blood glucose level was estimated according to standard procedures. Diuretic activity hydro-alcoholic extracts of A. latifolia was evaluated by Lipshitz method. The result shows that hydro-alcoholic extract from bark of Anogeissus latifolia 300 mg/kg (ALBE-II) shown significant hypoglycemic activity as compared to glibenclamide and diabetic group. The ALBE does not exhibit significant diuretic activity which is considered as positive marker in diabetic phenomena. Hence in present study extract of A. latifolia posses antidiabetic activity. This study may be benchmark in future to use of this drug scientifically.

409-415

Authors: Sasikala Chenniyappan*, Geetharamani Durairaj, K Evetha

The study is planned to find the antimicrobial activity of the extract of Jania rubens and to isolate the bioactive compound against MRSA and VRSA. Jania rubens collected from Mandapam (Pudumadam) Coastal water, East coast of India and extracted with ethanol. Antibacterial activity of J. rubens was tested against gram positive, gram negative bacteria and drug resistant bacteria). The antibacterial activities were expressed as zone of inhibition, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) Identification of compounds from crude extract of J. rubens carried by column chromatography, thin layer chromatography and NMR analysis. Finally J. rubens could serve as useful source of new antibacterial agent.