International Journal of Pharmaceutical Sciences and Drug Research

432-443

Authors: Manisha Mandal*

Tremendous advances have occurred in recent decades in the development of safe and effective medications for the treatment of viral diseases. Currently there are more than 20 HIV drugs approved for use in humans. Combined chemotherapy has been found useful for a number of viral infections comprising drugs with different mechanism of action. HIV treatment guidelines recommend the use of two nucleoside reverse transcriptase inhibitors (NsRTIs) plus a third antiretroviral drug for treatment-naive patients with AIDS that include non-nucleoside reverse transcriptase inhibitors (NNRTIs; eg, efavirenz), ritonavir-boosted protease inhibitors (eg, darunavir, atazanavir), and integrase inhibitors (eg, raltegravir, dolutegravir). However emergence of drug resistant HIV variants and their dissemination impede proper treatment of AIDS. Preferred regimens as first-line treatment in patients with suboptimum adherence comprise drugs with improved potency, safety and infrequent selection for resistance-associated mutations. The present review stands for an update on facts and phenomena of present, past, and future use of antiretrovirals based upon the available documents in SCI and non-SCI journals.

451-455

Authors: Aruna Devi Mantena*, Basava Raju Dontamsetti, Archana Nerella

The aim of the present investigation was to develop, optimize and evaluate nanoemulsion of rifampicin to improve the solubility, stability and oral bioavailability. Rifampicin nanoemulsions were prepared by o/w nanoemulsion region of the phase diagrams, which were subjected to physical stability and phase separation tests. Prepared rifampicin nanoemulsions were evaluated for particle size, zeta potential, PDI and drug content. In vitro dissolution was performed by using dialysis bag method and morphology by transmission electron microscopy (TEM). Best results were obtained with the formulation which consisted of 10 mg of rifampicin, 15% w/w of sefsol 218, 25% w/w of tween 80, 15% w/w of tween 20 and 45% w/w of water. In vitro release studies revealed that 99.85 ± 1.85% was observed in 12h. TEM studies shows the globules are in spherical shape with dark surroundings. DSC studies revealed that no interaction between the drug and excipients. The optimized formulation was also subjected to stability studies according and was found to be stable for one month with no phase separation. These results indicated the potential of nanoemulsions of rifampicin could be promising to improve solubility, stability and oral bioavailability.

465-473

Authors: N. Yakubu1, A. Faridah2, S. Mohd Noor3, M. S. Mohamad Ali1, A. Syahida1*

Previously, curcumin analogue, 2, 6-bis (2, 5-dimethoxybenzylidene) cyclohexanone (BDMC33) with high anti-inflammatory activity was chemically synthesized in our laboratory to enhance the biological activity of curcumin. In this study, the toxicity and permeability activities of 2,6-bis(2,5-dimethoxybenzy-lidene)cyclohexanone (BDMC33) in Caco-2 cells was investigated. Toxicity effects using MTT assay and apparent permeability coefficient (Papp), uptake (UR) and efflux (ER) ratios, and mass balance of BDMC33 after permeation in Caco-2 cells for 180 min were evaluated in apical (A) to basolateral (B) and basolateral (B) to apical (A) directions. The similar analyses on 3-(2-fluoro-benzylidene)-5-(2-fluorocyclohexylmethylene)-piperidin-4-one; (EF-24) (check control) were also conducted. The 24 hr LC50 value for BDMC33 and EF-24 on Caco-2 cells were both 50 µM. The Papp value in A→B direction was 3.37 ± 0.47 cm/s (BDMC33) and 2.47 ± 0.15 cm/s (EF-24). Whereas in B→A direction, it was 1.9 ± 0.36 cm/s (BDMC33) and 1.8 ± 0.15 cm/s (EF-24) upon 120 min incubation. The UR and ER ratios calculated were 1.77% and 0.56%, respectively, and the mass balance calculated were 41-44% (BDMC33) and 31-34% (EF-24) in A→B and B→A direction. This study has suggested BDMC33 to be more absorbable than EF-24 in Caco-2 cells. Therefore, BDMC33 could be a leading feature, the anti-inflammatory agent, as it biological activities would be expected outside the intestine.

478-483

Authors: Santosh R. Butle1*, Padmanabh B. Deshpande2

A new simple, accurate, precise and selective stability-indicating high performance thin layer chromatographic (HPTLC) method has been developed and validated for simultaneous estimation of Telmisartan and Cilnidipine in combined tablet dosage form. The mobile phase selected was Toluene: Methanol: Glacial acetic acid (8: 2: 1, v/v/v) with UV detection at 260 nm. The retention factor for Telmisartan and Cilnidipine were found to be 0.38 ± 0.004 and 0.62 ± 0.007. The method was validated with respect to linearity, accuracy, precision and robustness. The drugs were subjected to stress condition of hydrolysis (acid, base), oxidation, photolysis and thermal degradation. Results found to be linear in the concentration range of 200-1400ng band-1 and 50-600ng band-1 for Telmisartan and Cilnidipine, respectively. The method has been successfully applied for the analysis of drugs in pharmaceutical formulation. The % assay (Mean ± S.D.) was found to be 100.79 ± 1.38 for Telmisartan and 99.55 ± 1.13 for Cilnidipine. The developed and validated stability indicating method can be used for assessing the stability of Telmisartan and Cilnidipine in bulk drug and pharmaceutical dosage form.

489-492

Authors: B. Jaikumar, R. Sharmila*

Andrographis paniculata (Acanthaceae) is an annual herb. It is found in Sri Lanka, and throughout the plains of India especially Tamilnadu, Maharashtra, Karnataka, and Orissa. Various medicinal properties like cholevetic, antidiarrheal, immunostimulant and anti-inflammatory have been attributed to this plant in the traditional system of Indian medicine. Further reported activities are hepatoprotective, antimalarial, anticancer, antihypertensive, antipyretic, antithrombotic and antidote for snake bites. The present study aimed to evaluate the anti-microbial activity for the isopropanol extract of A. paniculata against different bacterial strains such as E. coli, K. pneumoniae, P. vulgaris, S. pneumoniae, P. aeruginosa, S. aureus by determining inhibitory concentration and zone of inhibition. Minimum inhibitory concentration and zone of inhibition values and the high bioactive metabolites production was observed in different extracts of A. paniculata under different physical stress (Light and temperatures). The results revealed that, the isopropanol extract of A. paniculata is potent for inhibiting bacterial growth and various secondary metabolites production in dark condition at 37°C than other tested parameters.

376-383

Authors: Thillaivanan. S1*, Parthiban. P2, Kanakavalli. K3, Sathiyarajeshwaran. P4

Siddha medicine is one of the oldest medical systems in the world. This system is most commonly practicing in India especially in southern regions. Siddha medicines become popular nowadays because of various outbreaks of communicable and very infectious diseases like chikungunya, dengue, swine flu etc. These diseases of viral origin are very challenge to the modern world because of lack of ideal anti-viral therapy. Pandemic flu is different from ordinary flu because it’s a new flu virus that appears in humans and spreads very quickly from person to person worldwide. Because it’s a new virus, no one will have immunity to it and everyone could be at risk of catching it. This includes healthy adults as well as older people, young children and those with existing medical conditions. The polyherbal decoction Kapa Sura Kudineer (KSK) is a well-known one in this series next to Nilavembu kudineer (NVK). This KSK is introduced for the prevention and the management of Swine flu. And the people of Tamil Nadu are very attentive about this Siddha drug KSK because to prevent and protect from the deadly life threatening disease, Swine flu. Here, an attempt has been made to review the explored ethno pharmacological activities of the ingredients of KSK to strengthen the scientific facts favoring this formulation.

395-400

Authors: Srikant Pimple*, Akash Joshi, Pravin Maurya, Astik Swami, Mahesh Digge, Ruby Singh

Olmesartan Medoxomil blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively binding to the AT1 angiotensin II receptor. ACE inhibitor is used in treatment of hypertension. The objective of the present study was to formulate an immediate release tablet of an antihypertensive drug, Olmesartan Medoxomil. Pre-formulation studies were carried out and results were within the limits. Tablets of Olmesartan Medoxomil were initially prepared by direct compression approach which resulted in poor flowability of the blend. Then the tablets were prepared by wet granulation techniques and the dissolution observed was on lower side. To obtain the desired dissolution pattern various trials had been taken with different excipients. Tablets were evaluated for their weight, hardness, friability, drug content, in-vitro dissolution. Similarity and dissimilarity factor were also calculated for Olmesartan Medoxomil with reference tablet. Stability study indicates that the formulation was stable.

407-411

Authors: V. Eugin Amala*, M. Jeyaraj

Terminalia chebula, Terminalia bellirica, Phyllanthus emblica and their formulations are used as a phytotherapeutic medicine for hepatic diseases. In the present study the effect of methanolic extract of herbal powder was administered against Imidacloprid in Albino Wistar Rats. Single dose of herbal (500 mg/kg/b.w) was given orally for 28 days to Imidacloprid toxicity exposed to rats. They were observed each hour and each day for 28 days for any changes in behavioural activity loss of ability to move, cramping, lethargy, muscle weakness, convulsion, irritation of the eye, excess salivation, change in gait. Clinical observations body weight, organ weight, biochemical analysis and histopathological examination were carried out. Administration of Imidacloprid, produced liver degeneration such as cytoplasmic vacuolation, mild vacuolar degeneration, mild hepatic damage in low dose (40 mg/kg b.w) and appearance of blood streaks, hepatic damage and severe vacuolar degenerations were observed in high dose of induction (80 mg/kg b.w). Animals were treated with the phytotherapeutic products of Terminalia chebula, Terminalia bellirica, Phyllanthus emblica and their formulations. Triphala extract was possessed more hepatoprotective activity, while comparing the four samples which was proved experimentally.

417-420

Authors: R. Bhatt, S. Sharma, A. K. Patidar, K. K. Rathore, R. C. Senwar, A. Mehta*

In the present investigation, synthesis of 4-(1-(3-chlorobenzo[b]thiophene-2-carbonyl)-1H-indol-3-yl)-7, 7-dimethyl-3, 4, 7, 8-tetrahydroquinazoline2, 5(1H, 6H)dione (3a-d) is described. These unreported compounds are obtained starting from indole- 3-aldehyde and3-chloro-1benzothiophene-2-carbonylchloride (1a-d). A series of compounds (3a-d) were prepared. The structures of the newly synthesized compounds were elucidated on the basis of IR and 1H NMR spectral data of the compounds. All the compounds have been screened for antibacterial activity against S. aureus, E. coli, and P. aeruginosa and for antifungal activity against Candida albicans, A. niger, and A. clavatus using broth dilution method and they were found to exhibit good to moderate antimicrobial activity.

425-431

Authors: Poovizhi. J1*, Krishnaveni. B2

The aim of the study was to compare the yield, nature and antimicrobial activity of nanoparticles synthesized using Calotropis procera leaf extract. ZnO NPs synthesized were characterized by FTIR and SEM. It was evident from SEM images that the size of the particles obtained by biological method is ranging from 100-200 nm. Antibacterial study was carried out on human bacterial and plant bacterial pathogens and their MIC values were determined. The antibacterial activity towards human bacterial and plant pathogen showed good sensitivity towards the green synthesized ZnO NP’s at all concentrations and maximum zone of inhibition occurred at the concentration of 30μg/mL. Minimum Inhibitory concentrations of NPs against human pathogenic bacteria and plant bacterial pathogens, shows that all tested microorganisms were completely inhibited at the concentration of 50 to 12.5μg/ml of nano-ZnO. The antifungal activity of ZnO NPs against fungi shows that different concentration of ZnO nanoparticles caused significant inhibition in the spore germination.

308-314

Authors: D. Nagasamy Venkatesh*, H. C Kiran, S. Shashikumar, V. Indurekha, K. J Thirumalai Subramaniam, A. Uma Rani

Dendrimers are synthetic, highly branched, monodisperse macromolecules of nanometer dimensions with exact and large number of functional groups, distributed with unprecedented control, makes them a promising scaffolds, for drug delivery. Dendrimers serves as an ideal vehicle for cancer therapy, immunology, vaccines, antivirals, biosensors for diagnostics, neuron capture therapy, photodynamic therapy and photo thermal therapy. Dendrimers chemistry is one of the most fascinating and rapidly expanding areas in the field of chemistry. Prior to the dendrimer technology, nanoparticle drug delivery systems were one of the choicest systems owing to their selectivity and stability of therapeutic agents incorporated into the system. However, few drawbacks such as reticuloendothelial system (RES) uptake, drug leakage, immunogenicity, hemolytic toxicity, cytotoxicity, hydrophobicity etc., impede the usage of these nanostructures. Further, these shortcomings shall be circumvented by modifying the surface engineering, such as poly ester dendrimer, arginine dendrimer, glycol dendrimer, PEGylated dendrimers etc., Unique properties of uniform size, water solubility, modifiable surface functionality and availability of internal cavities makes them intriguing carrier for biological and drug delivery system. In the present review, we focused on the bioactive agents that can be easily encapsulated into the interior cavity (or) chemical attachment, conjugation (or) physically adsorbed on to the dendrimer surface to serve the desired properties of the carrier to cater specific needs of the active components, its characterization and application.

321-328

Authors: Karva G. S.1*, Katariya V. R.2, Shahi S. R.1

The aim of present work was to improve the dissolution rate of Ritonavir by preparing micro-particles with certain hydrophilic polymers via spray drying technique. Role of spray drying method was studied for solubility enhancement of poorly aqueous soluble model Ritonavir using solid dispersion approach. All the carriers showed dissolution improvement vis-à-vis pure drug in varying degrees. The solid dispersions were characterized in comparison with pure drug and corresponding Physical mixture (PM). The prepared solid dispersion were evaluated by drug content analysis, saturation solubility, DSC (Differential scanning calorimeter), SEM (Scanning electron microscopy), PXRD (Powder X-ray diffraction), FTIR (Fourier transform infrared spectroscopy).and in vitro drug release. Absence of pure drug peaks in PXRD suggests transformation of crystalline drug into an amorphous form. The transformation of Ritonavir from crystalline to amorphous state by spray drying and the hydrophilic coating of drug particles by the polymers are considered for improvement of Solubility and dissolution of Ritonavir.

334-339

Authors: Dharmik D Patel1*, Ketan P Modi2, Anil K Patel3

The present study was conducted to find out the changes in immunosuppressant drug prescription pattern and trends in kidney transplant patients. In this study 613 Indian transplant patients who underwent kidney transplantation between July 2004 and June 2011 were enrolled. Various data of all transplant patients including immunosuppressant drug medication, changes in the prescription, use of antibody for induction and antirejection treatment were collected during their hospital stay and ambulatory visit. Antibody use as an induction agent has increased from during the study period. Induction was used in 23.1% during the year 2005 and increased to 44.4% during the year 2009. Among induction agent ATG was most commonly preferred agent, followed by daclizumab and basiliximab (24% ATG Vs 6.9% daclizumab Vs 6.9% basiliximab). Use of tacrolimus has increased (94% on tacrolimus vs 6% on cyclosporine in 2010). Mycophenolate mofetil is most commonly used antiproliferative agent (80% on MMF vs 20% on azathioprine in 2010). Trend is towards more use of MMF though azathioprine is being used in significant number of patients. Analysis of maintenance immunosuppression after renal transplant showed 60% patient maintained their original regimen over 7 years of follow up. Sirolimus was introduced in 1.5 to 7% patients during follow up period. Anti rejection treatment was required in 22-47% renal transplant recipients and trend towards decreasing rejection episode was seen. Steroids were used in the treatment of rejection in 90-100% patients. Use of ATG for treatment of rejection has increased from 11.5% in 2005 to 40% in 2010-11. By this study we conclude that immunosuppressant drugs have passed through significant changes during the year 2005 to 2011. Use of ATG as an induction agent and for treatment of rejection has increased. Similarly MMF and tacrolimus are most commonly used in maintenance regimen for renal transplant patients.

345-348

Authors: Praveen R.P.*, Ashalatha S Nair

Myxopyrum smilacifolium is a large woody climbing shrub belonging to the family Oleaceae which is known for many medicinal properties. In the present study, initially a short term cytotoxic study (3 hours) with hepatocarcinoma cell line HepG2 using Trypan Blue Assay was carried out against methanolic extracts of root and callus and found an appreciable result for both extracts. Then the study was extended to the same cell line employing MTT assay. In this procedure extracts were subjected to 24 hours treatment and cytotoxicity was measured using a colorimetric method based on the ability of metabolic active cells to cleave the yellow tetrazolium salt MTT to an insoluble purple formazan crystal. A concentration dependent activity was observed in both Trypan Blue as well as MTT assay. The results showed that both the extracts possess potent cytotoxic activity. IC50 value from MTT assay was found to be 63.75µg/l and 98.75µg/l for root and callus extracts respectively. To the best of our knowledge, this is the first study to demonstrate the cytotoxic potential of callus extracts of Myxopyrum smilacifolium Blume.

354-360

Authors: Samir Baniya1*, Dhananjaya D.R.1, Ankit Acharya2, Bishal Dangi1, Arjun Sapkota1

The present study was designed to evaluate the cardioprotective potential of Citrus grandis (L.) Osbeck (CGO) peel extract in rats. Citrus grandis (L.) Osbeck peel extract was evaluated for protection against cyclophosphamide (200 mg/kg body wt., i.p.) and doxorubicin (15 mg/kg body wt., i.p.) induced cardiotoxicity in male albino rats. Biomarkers like lactate dehydrogenase (LDH), alanine aminotransaminase (ALT), aspartate aminotransaminase (AST), alkaline phosphatase (ALP), total cholesterol (TC), triglyceride (TG) and creatinine kinase (CK-MB) along with heart weight index and antioxidant enzymes was considered to determine the cardioprotective property. Histopathological study was also carried out on heart of experimental animals. The CGO peel extract was found to contain alkaloids, flavonoids, steroids and triterpenoids, saponins, phenolic compounds and tannin as chemical constituents. Cyclophosphamide (CYP) and doxorubicin (DOX) treated groups exhibited significant increase in LDH, ALT, AST, ALP, TC, TG and CK-MB level and decrease in catalase (CAT), superoxide dimutase (SOD) when compared to control group. Pretreatment with different doses of CGO significantly reduced the serum biomarkers and increased the tissue antioxidant level when compared to DOX and CYP alone treated groups. Moreover, treatment with CGO also improved CYP induced changes in histopathology of heart which may be due to its antioxidant property. The Citrus grandis (L.) Osbeck exerted protective effect against CYP and DOX induced cardiotoxicity in rats, which may be due its lipid lowering and antioxidant properties. These findings might be helpful to understand the beneficial effects of CGO extract against myocardial injury although further study is needed to confirm its mechanism.

365-369

Authors: Parth U. Patel*, T. Y. Pasa, Khushbu A. Thakor, Ruchita J. Chauhan

A stability indicating RP-UPLC method was developed and validated for simultaneous estimation Ofloxacin and Ornidazole in tablet dosage form. The separation was achieved under optimized chromatographic condition on a Waters® C18 Acquity UPLC BEH (100 mm × 2.1 mm, 1.7μm) column with mobile phase consist of Water: Acetonitrile: Triethylamine in the ratio of 85: 15: 0.1 v/v. An isocratic elution at a flow rate of 0.2 ml/min at ambient oven temperature was carried out with PDA detection at 300 nm. The retention time for Ofloxacin and Ornidazole was 3.9 min and 6.4 min respectively. The degradation was observed under acidic, alkali, oxidative, photolytic and thermal conditions. The linearity was found to be in the concentration range of 50-150μg/ml for Ofloxacin and 125-375μg/ml for Ornidazole. The % recoveries at 50% were found to be 100.46% & 100.22% for Ofloxacin & Ornidazole respectively. The % recoveries at 100% were found to be 99.70% & 99.83% for Ofloxacin & Ornidazole respectively. The % recoveries at 150% were found to be 99.67% & 100.30% for Ofloxacin & Ornidazole respectively. The method was validated as per ICH guideline and the values were found to be within the limits. So, the proposed method was found to be simple, linear, accurate, precise, stability indicating, robust and specific.

211-228

Authors: C. S. Barik1*, S. K. Kanungo1, N. K. Tripathy2, J. R. Panda3, M. Padhi4

Nature has been a source of medicinal agents for more than thousands of years and herbal therapy predominates in traditional systems of medicine as well as in alternative medicine practiced in various cultures such as Indian system of medicine, Chinese Traditional Medicine, Unani classical literature. The present review deals with various polyherbal formulations used by different countries of the world. Information on traditional herbal formulations was documented in the form of research and review articles in various journals. The aim of this review is to summarize the different types of herbs used for the preparation of polyherbal formulations, their therapeutic potentials including clinical and preclinical results along with their safety and efficacy. This review will facilitate to gain all about the past scientific research and the necessary information about the enormous pharmacological activities of polyherbal formulations which will insist the young researchers for future research to protect human beings from various types of diseases and may serves as a natural gold for the promotion of mankind.

235-243

Authors: Ganesh. M1, Ramesh. K2*, Madhusudan Rao. Y3, Chandra Shekar. B4

In present study, immediate release solid dispersion formulation of Entacapone with various lipids was developed using spray drying method. Entacapone is indicated for the treatment of Parkinson’s disease (PD) as an adjunct to levodopa/carbidopa therapy. Based on the process feasibility and solubility of resulting spray dried powder, formulation ENSD10 was selected for characterization and analyzed for in vitro dissolution profiles in three different pH media. The particle size of Entacapone in spray dried formulation ENSD10 was drastically reduced down to d90 of 25.86µ against d90 of as such drug substance, i.e., 124.74µ. Analysis by differential scanning calorimetry showed that the percentage of crystallinity has been significantly reduced in formulation ENSD10.The optimized solid dispersion formulation (ENSD10) by spray drying method comprising drug to lipid to lipid carrier ratio of 0.5:1:3 (Entacapone: Gelucire 50/13: Compritol) enhanced solubility nearly 6.31 fold and 3.75 fold as compared to pure drug and spray drug alone, respectively. The rate of drug release from spray dried powder was significantly improved and found to be on higher side as compared to the drug release from as such drug and spray dried drug alone. The obtained results suggested that developed Entacapone along with lipid carrier mixture by spray drying method has promising potential for oral delivery and might be an efficacious approach for enhancing the therapeutic potential of active substance.

251-258

Authors: Sija. S. L1*, Potty. V. P2, Santhoshlal. P. S1

Anacardium occidentale L. is much known for its commercially valuable kernals and also bioactive compounds like polyphenols which serve as natural antioxidant having an ability to quench cytotoxic free radicals that may prevent many diseases. The present study was carried out to evaluate the presence of anacardic acid, total phenolic compound, antioxidant activity and antibacterial activity in methanolic extract of callus and various plant parts such as flower, young leaves, shoot and cotyledon. Total phenolic contents were measured by the Folin-Ciocalteau method using gallic acid as standard compound. The maximum phenolic content was found in the methanol extract of flower (260.8 ± 5.543 mg/g) whereas the methanol extract of cotyledon (16.2 ± 3.284 mg/g) showed the lowest total phenolic content. The action of 1, 1-diphenyl-2-picrylhydrazyl (DPPH) on radical scavenging effect of the extracts was determined spectrophotometrically using ascorbic acid as standard compound. All extracts exhibited a DPPH radical scavenging activity and among the extracts, A. occidentale flower demonstrated greater antioxidant potential with a low IC50 (206.312 ± 0.38µg/ml) in comparison with those of the other extracts. Total phenolic contents showed positive correlations with the DPPH radical scavenging activity (r = 0.979; p<0.01) and negative correlations with IC50 (r = -0.984; p<0.01). The antibacterial capabilities of various extracts were also investigated against two common human pathogens of clinical importance, Escherichia coli and Staphylococcus aureus. Presence of anacardic acid in various extracts was also estimated by using HPTLC method. Pre-coated aluminum silica gel plate 60F254 was used as stationary phase and chloroform: ethyl acetate (9:1) was used as mobile phase.

263-269

Authors: Sayanti Sau*, Mukund Handral

Dalbergia sissoo (family: Fabaceae) is an Asian deciduous rosewood tree. It is the state tree of Punjab state (India) called as Shisham used for antipyretic, emesis, ulcers, leucoderma, stomach troubles and skin disease, memory enhancer etc. The aim of this study is to evaluate the learning and memory activity of ethanolic leaf extracts of Dalbergia sissoo in mice. The animals were divided into six groups of 6 each. Group I was considered as normal control, II as Standard control (Imipramine), III, IV and V was treated group (ELDS 300, 450 and 600 mg/kg respectively) and VI as scopolamine treated (negative control).The effect of ethanolic leaf extract of Dalbergia sissoo was investigated in mice for memory enhancing activity using various experimental paradigms of learning and memory viz. Transfer latency (TL) on elevated plus maze and passive avoidance. For memory and learning activity vehicle/ extracts / STD drug administered daily for first seven days, on 8th day dementia was induced by scopolamine. ELDS significantly enhanced the learning and memory activities against the scopolamine induced dementia and significant decrease in Acetylcholinesterase level in brain in animals. The memory enhanced activity as evidenced by learning and retrieval was due to cholinergic facilitatory effect in animals. These results indicate a possible memory enhancing action of Dalbergia sissoo which qualitatively comparable with that of piracetam.

275-278

Authors: Mohd Aslam1, Mohd Tariq2*, Katheem M. Farhan3, Mohd Aftab Ahmad2, Reshma Jolly4, Aisha Siddiqui1

Kushta Marjan (KM) is one well-known formulation prepared from coral used by Unani physicians for effective treatment of a various ailments. Coral is the calcareous skeleton of the minute marine organism and belongs of phylum coelenterate and is used internally in the form of kushta. It is highly efficacious in Cough, Asthma and Anorexia. Till date no scientific work has been performed to establish quality control of KM. In this study we have enlightened the preparation procedures, structural, functional and physico-chemical properties of KM by analyzing it on classical tests along with modern scientific techniques like FTIR (Fourier-transform infrared spectroscopy), TGA (Thermogravimetric Analysis) and DSC (Differential Scanning Calorimetry) to establish its quality control parameters. FTIR spectra showed peaks attributed to calcium oxide, organic matter and several other substances. Total weight loss during TGA was 30.09% and DSC curve showed peaks at 20°C, 65°C, 183°C and 261°C. Since the study has been first of its kind the results obtained might be taken as standard finger print of kushta marjan and might be helpful for further formulation and standardization of KM in routine analysis.

284-289

Authors: S. V. Kulkarni, M. C. Damle*

Embelin, a naturally occurring benzoquinone, is obtained from fruits of Embelia tsjeriam cottam, which plays a vital role in the Ayurvedic system of medicine. An approach for the stress degradation was successfully applied for the development of stability indicating HPTLC method for the determination of Embelin. It was spotted on the plates precoated with silica gel 60 F254 and developed using toluene: ethyl acetate: formic acid, (6:3.5:0.5 v/v/v) as mobile phase. Densitometry analysis was carried out at 291 nm. The method showed high sensitivity with good linearity over the concentration range of 200-1000ng/spot with correlation coefficient value 0.997. The accuracy of the method was established based on the recovery studies. The LOD and LOQ were 6.09ng/band and 18.48ng/band respectively. The system showed a peak for Embelin at Rf of 0.68 ± 0.02.The aim of our study was to observe the effect of various stress conditions on this potential drug candidate. Stress testing of Embelin was carried out according to the International Conference of Harmonization (ICH) guideline Q1A (R2). Embelin was subjected to stress conditions of acid, alkaline hydrolysis, oxidation, photolysis and thermal degradation. A significant degradation was found to occur by acid and oxidation hydrolysis and to a lesser extent under thermal stress and alkaline hydrolysis; and much lesser with photolytic stress. Stress degradation studies on embelin provide an insight into its stability.

298-303

Authors: S. Manivannan1*, P. Madhavi1, S. Bhuvaneswari2

Alpha amylase is one of the important and well known industrial enzymes that cause the breakdown of starch or glycogen. Use of microorganism for the production of amylase is economical as microbes are easy to manipulate to obtain enzymes of desired characteristics. However fungus is preferred over bacteria for enzymes production because of its filamentous nature. Agricultural wastes byproducts have great potential for the production of enzymes. Two indigenous carbon sources namely wheat bran and rice bran were used as substrate for amylase synthesis by Aspergillus flavus through solid state fermentation. Wheat bran gave the highest (670 ± 36μmol./min/mL) and Rice bran (428 ± 24μmol./min/mL) gave the lowest enzyme activity was obtained. Optimum inoculum size of 10% (660 ± 36μmol./min/mL), incubation period 120 hours (670 ± 28 μmol./min/mL), pH 6 (680 ± 42μmol./min/mL), temperature at 30°C (660 ± 46μmol./min/mL) gave highest yield of enzyme production. The highest yield of amylase production was obtained by the addition of MgSO4 0.2% and CaCl2 0.02% respectively. The results obtained in the present study suggest that the Aspergillus flavus may act as a potent strain for industrial production of α-amylase.

129-137

Authors: J. Balasubramanian1*, T. Sravanthi2, V. Sujitha2

The aim of the present review provides the relationship between therapeutic nanoparticles and mononuclear phagocytic system. Reticuloendothelial system (RES) represents a group of cells having the ability to take up and sequester inert particles and vital dyes. This includes macrophages and macrophage precursors, specialized endothelial cell lining the sinusoids of the liver, spleen and bone marrow, and the reticular cell of the lymphatic tissue (macrophages) and of the bone morrow (fibroblast). Nanoparticles are rapidly sequestered and retained by the organs comprising of the reticuloendothelial system (RES), mainly the liver, spleen and the bone marrow. Thus, targeting of the nanoparticles to the reticuloendothelial system (RES) is much simpler than to any other organ. In the liver, the particles are mainly retained by the scavenging periportal and midzonal Kupffer cells, while the hepatocytes and liver endothelial cells may play a secondary role under special pathophysiological conditions or for special physic- chemical characteristics of particles. The clearance of conventional nanoparticles has been proposed to occur by uptake of the nanoparticles by the reticuloendothelial system (RES). The mononuclear phagocytic system uptake of nanoparticles results in their rapid removal from the blood and accumulation in tissues involved in the RES, such as the liver and spleen. Uptake by the RES usually results in irreversible sequestering of the encapsulated drug in the RES, were it can be degraded. In addition, the uptake of the nanoparticles by the RES may result in acute impairment of the mononuclear phagocytic system and toxicity. Sterically stabilized nanoparticles, such as STEALTH nanoparticles, prolong the duration of exposure of the encapsulated nanoparticles in the systemic circulation. The presence of the PEG coating on the outside of the nanoparticles does not prevent uptake by the reticuloendothelial system, but simply reduces the rate of uptake.

143-150

Authors: Sameh S. Zaghlool1*, Basim A. Shehata2, Ali A. Abo-Seif1, Hekma A. Abd El-Latif3

Gastric ulcer is one of the most serious diseases over wide the world. There are many drugs used for the treatment of gastric ulcer, but most of these produce several adverse reactions. This study aims to investigate the protective effects of extracts of Ginger and Marshmallow on pyloric ligation-induced gastric ulcer in rats. Animals were divided into 5 Groups; a normal control group, an ulcer control group, a standard treatment group receiving famotidine (20 mg/kg), and two treatment groups receiving Ginger (100 mg/kg) and Marshmallow (100 mg/kg). Treatments were given orally for 14 days. On the 15th day, animals were subjected to pyloric ligation except for the normal control group. Four hours later, rat stomachs were excised and gastric juice and blood samples were collected. Pyloric ligation caused significant elevations in ulcer number, ulcer index, gastric volume, titratble acidity, acid output, mucin content and peptic activity, accompanied by significant decreases in blood superoxide dismutase activity (SOD) activity and gastric mucosal nitric oxide (NO) and glutathione (GSH) contents. In addition, elevations in gastric mucosal lipid peroxide and histamine contents were observed. Pretreatment with famotidine, ginger or marshmallow significantly corrected all blood and tissue parameters by varying degrees. Famotidine, ginger and marshmallow may protect against pyloric ligation-induced peptic ulcer in rats, being promising for further clinical trials.

157-162

Authors: Pallavi Thakur1, Raman Chawla1*, Ankita Singh Chakotiya1, Raghav Nagpal1, Ankit Tanwar1, Rajeev Goel1, Alka Narula2, Rajesh Arora3, Rakesh K. Sharma1

The herbal extracts of Camellia sinensis (Cs) and Andrographis paniculata (Ap) with standard F/P ratio (flavonoid/ polyphenol) of 0.26-0.27 were used for evaluation of anti-microbial efficacy against Vancomycin Resistant Enterococci (VRE). The bioactivity fingerprints useful for standardizing both extracts were found to be coherent with respect to their Diphenyl picryl hydrazyl radical scavenging potential (IC50 = ~ 30µg/ml). In vitro efficacy analysis of Cs and Ap extracts using exponentially growing culture of VRE revealed Minimum Inhibitory Concentration (MIC) as 200µg/mL and 50µg/mL respectively. The comparative analysis of their Minimum Bactericidal Concentration (MBC) revealed that 5X concentration of Cs as against 10X concentration of Ap was required to achieve zero microbial count. Such analysis indicated that both extracts would be useful for future analysis. In vivo pre-clinical evaluation studies are underway for utilization of identified herbal leads for trials on humans.

168-171

Authors: Meghraj Singh Baghel*, Kavita Goswami

Cancer is referred as uncontrolled growth of abnormal cell mass. Out of the several types of cancer, prostate cancer (PC) has become a major public health problem in men worldwide. Bcl-2 and p27 proteins are important regulatory molecules of cell cycle. Failure of cell cycle regulation leads to uncontrolled cell proliferation and causes cancer. For designing an effective structural based targeted drug, the assessment of protein-protein and protein-ligand interaction is indispensable. Therefore for treatment of PC, we selected a ribosome inactivating protein, Ricin, for assessment of its therapeutic nature. In the present work through CLUSTAL-W phylogenetic analysis, we found that Bcl-2 protein was found more conserved than p27. Further Bcl-2 was selected as target molecule for docking study with Ricin protein and other chemically synthetic inhibitor molecules i.e. 2-difluoromethylornithine (DFMO) and Sarcosine, as lead molecule. Through HEX5.1 docking software docking was performed between targeted receptor and lead molecules. Energy maximum (Emax= -93.12) and energy minimum (Emin= -163.07) was observed for docking complex of optimised and energy minimised structure of Bcl-2 receptor with Ricin, which in turn shows that it is highly stable interaction. On the other hand, for synthetic inhibitors, we found energy maximum (DFMO; Emax= -77.17, Emin= -117.83 and Sarcosine; Emax= -72.23, Emin= -103.00) and energy minimum, which are significant more as compared to Ricin docking complex. Due to ricin docking complex having less energies shows stable interaction with Bcl-2. We also observed that Ricin is less toxic (lesser log P value) as compared to other molecules by toxicity analysis by ADME/TOX server. These evidences show this Ricin could be better drug for PC. Further results are needed to validate by in vitro and in vivo study to make proper elucidation of drug for better PC treatment.

176-181

Authors: T. K. Laha1*, S. Sen1, G. Mishra2

A rapid and sensitive high performance liquid chromatographic method is described for simultaneous determination of duloxetine and its major metabolites, such as 4- hydroxy duloxetine (M7), Glucuronide conjugate of 5-hydroxy-6-methoxy duloxetine (M6) and Glucuronide conjugate of dihydrodiol duloxetine (M12) in rabbit plasma. HPLC analysis was carried out on a µ-Bondapak C18 column (250 mm × 4.6 mm, 5µm particle size) using methanol: phosphate buffer (pH 7.9, 50 mM) (7:3 v/v) as the mobile phase at a flow rate of 1.5 ml/min. Detection was carried out at 224 nm with an UV detector. The above metabolites present in the rabbit plasma were characterized by retro-synthesis followed by NMR and MS study for structure confirmation and finally injected separately into the HPLC system. All the three retention time matches with the metabolites present in the plasma sample.

188-192

Authors: Ayyagari Rama Murthy1*, K. Raghu Babu1, N. A. Vekariya2

Objective of the study was to develop and validate a new rapid, sensitive, reverse phase High Performance Liquid Chromatography technique for the estimation of Olanzapine in bulk and dosage form. Chromatographic separation was achieved on a BDS Hypersil C18, (150 mm × 4.6 mm, 5μm) with a mobile phase of 0.01M Tetra butyl ammonium hydrogen sulphate: Methanol (60:40) v/v. The flow rate was 1.0 ml/min, temperature of the column was maintained at ambient and detection was made at 228 nm. The run time was as short as 10.0 min. The developed method was validated according to the International Conference on Harmonization (ICH) guidelines with respect to linearity, accuracy, precision, specificity and robustness. The developed method was linear for Olanzapine from 10 - 80μg/ml and the linear regression obtained was 0.9994. Recovery of Olanzapine was found to be in the range of 99.6 -101.7%. Precision, evaluated by intra- and inter-day assays had relative standard deviation (R.S.D) values within 1.0 %. The ruggedness of the method was validated by performing the analysis by two different analysts and no significant difference in the result was found. Robustness of the method was checked by varying flow rate by 0.2 ml/min and the result was not affected significantly. The analysis of the marketed sample indicated that the method can also be applied to dosage form successfully. The method is precise, accurate, linear, robust and fast. The retention time and run time was very short; hence it is cost effective, making it more economical and rapid. Hence, this method can be used for the analysis of large number of samples.

198-204

Authors: Jasmine Karanjia*

This paper describes two sensitive, accurate and precise chemometric spectrophotometric methods for the simultaneous determination of Cinitapride hydrogen tartarate (CNT) and Pantoprazole sodium (PANTO) in bulk powder and capsules without prior separation. Multivariate calibration chemometric methods are proposed for simultaneous determination of CNT and PANTO. The chemometric methods applied are Principal Component Regression (PCR) and Partial Least Squares (PLS). These approaches are successfully applied to quantify both drugs using the information included in the absorption spectra of appropriate solutions. In these multivariate methods, calibration sets of standard samples composed of different mixtures of CNT and PANTO have been designed. The methods were validated according to The International Conference on Harmonization (ICH) guidelines. The specificity of the proposed methods was tested using laboratory-prepared mixtures. The developed methods were successfully applied for the determination of CNT and PANTO in bulk powder and dosage form combination.