Abstract

Before fitting with a receptor a drug has to cross several bio-membranes, containing lipid as one of the important components. Interaction of a drug with lipid may lead to lipid peroxidation, an oxidative process which produces several toxic end products, including malonyldialdehyde (MDA), 4-hydroxy-2-nonenal (4-HNE) etc. Antioxidants have the capacity to minimize lipid peroxidation. In view of the above context the present in vivo study was conducted to find out lipid peroxidation induction potential of Tobramycin, an aminoglycoside antibiotic and its inhibition with Ascorbic acid, an antioxidant. Rabbits are used as animal model. Rabbits divided into different experimental groups are treated with drug and co-administered with ascorbic acid. The levels of MDA, HNE, GSH and NO in the blood are estimated and compared with the control. The results revealed that Tobramycin significantly increases MDA and HNE contents, but decreases GSH and NO levels; and though ascorbic acid shows pro-oxidant effect but on co-administration with tobramycin, ascorbic acid has the capability to inhibit drug-induced lipid peroxidation.

Abstract

Two classic animal behavior despair tests—the Forced Swimming Test (FST) and the Tail Suspension Test (TST) were used to evaluate the antidepressant activity of methanolic extract of Celtis timorensis mice. It was observed that of 200 and 400 mg/kg significantly reduced the immobility time in the FST and TST in mice 30 min after treatment. Immobility displayed in both of these behavioral despair models has been hypothesized to reflect behavioral despair which in turn may reflect depressive disorders in human. The probable mechanism of action may be MECT ability to increase levels of Ach and serotonergic transmission however the exact mechanisms have to be investigated further. The standard antidepressant used here is fluoxetine.

Abstract

The objective of the present study was to review the recent advances in targeted drug delivery to tumors.Now a days cancer is second cause of death.Despite several advancements in chemotherapy, the real therapy of cancer still remains a challenge.The development of new anti-cancer drugs for the treatment of cancer has not kept pace with the progress in cancer therapy, because of the nonspecific drug distribution resulting in low tumour concentrations and systemic toxicity. The main hindrance for the distribution of anti-cancer agents to the tumour site is the highly disorganized tumour vasculature, high blood viscosity in the tumour,and high interstitial pressure within the tumour tissue.Recent approaches to fight tumor is to impede and interfere with its blood supply i.e turning off angiogenesis or neovascularisation. This review discusses different strategies employed for the delivery of anti-cancer agents to tumours, such as through EPR effect, local chemotherapeutic approaches using drug delivery systems, and special strategies such as receptor-mediated delivery, pH-based carriers,application of ultrasound and delivery to resistant tumour cells and brain using nanoparticles.

Abstract

To continue the other plants with organ protective potential, the present study was undertaken to investigate the hydroalcoholic extract (70% alcoholic extract) of Samanea saman (Jacq.) Merr leaves for its protective effects on paracetamol induced renal damage in rats.  Rats were divided into four groups containing 6 animals in each; normal saline, paracetamol 2G/kg, hydroalcoholic extract of Samanea saman in lower (250 mg/kg p.o) and higher dose (500mg/Kg p.o) levels. Total phenolics and flavonoids were quanitified. Invitro and invivo antioxidant activities were also performed. BUN and serum creatinine were also estimated as a part of investigation. The phenolic and flavonoidal content of 70% alcoholic extract were found to be 77.14 mg/G and 229.0 mg/G respectively. Paracetamol induced nephrotoxicity as revealed by marked changes in physical, tissue and blood parameters. Administration with hydroalcoholic extract of leaves of Samanea saman improved all these parameters.  Even elevated LPO and reduced tissue GSH level were significantly reversed.  These changes in parameters clearly indicate the potential use of this plant in paracetamol induced nephrotoxicity and this may be attributed to the presence of antioxidant principles.

Abstract

A  novel,  simple  and  economic  reverse  phase  high  performance  liquid  chromatography  (RP-HPLC) method has been developed for the related substance in Imatinib mesylate with greater precision and accuracy. A SunFire^TM C18, (4.6 X 150) mm, using acetonitrile: methanol mobile phase at a flow rate of 1.0 ml/min, and UV detection at 230 nm, was employed. The retention times of Imatinib mesylate, acid impurity and amine Impurity were about 17.96, 1.47 min and about 14.11 min, respectively. The standard curves were linear over the concentration range of 0.25 µg/ml to   3.75 µg/ml. The LOD and LOQ values for acid impurity were 0.01 µg/ml and 0.03 µg/ml, for amine impurity were 0.002 µg/ml and 0.005 µg/ml, and for Imatinib mesylate were 0.01 µg/ml and 0.04 µg/ml respectively. The  percentage recovery  was  found  to  be 96.2  to 99.9  and  the  %  RSD  of intraday and inter day precision was found to be 0.00  and 0.00 respectively. The method was validated as per ICH guidelines. Validation studies demonstrated that the proposed RP-HPLC method is simple, specific, rapid, reliable and reproducible and found to be specificity, linearity, and precision, intermediate precision, and accuracy, stability in the RS solution and robustness.

Abstract

In traditional medicine most of the diseases have been treated by administration of plant or plant product. Echinops echinatus Roxb is the useful traditional medicinal plant in India. Each part has some medicinal property. During the last five decades, apart from the chemistry of the Echinops echinatus Roxb compounds, considerable progress has been achieved regarding the biological activity and medicinal applications of Echinops echinatus Roxb. It is now considered as a valuable source of unique natural products for development of medicines against various diseases and also for the development of industrial products. This review gives a bird’s eye view mainly on the biological activities of the Echinops echinatus Roxb and some of their compounds isolated, pharmacological actions of the Echinops echinatus Roxb extracts, clinical studies and plausible medicinal applications ofEchinops echinatus Roxb along with their safety evaluation.

Abstract

The benzene sulphonamides moiety exploited to prepared anticancer drugs. Benzene Sulphonamides posses many types of biological activities and representatives of this class of pharmacological agents are widely used in clinic as antibacterial antifungal, hypoglycaemic, diuretic and anti-carbonic anhydrase among others. Recently, a host of structurally novel sulfonamide derivatives have been reported to show substantial antitumor activity in vitro and/or in-vivo. Also, quinoline derivatives are important biologically active compounds showing anticancer activity.

Abstract

Curcumin, a yellow pigment from Curcuma longa, is a major component of turmeric and is commonly used as a spice and food-coloring agent. It is also used as a cosmetic and in some medicinal preparations. The desirable preventive or putative therapeutic properties of curcumin have also been considered to be associated with its antioxidant and anti-inflammatory properties. In the present study, we determined the antioxidant , anti inflammatory and anti diabetic (amylase inhibition) activities of curcumin by employing various in-vitro antioxidant assays such as Ferric reducing antioxidant power, Free radical scavenging activity, Hydroxyl radical scavenging activity, Nitric oxide radical scavenging activity and Amylase inhibition assay. The curcumin exhibited its radical scavenging effect in concentration dependent manner and the effect was compared with a known antioxidant agent (BHA/Ascorbic acid).  The curcumin was also evaluated for its anti inflammatory activity by using hyaluronidase inhibition assay. The anti-inflammatory effect of curcumin is most likely mediated through its ability to inhibit cyclooxygenase-2 (COX-2), lipoxygenase (LOX), and inducible nitric oxide synthase (iNOS). COX-2, LOX, and iNOS are important enzymes that mediate inflammatory processes. Curcumin exhibited concentration dependent anti inflammatory activity. The anti-diabetic potential of curcumin was also evaluated by assessing amylase inhibition assay. The results for amylase inhibition activity reveal that the curcumin inhibits alpha-amylase in a concentration dependent manner. This study indicates significant amylase inhibition, free radical scavenging and hyaluronidase inhibition potential of curcumin which can be exploited for the treatment of various free radical mediated disease like inflammation and diabetes mellitus.  The present study reveals that curcumin is a good antioxidant, anti inflammatory and anti diabetic agent hence, can be used in the pharmacological and food industry and as neutraceutical products.

Abstract

The objective of the study was to evaluate the association between marital status and diabetic duration with regard to Cognitive dysfunction in Diabetic patients. The study carried out on 500 diabetic patients of various socio demographic characteristics over a period of eighteen months with Mini Mental State Examination (MMSE scale).  The objective of the research was to investigate the cognitive effects of different factors associated with health care in diabetes management in their course over time.  The results of the studies show that diabetes and its complications along with socio demographic factors impart a significant impairment in cognitive domains.  It is highly necessary that subjects with diabetes be screened for cognitive functioning at the earliest, considering the fact that diabetes requires high level of self management especially for better compliance.  Through the research conducted the result shows that there is no significant difference in TMMSE base, 1^st follow up and second follow up. There is a significant difference in cognitive function on the basis of duration of diabetes. Result concluded that patients who have diabetes for more than 2 years have a significantly decline in cognitive function.

Abstract

Oral route of administration continues to be the most preferred route among the different routes of administration of drugs due to various advantages including ease of ingestion, avoidance of pain, versatility and most importantly patient compliance. Immediate release tablets have gained popularity and acceptance as a drug delivery system, mainly because they are easy to administer and lead to better patient compliance. The present work involves the formulation development, optimization and in-vitro evaluation of immediate release Bromocriptine Mesylate tablets. To minimize critical process parameters and since Bromocriptine Mesylate is moisture and heat sensitive potent crystalline drug, direct compression method was selected for the formulation of immediate release tablets. Tablets were prepared containing Bromocriptine Mesylate, pharmatose DCL 21, starch, aerosil-200, magnessium stearate, sodium starch glycolate and cross carmellose sodium, in different concentrations. During the course of study it was found that the formulation F5 containing cross carmellose sodium as super disintegrant exhibited acceptable disintegration time, percentage drug content per tablet and In vitro drug release. So at last it was concluded that immediate release Bromocriptine Mesylate tablets containing pharmatose DCL 21 as diluent and 5% cross carmellose sodium as super disintegrant can be prepared using direct compression which met the required specifications.

Flax is a nutraceutical with many nutritional benefits. Aside from the vitamins, minerals, fiber and protein it contains some primary and secondary metabolites. Flaxseed is a good source of omega-3 fatty acids. Through its high concentration of alpha-linolenic acid, flax provides more omega-3 fatty acids than any other grain. (57% of its fatty acids are omega-3s.) As the health revolution continues to evolve, look for it to be added to more and more processed foods to attain the health smart claim. Flaxseed (FS), a whole grain used as a nutritional supplement, has gained popularity because it is a rich source of natural antioxidants. Dietary intake of polyphenols has been associated to reduce risk of chronic diseases, such as heart disease, stress induced diabetes and cancer. This is probably due to their antioxidant properties. Many phenolic compounds have been detected in Flaxseed. Hence with the objectives to analyze the phytonutrient composition, assess the non-antioxidant enzymes vitamin A, E and C and find the antioxidant activity of processed flaxseed the study was carried out. The flaxseed was subjected to various methods of food processing like roasting, pressure cooking and soaking. The processed flaxseed was further analysed the primary and secondary metabolites and their antioxidants activity. This study does not show much variation in primary and secondary metabolites between the raw and roasted seeds. The acceptance and palatability was high in the case of roasted soybean and flaxseed because of their nutrients nutty flavour, colour and texture than the unprocessed seeds. Non- antioxidant enzymes, vitamin A, vitamin E and vitamin C content was high in both soaked and roasted flaxseed. Antioxidant activity was high in roasted and soaked flaxseed. Thus the presence of these phytonutrient and antioxidant activity of processed namely roasted and soaked flaxseeds indicates that, it has a potential of being used in formulations prepared for food consumption. Flaxseed could also be a remedy for the major killer diseases like cancer, diabetes and cardiovascular diseases. 

Human brain is the most evolved complex structure in the body. Various neurodegenartive diseases like alzemiers disease, Dementia, attention deficit, were set as tough challenges in the medical field. The current medical research studies focuses on the potential usage of herbal drugs. The present study was carried out with an interest and contribution for herbal medicines as essential potent drugs. Ervatamia coronaria (Linn) is glabrous, evergreen tree commonly grown in gardens and various parts of the plant were used in the indigenous system of medicine for the treatment of various disorders. To validate the ethnotherapeutic claims of the plant for its use as a brain tonic, the Learning & memory enhancing activity of ethanolic and aqueous extracts of aerial parts of Ervatamia coronaria was evaluated by Elevated plus maze apparatus in mice. The effect of transfer latency (TL) due to extracts (ethanolic & aqueous at 200,400 mg/kg) and standard drug (Piracetam 200mg/kg) were compared to that of control and negative control (Diazepam 5mg/kg). The effect of herbal extracts was evaluated on elevated plus maze apparatus in Diazepam induced amnesia in mice. It is observed that the ethanolic & aqueous extracts at various doses(200 mg/kg) has significantly reduced the transfer latency in mice compared to control and negative control groups in a dose dependent manner and results were comparable to the standard Piracetam treated group. From the results obtained, it is evident that the traditional herbal extracts have significant learning and memory enhancing property. 

Controlled release dosage forms have been extensively used to improve therapy with several important drugs. Oral sustained release gastroretentive dosage forms offer many advantages for drugs with absorption from upper parts of gastrointestinal tract and for those acting locally in the stomach. Floating drug delivery system is one amongst the gastroretentive dosage forms used to achieve prolonged gastric residence time. In recent years various scientific and technological advancements have been made in the research and development of oral drug delivery systems to overcoming physiological activities, such as short gastric residence times and unpredictable gastric emptying time. In order to avoid such adversities, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours via floating drug delivery systems. The purpose of this paper is to review the recent literature and current technology used in the development of gastroretentive dosage forms. The recent developments of floating drug delivery systems include the physiological and formulation variables affecting gastric retention, approaches to design single unit and multiple unit floating systems, their classification and formulation aspects and also in-vitro and in-vivo studies are covered in detail. 

The crushed seeds of Tamarindus indica and the crushed roots of Asparagus racemosus were soaked in water separately for 24 hours and then boiled for 1 hour and kept aside for 2 hours for the release of mucilage into water. After extraction with hot water and acetone treatment, the Tamarind seeds yielded 78% mucilage and Asparagus racemosus roots yielded 28% mucilage. Sustained release tablets of Diclofenac sodium were fabricated using Tamarindus indica, Asparagus racemosus mucilage and HPMC. The tablets were evaluated the physical characteristics like hardness, weight variation, friability and drug content. In-vitro release of drug was performed in phosphate buffer pH 6.8 for twelve hours. All the physical characters of the fabricated tablet were within acceptable limits. The tablet with HPMC (Batch C-I) exhibited greater drug content than those with natural tree mucilage and other batches of HPMC. A better sustained drug release was obtained with the matrix tablet made-up with the natural mucilage compared to HPMC polymer. It is cleared through the dissolution profile of Diclofenac sodium from matrix tablets prepared using different polymers were indicated an increase in the polymer ratio retarded the drug release to a greater extent. In case of tablets prepared with Asparagus mucilage, almost maximum drug was released within 8-10 hours. Only at the highest concentration of mucilage (i.e.,14%),the drug release was found to sustain upto 12 hours in a steady manner.

A novel, simple and economic reverse phase high performance liquid chromatography (RP-HPLC) method has been developed for the related substance in Imatinib mesylate with greater precision and accuracy. A SunFireTM C18, (4.6 X 150) mm, using acetonitrile: methanol mobile phase at a flow rate of 1.0 ml/min, and UV detection at 230 nm, was employed. The retention times of Imatinib mesylate, acid impurity and amine Impurity were about 17.96, 1.47 min and about 14.11 min, respectively. The standard curves were linear over the concentration range of 0.25 ?g/ml to 3.75 ?g/ml. The LOD and LOQ values for acid impurity were 0.01 ?g/ml and 0.03 ?g/ml, for amine impurity were 0.002 ?g/ml and 0.005 ?g/ml, and for Imatinib mesylate were 0.01 ?g/ml and 0.04 ?g/ml respectively. The percentage recovery was found to be 96.2 to 99.9 and the % RSD of intraday and inter day precision was found to be 0.00 and 0.00 respectively. The method was validated as per ICH guidelines. Validation studies demonstrated that the proposed RP-HPLC method is simple, specific, rapid, reliable and reproducible and found to be specificity, linearity, and precision, intermediate precision, and accuracy, stability in the RS solution and robustness. 

The present study was aimed to reveal the alkaloid profile of Clitoria ternatea seed, stem and leaves using HPTLC. Preliminary phytochemical screening was carried out by Harborne method. HPTLC studies were followed by Harborne and Wagner et al. method. The ethyl acetate-methanol-water (100: 13.5: 10) was employed as mobile phase for alkaloids. The methanolic extract of stem, leaves and seeds of Clitoria ternatea showed the presence of 26 different types of alkaloids with 21 different Rf values with range 0.02 to 0.93. In general more degree of alkaloids diversity has been observed in reproductive parts (seeds) when compared to the vegetive parts leaves and stem. Maximum number (10) of alkaloids has been observed in seeds followed by leaves (9). Among the ten different alkaloids of seeds, seven (0.15, 0.23, 0.41, 0.52, 0.62, 0.67 and 0.79) are unique to the seeds only and they are not present in the vegetaive parts of the plant. The proposed HPTLC profile can be used for the identification of the medicinally important plants and distinguish from its adulterant. 

The methanol extract of Ichnocarpus frutescens roots were fractionated in hexane (HF), petroleum ether (PEF), chloroform (CF), ethyl acetate (EAF) and n-butanol (BF) soluble fractions and n-butanol fraction was sub fractionated by column chromatography through Diaion HP-20 into four sub-fractions, BF-1, BF-2, BF-3 and BF-4 and the DPPH radical scavenging potential of these fractions was evaluated as per modified procedure of Cotelle et al. using BHT as a positive control. Out of eight fractions tested, BF-1 and BF-2 fractions have shown outstanding scavenging activity with inhibition of 90.590 ± 0.249 and 94.012 ± 0.340 %, respectively at the concentration of 200 ?g/mL, which were comparable to that BHT having 95.023 ± 0.156 % inhibition. The remaining fractions viz BF-3, BF-4, EAF, CF, PEF and HF showed considerable antioxidant potential of 48.920 ± 0.684, 29.562 ± 0.384, 67.960 ± 1.130, 87.483 ± 0.262, 55.923 ± 0.356, 9.890 ± 0.740%, respectively at the same concentration. The sub-fractions BF-1 and BF-2 exhibited stronger antioxidant activities (IC50 values of 1 and 11.5 ?g/mL, respectively) than that of known antioxidant BHT (IC50 value of 12 ?g/mL). 

The present investigation is concerned with formulation and evaluation of Mucoadhesive buccal tablets containing antidiabetic drug, Glimepiride to circumvent the first pass effect and to improve its bioavailability with reduction in dosing frequency and dose related side effects. The tablets were prepared by direct compression method. Six formulations were developed with varying concentrations of polymers like Carbopol 934P, HPMCK4M and Chitosan. The tablets were tested for weight variation, hardness, surface pH, drug Content uniformity, percentage swelling index, bioadhesive strength, ex-vivo residence time in-vitro drug dissolution study, In-vitro drug release kinetic study, ex-vivo permeation study and Stability study. FTIR studies showed no evidence on interactions between drug, polymers and excipients.The best in-vitro drug release profile was achieved with the formulation FIII which contains the drug, Carbopol 934p and HPMC K4M in the ratio of 1:3.75:10. The surface pH, bioadhesive strength, ex-vivo residence time and swelling index of formulation FIII was found to be 6.88±0.5, 41.6±0.15g, 330min and 191.94±0.71%, respectively. The formulation FIII, containing 4 mg of Glimepiride exhibited 6 h sustained drug release i.e. 99.32±0.5% with desired therapeutic concentration. The drug permeation from the formulation FIII was slow and steady and 3.56 mg of Glimepiride could permeate through sheep buccal membrane with a flux of 0.27 mg hr-1 cm-2.The in-vitro release kinetics studies reveal that all formulations fits well with zero order kinetics and followed non-Fickian diffusion mechanism. As in-vitro dissolution studies and in-vitro buccal permeation study showed satisfactory results, it can be further subjected to in-vivo studies in normal and diseased volunteers to find out the adverse effects, by pharmacodynamics andPharmacokinetic parameters. 

The present study reveals detailed analysis of Macro and Microscopical characters of the leaves of Rivea hypocrateriformis (Desr.) Choisy. with the scope of Ethnic importance. This plant is used by the chenchu tribes of Kadapa district as a single drug remedy to treat rheumatism. The plant belongs to Convolvulaceae family and the identification of the plant is very difficult, because of the resemblance with other species of same family. In the present work the leaf part of the plant was subjected to various pharmacognostical studies like, powder microscopy, sectioning, maceration and florasense studies (Table No-1) to identify authentically. In the microscopical studies, the different cell structures like Calcium oxalate crystals, trichomes, elongated fibers and different arrangements like, xylem vessel with spiral thickenings, reddish tannin content in the parenchymatous cells were noticed. 

Type-1 diabetes (T1D) is an autoimmune disease characterized by insulitis and islet ?-cell loss. At the onset of T1D, more than 70% of ?-cells are destroyed, whereas the residual ?-cells most likely represent the only reservoir for the regeneration of islet ?-cell mass. Indeed, an effective therapy of T1D requires suppression of the autoimmune process and restoration of islet ?-cells. GABA can be a potential target for Type-1 diabetes mellitus. GABA is inhibitory neurotransmitter and released from pancreatic ?-cell. It acts on GABAAR in the ?-cells, causing membrane hyper polarization and hence suppressing glucagon secretion. GABA treatment can reduce lymphocytic islet infiltration, restore the ?-cell mass, and completely reverses hyperglycemia. This is associated with increased insulin, decreased glucagon levels in the circulation, and improved metabolic conditions. So, GABA or GABA-mimic drugs may be utilized as potential therapeutic option in the prevention and treatment of Type-1 Diabetes mellitus. 

In the present research work, aimed to prepare and evaluate the fast dissolving oral films containing Rizatriptan Benzoate, an antimigraine drug using different ratios of polymers, Hydroxypropyl methylcellulose E15, Polyvinyl alcohol and Maltodextrin. The film was prepared by solvent casting technique using Propylene Glycol, Aspartame and Mannitol as plasticizer, sweetening and cooling agent respectively. The study examines the influence of polymers ratio on physicochemical properties and drug release potential of films. Rizatriptan Benzoate, a serotonin 5-HT1 receptor agonist is a new generation antimigraine drug which has oral bioavailability of 45% due to hepatic first pass metabolism. The present study investigated the possibility of developing Rizatriptan benzoate fast dissolving sublingual films allowing fast, reproducible drug dissolution in the oral cavity, thus bypassing first pass metabolism to provide rapid onset of action of the drug. The films were thin, smooth, flexible, and uniform in drug content, weight and thickness as observed from low SD values. The film formulation, (F11) consisting of 200mg of polyvinyl alcohol and 200mg of Maltodextrin was found to be suitable in the form of fast dissolving oral film based on in vitro evaluation studies. From the Ex vivo studies it was found that 82.93% drug was permeated through porcine oral mucosa. The optimized formulation, F11 showed less disintegration time and faster drug release. All the systems were found to be stable with respect to drug content as well as physical changes at 400C and 75% RH. The results suggest that polymer based fast dissolving films are potential means to achieve rapid drug release for effective therapy. 

A simple, efficient, accurate, precise and new spectrophotometric method has been developed for spectroscopic estimation of Lamotrigine in bulk and in tablet dosage forms. In the present study, a very slightly soluble drug, Lamotrigine has been solubilised in water using hydrotropic blend containing 5% urea, 5% sodium benzoate, 10% nicotinamide, and scanned between 200-400nm taking respective reagent blanks in a double beam spectrophotometer. The ?max was found to be 306nm and Lamotrigine was found linear in the range of 10-50 mcg/ml. The mean percent Lamotrigine estimated in Lamotrigine tablets were 100.07 (formulation I) and 99.05 (formulation II). These values are very close to 100, indicating accuracy of proposed method. The proposed method was validated statistically by low values of statistical parameters such as standard deviation, per cent coefficient of variation and standard error. In this proposed method, organic solvents are not used which makes it eco-friendly.This mixed hydrotopy, a novel approach can be used not only for estimation but also used to increase solubility and release of poorly water soluble drugs.The hydrotropes used are cost efficient, safe and non-harmful to environment, hence it can be employed for routine analysis of Lamotrigine in bulk and in tablet dosage forms. 

An attempt has been made to prepare the various trials of extended release film coated matrix tablets of Felodipine using polyoxyl 40 hydrogenated castor oil (Cremophor RH40) as solubilizer with the different grades of hydroxy propylmethylcellulose (HPMC) as the release retardant polymers by wet granulation method. The prepared granules and tablets were evaluated for the various pre and post compression parameters. The dissolution profile of the various trials with the dissolution profile of marketed formulation was compared by using Food and Drug Administration-recommended similarity factor (f2) determination. The formulation trail containing methocel E50 premium, with a similarity factor (f2) of more than 80 % was selected as the optimized formulae for scale-up batches. Finally, it was compared with the in-vitro release profile of the marketed product with various dissolution media such pH 6.5 phosphate buffer with 1% sodium lauryl sulfate and 1% (w/v) polysorbate 80 in water. The results were found to be satisfactory. 

The project, for the first time, reports the development of sustained release granules of Diclofenac sodium and Eperisone hydrochloride. The granules were subjected to physical tests, dissolution profiling as well as assay. The analytical method was developed for both the drugs as API and for sustained release granules on Shimadzu UV-1800 spectrophotometer by simultaneous equation method. Phosphate buffer of pH 6.8 was selected as a common solvent for estimation of Diclofenac and Eperisone at 276 nm and 261.4 nm respectively. Beer law was obeyed in the range of 2-22 g/ml and 2.5-32.5 g/ml with correlation coefficient of 0.999 and 0.998 respectively. Detection limit and quantification limit were found to be 0.082 g/ml and 0.22 g/ml for Eperisone and 0.109 g/ml and 0.331g/ml for Diclofenac respectively. Developed method was found to be simple, accurate, precise, reproducible and in agreement with all the validation criteria as per ICH with negligible interference from excipients. Assay results were found to be 98.76% and 100.09% for Eperisone HCl and Diclofenac Na respectively. The sustained release granules passed all the physical tests and demonstrated good dissolution profile. 

The present was carried out to know the pharmacologically active chemical constituents present in Aerva lanata (L.) Juss. Ex. Schult leaves, stem, root and flower. 2 ?L of the methanolic extract of roots, flowers, stems and leaves were employed for GC-MS analysis. Mass spectra were taken at 70 eV; a scan interval of 0.5 s and fragments from 45 to 450 Da. The MS detection was completed in 36 minutes. The compound biological activity prediction is based on Dr. Duke’s Phytochemical and Ethnobotanical Databases by Dr. Jim Duke of the Agricultural Research Service/USDA and PASS. The A. lanata methanolic root, flower, stem and leaves extracts revealed the presence of 23, 25, 23 and 23 different compounds respectively. The A. lanata methanolic root, flower, stem and leaves extracts. The Dukes database and PASS prediction results showed that the major components displayed different biological activities such as antineurotoxic, anticarcinogenic, antialcoholic, antiviral, antiinflammatory, antiprotozoal, antiparasitic, antimutagenic, antineoplastic, antianemic, antiamyloidogenic, antimetastatic, antimycobacterial, antituberculosic, anticataract, cytoprotectant, fibrinolytic, immunomodulator, antileprosy, antianorexic, antirickettsial, CNS active muscle relaxant and psychostimulant. The present study results suggest that methanolic extract of Aerva lanata is a potent therapeutic agent. Further work is needed to isolate and identify these bioactive compounds. 

(apto: “to fit”& mer: “smallest unit of repeating structure”). Aptamers are single stranded folded oligonucleotides and peptide that bind to molecular (protein) targets with high affinity and specificity.In addition to target validation and research applications, aptamers are being developed as therapeutic agents. A number of aptamers have completed various stages of pre-clinical development, ranging from pharmacokinetic analysis, characterization of biological efficacy in cellular and animal disease models, and safety assessment. In particular, one aptamer, targeting vascular endothelial growth factor (VEGF), has completed phase III clinical trials for age-related macular degeneration (AMD), a leading cause of blindness16. Aptamers constitute one of four classes of oligonucleotide reagents, the others being antisense oligonucleotides, ribozymes and small interfering RNAs (siRNAs) SiRNAs, discovered less than a decade ago, have generated tremendous interest as potential therapeutic agents, and several compounds have already entered clinical trials. Ribozymes and antisense oligonucleotides have been under study for more than two decades, but to date only one commercially available therapeutic agent, fomivirsen (Vitravene,Novartis), an antisense oligonucleotide used to treat cytomegalovirus retinitis, has resulted from these approaches. Difficulties with the development of these agents include instability in biological media and, more importantly, a requirement to cross cellular membranes in order to exert their therapeutic actions. Like other oligonucleotide agents, aptamers are not bioavailable when administered orally and do not readily cross cell membranes. 

The aim of this study is to review the advantage of Mucoadhesive microsphere, mechanism and theories involved in mucoadhesion, factor that affect the mucoadhesion and polymers in the drug delivery systems. Gastroretentive systems are those which are retained in the stomach for a longer period of time and thereby improve the bioavailability of drugs. Also to evaluate the potential use of mucoadhesive microspheres for Gastroretentive delivery.Chitosan, thiolated chitosan, Carbopol 71G and Methocel K15M were used as mucoadhesive polymers. The poor bioavailability of microsphere is attributed to short retention of its dosage form at the absorption sites (in upper gastrointestinal tract to duodenum and jejunum). Overall review indicated prolonged delivery with significant improvement in oral bioavailability of mucoadhesive microspheres due to enhanced retention in the upper GI tract.Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours.. The present review addresses briefly about the floating drug delivery systems. Uniformly sized polymeric microspheres that support a variety of applications in the life sciences. Available in diameters ranging from 20nm to 20?m, products exhibit excellent size uniformity. Most of our microspheres are polystyrene-based, although some other base polymers are also offered. Plain (non-functionalized) polymer microspheres are ideal for protein adsorption applications, while surface modified microspheres (COOH or NH2) are used for covalent ligand attachment. Cross-linked polymer microspheres are available for improved solvent, heat, and pressure resistance. Polymer microspheres are also available with impregnated visible or fluorescent dyes.