Papers by Pharmaceutical and Biological Evaluations

Objective: This research work focus on synthesis of silver nanoparticles from Morinda tinctoria R... more Objective: This research work focus on synthesis of silver nanoparticles from Morinda tinctoria Roxb leaves. The synthesis of nanoparticles from biological processes is evolving a new era of research interests in nanotechnology. Silver nanoparticles are usually synthesized by chemicals. M. tinctoria Roxb leaves are reputed plant in traditional system of medicine and it is used for the treatment of illness such as arthritis, cancer, gastric ulcer and other heart disease etc. Methods: The present study the leaves were collected, air dried and subjected to synthesis of silver nanoparticles (MtNps). The obtained nanoparticles from M. tinctoria Roxb leaves was characterized and antimicrobial activity, antidiabetic and anticancer activity was analyzed by standard procedures. Results: M. tinctoria silver nanoparticles study showed the evaluation of antioxidant and anticancer activity. Antioxidant activities were done using DPPH antioxidant assay and hydrogen peroxide assay. The anticancer study was conducted to evaluate the in-vitro anticancer activity of green synthesized nanoparticles using human hepatic carcinoma cell lines (HepG2). Conclusions: M. tinctoria silver nanoparticles evaluation showed higher antioxidant activity and anticancer activity in M. tinctoria Roxb.

Objective: To design, synthesize and screen biologically newer Substituted Schiff bases by conden... more Objective: To design, synthesize and screen biologically newer Substituted Schiff bases by condensing substituted acid hydrazides with various benzaldehydes and explore their antimicrobial potential. Methods: Present study synthesis of various derivatives of Schiffs bases was carried out by: firstly converting substituted acids to acid hydrazides and then to Schiff's bases after condensation with substituted benzaldehyde. Synthesized compounds were characterised on the basis of spectral studies (like UV, IR, and NMR). All the synthesized derivatives were screened further for their antibacterial effect against Salmonella typhimurium, Shigella sonnei, Staphylococcus aureus& Bacillus cereus. Results: From this study it could be observed that schiff's bases 2-[(aminophenylhydrazinyldene o,m,dinitrobenzoyl] aniline (H) and compound 2-[(aminophenylzinyldene) p amino benzoyl] aniline (I) showed very good zone of inhibition against almost all strains tested for. Conclusions: So further attempts could be made to extend the series and explore their antibacterial potential to achieve hopeful goal.

Obesity is one of major health disorders that has become epidemic worldwide. Studies have demonst... more Obesity is one of major health disorders that has become epidemic worldwide. Studies have demonstrated that oxidative stress and inflammation in adipose tissue is involved in obesity linked complications. The ectopic synthesis of melanin in adipocytes of obese patients has been newly discovered. It is hypothesized that there is potential role of melanin and its intermediates to ameliorate oxidative stress in adipose which may prevent the secondary complications to obesity. This study was done to determine whether melanin interferes with the level of oxidative stress produced in adipocyte cells in culture. Adipocyte cells were cultured in vitro and exposed to high concentration of glucose oxidase to induce oxidative stress, then cells were treated with melanin for different periods. Thereafter the levels of some oxidative stress and inflammatory biomarkers such as glutathione, TNF-alpha, Malondialdehyde (MDA), and protein carbonyl were measured. It was found that when cells were exposed to glucose oxidase the level of oxidative stress increased over time as reflected by the decrease of Glutathione. Interestingly, when melanin was added the level of oxidative stress decreased over time as reflected by increase in glutathione concentrations. It was also found that TNF-alpha decreased upon treatment by melanin but after 72 hours but not on 24 and 48 hours treatments. However, protein carbonyl and MDA appeared to be less affected by melanin treatments. These results may indicate that melanin is capable of diminishing the effects of oxidative stress on the cells at early stages probably by interfering with lipids peroxidation and production of reactive oxygen species.

Objective: The diabetes mellitus is most common diseases. Which are spread all over the world. At... more Objective: The diabetes mellitus is most common diseases. Which are spread all over the world. At they are change in modified in life style disease in this study where the prescribe drugs while using in the diagnostic and treatment of diabetes mellitus .the most commonly use drugs Sitagliptin +Metfomin in the community clinic in U.P. In the survey which are found to be the prescription pattern in Jajmau (Kanpur, U.P.) areas the most common drug which are running Sitagliptin + Metformin the survey which are randomly collect the prescription there are many variation in prescribing pattern of diabetes mellitus .the prescribing pattern is most strong tools to role of drug use in the society which are treat the DM during medication follow the proscription pattern of the drugs. There is need for appropriate safe &effective treatment and economical study to find out the pattern of drug therapy among DM. Methods: In this study the method randomized and non randomized study design was conducted in October 2016 – November 2016 community clinic in U.P. this study found to the date which group gender in fasting blood sugar various classes of drugs analyzed them. Results: A total of 200 patients were included in this one month's study. All the patients had Type 2 diabetes. Metformin is the drug of choice and Sitagliptin is the most preferred combination with Metformin. Conclusions: Insulin was not preferred as mono-therapy. Despite combination therapy, the postprandial glucose levels were not in range– suggesting either poor patient compliance or inadequate dosing/inappropriate therapy. In addition to drugs, the services of a clinical pharmacist might be helpful in these patients. Metformin is the drug of choice and Sitagliptin is the most preferred combination with Metformin.

Objective: The objectives were to study the in-vitro and in-vivo aldose reductase and in-vitro ad... more Objective: The objectives were to study the in-vitro and in-vivo aldose reductase and in-vitro advanced glycation end products formation inhibitory activities of the standardized extracts of Picrorhiza kurroa roots and Hibiscus rosa-sinensis flowers. Methods: In-vitro Aldose reductase inhibitory activity was studied by using isolated rat lens and kidney Aldose reductase by UV-Visible spectro photo metric method by using Quercetin as reference compound. In-vivo Aldose reductase inhibitory activity was evaluated by using experimental rat models of galactosemia and the final lens galactitol was evaluated by High performance liquid chromatography and Gas chromatography methods by using Quercetin as reference compound. In-vitro advanced glycation end products formation inhibitory activity was estimated by using laboratory test reaction with protein and sugars by spectro fluorimetric method by sung aminoguanidine as reference compound. Statistical analysis of the results was done by using Analysis of the variance method. Results: The plant extracts were found to possess significant aldose reductase and advanced glycation end products formation inhibitory activity. Conclusions: More study is required for isolation and characterization of the chief chemical constituents responsible for the biological activity of the plant extracts.

Objective: The aim of the study was to determine the level of bacterial contamination of door han... more Objective: The aim of the study was to determine the level of bacterial contamination of door handles/knobs of toilets and bathrooms at Daeyang Luke Hospital. Methods: Fomite can be described as a non-living object capable of carrying infectious organism and it is considered as one of the major source of spread of hospital acquired infection. In this study, door handles/knobs were swabbed with sterile swab stick moistened with sterile water. The content was evenly transferred to nutrient agar petric dish and then incubated for 24 hours at 37˚C. The study was done between the months of May to August 2016. Results: The results of the study showed that during the period of study there was 41.6% bacterial contamination with the female medical and surgical ward toilets being more contaminated as compared to staff toilets. Private room bathrooms were more contaminated during the period of study as compared to the staff room bathrooms that were less contaminated. Among the bacterial contaminant isolated and identified, Staphylococcus aureus had the highest prevalence followed by Escherichia coli, Pseudomonas aeruginosa, Citrobacter species and Klebsiella pneumoniae respectively. Conclusions: Therefore, from the study, it can be concluded that general public needs observe hand hygiene and use of quality disinfection procedures in order to reduce hospital acquired infection.

Objective: In this study, the antipyretic effect of different extracts obtained from Matricaria c... more Objective: In this study, the antipyretic effect of different extracts obtained from Matricaria chamomilla L. (MC), Ormenis mixta L. (OM) and Pistacia atlantica DESF. (PA) was investigated experimentally in rats. Methods: Antipyretic activity of aqueous extracts was evaluated by yeast induced pyrexia method. The antipyretic effect was retained in all extracts tested and was comparable to that of paracetamol used as the standard drug negative control group (distilled water). The extracts were also phytochemically screened for alkaloids, tannins, saponins, flavonoids, terpenoids, quinones and anthraquinones. Results: Treatment with aqueous extracts at dose of 400 mg/kg showed a significant (p≤0.05) reaction of pyrexia in rodents. The results suggest that this Moroccan medicinal plants possesses potent antipyretic activity. Phytochemical screening of the plants showed the presence of flavonoids, terpenoids, saponins, tannins, alkaloids and quinons which may responsible for this activity. However, anthraquinones were absent in all plants and alkaloids from PA. Conclusions: This study might be the first formal report on antipyretic effects of these three plants in Morocco.

The major objective of any dosage form is to deliver an optimum therapeutic amount of active agen... more The major objective of any dosage form is to deliver an optimum therapeutic amount of active agent to the proper site in the body to attain constant & maintenance of the desired drug concentration. Mucoadhesive drug delivery systems are effective delivery systems with various advantages as compared to other oral controlled release dosage forms in terms of drug delivery at specific sites with prolonged retention time of drugs at target sites. The main advantage of these systems includes avoiding first pass metabolism of the drugs and hence availability of high drug concentration at target site. Oral mucoadhesive systems have potential ability for controlled and extended release profile so as to get better performance and patient compliance. The present manuscript briefly reviews the benefits of mucoadhesive drug delivery systems, mechanisms involved in mucoadhesion, different factors affecting mucoadhesive drug delivery systems.

Objective: In the present work, RP-HPLC procedure is optimized to finalize a different approach f... more Objective: In the present work, RP-HPLC procedure is optimized to finalize a different approach for the estimation of rivaroxaban in tablet dosage form. A novel drug rivaroxaban used as anti-coagulant in the patients for the prevention of thromboembolism. Methods: The molecule is identified with the molar mass of 435.882 g/mol and molecular formula C19H18ClN3O5S. The determination was executed by C18 column (Phenomenex 250 x 4.6 mm, 5 μm maintained at 35°C) at 251 nm with a mobile phase (ACN: Water, 55:45 v/v) and flow of 1.2 ml/min. Results: The retention time found to be about 3.8minutes.The validation parameters performed as per ICH guidelines and found to be within acceptance criteria. Linearity of the method is found to be accepted across five concentration level i.e. being studied by calibration curve. Accuracy was executed at three different concentrations, the amount being recovered are close to 100%. The % RSD values obtained for repeatability, intermediate and reproducibility under precision are within acceptance criteria. Conclusions: The method was accurate, precise, robust and rapid for quantitative determination of rivaroxaban by High Performance Liquid Chromatography.
Objective: A simple, specific, accurate and precise RP-HPTLC method has been developed and valida... more Objective: A simple, specific, accurate and precise RP-HPTLC method has been developed and validated for simultaneous estimation of Avanafil and Dapoxetine. Methods: The chromatographic separation was achieved on Aluminium plates precoated with Silica gel 60 F254 using chloroform: methanol: ethyl acetate: glacial acetic acid (5:2:3:0.2, v/v/v/v) as mobile phase detected at 279 nm. Results: The correlation coefficient for RP-HPLC method was found to be 0.9987 for Avanafil and 0.9991 Dapoxetine and the linearity range was found to be 1040-3640 ng*spot-1 for Avanafil and 80-280 ng*spot-1 for Dapoxetine. Conclusions: The developed method was successfully applied to marketed tablet dosage form and the results were found with higher confidence.

Objective: The objective of present research work was to develop formulation of orodispersible ta... more Objective: The objective of present research work was to develop formulation of orodispersible tablets of Ivabradine HCl and evaluate it for different evaluation parameters. Methods: The tablets were prepared by direct compression method. The formulation of the tablets were evaluated before compression for characterization of flow properties and after compression for different parameters of orodispersible tablet formulation. Results: Ivabradine hydrochloride orodispersible tablets were developed with considerable increase in drug release as compared to marketed formulations; nine formulations were developed and studied. The difference in drug release values was found to be 100.88 ± 0.10 respectively. The drug was characterized according to different compendial methods, on the basis of identification by HPLC, pH, organoleptic properties and other tests. Parameters evaluated were within prescribed limits and indicated good free flowing properties. The F6 batch with disintegration time 21 ± 3.0 and dissolution 99.29% was selected as optimized formulation. This was compared with conventional marketed formulation and was found superior. Batch F6 was also subjected to stability studies for two months and was tested for its hardness, wetting time, disintegration time, drug contents and dissolution behaviour monthly. Conclusions: By appropriate selection of excipients, it was possible to develop orodispersible tablets of Ivabradine HCl.

Objective: This study investigated the antibacterial activity of the acetone, methanol, and ethan... more Objective: This study investigated the antibacterial activity of the acetone, methanol, and ethanol leaf extracts of Azadirachta indica and Psidium guajava against methicillin resistant Staphylococcus aureus (MRSA) and vancomycin resistant Staphylococcus aureus (VRSA) strains as well as the antimicrobial activity of some conventional antibiotics on these multidrug resistant organisms. Methods: MRSA and VRSA strains were obtained from the culture collection unit of a tertiary hospital in Ebonyi State, Nigeria. The test organisms and the plant extracts were processed using standard microbiology techniques. Kirby-Bauer disk diffusion technique was used to determine the antimicrobial susceptibility profile of the MRSA and VRSA strains to some conventionally used antibiotics; and the antibacterial activity of the plant extracts was evaluated using agar well diffusion technique with three solvents: ethanol, methanol and acetone. Results: It was revealed in this study that the extracts of A. indica and P. guajava demonstrated some level of antimicrobial activity against the test organism at concentrations of 100 mg/ml and 50 mg/ml. Compared to the conventional antibiotics used, the antibiotics showed better antimicrobial activity against the test organisms than the plant extracts which was least active against the MRSA and VRSA strains. Conclusions: Though the A. indica and P. guajava extracts showed some appreciable antimicrobial activity against the MRSA and VRSA strains, the conventional antibiotics produced better antimicrobial action against these multidrug resistant bacteria. The search for novel compounds with putative antimicrobial activity should be stepped up since plants holds the potential for discovering novel drugs.

Objective: Lysin specific demethylase 1 (LSD1) inhibits the tumor suppressor activity of p53 and ... more Objective: Lysin specific demethylase 1 (LSD1) inhibits the tumor suppressor activity of p53 and facilitates the progress of tumor. In order to check the tumor growth, the activity of LSD1 enzyme is to be blunted. Methods: Phytochemicals from naturally occurring plant-based anti-cancer compound-activity-target (NPACT) database are screened with LSD1 as target applying genetic algorithm (GA) method to study best ligand poses and free energy of binding using Argus Lab. The prediction of drug-likeness and oral toxicity of the ligands are performed by the online tools Molsoft and ProTox respectively. Results: Calyxin H shows optimum binding affinity to both the substrate and FAD binding sites of LSD1. The LD50 value (median lethal dose) of calyxin H is more than 1000 mg/kg body weight and the toxicity class is 4. Conclusions: Calyxin H is the inhibitor of choice against target LSD1. The lead molecule may be the future potential herbal drug for cancer treatment.

The article reviewed various therapies other than dopamine treatment like A2a antagonists: antipa... more The article reviewed various therapies other than dopamine treatment like A2a antagonists: antiparkinson medication reducing the over reactivity of substantia nigra due to loss of dopamine; Levodopa/Carbidopa Intestinal Gel: an aqueous gel containing levodopa and carbidopa; stem-cell therapies like embryonic and adult stem cell can be act through several mechanism; acupuncture: reduced the motor symptoms and other disease related factors; various antiparkinson medications like IPX066 and ND0611 are sustained release and transdermal patches which are transported to GIT through high nutrients and patches are found to be useful in increasing the concentration, half-life of levodopa, thus downs the threatening risk of PD. The future treatment for PD should be considered as they have less side-effect and better results than other treatment as they not only decrease the symptoms but also the incidences of PD. If the symptoms are diagnosed early patient should go for genetic therapy to relieve from the disease which not only reduce the progressive increase of symptoms and disease. Considering all therapies, future treatments shows the weightage in reducing the progressive increase of PD in patient. Though these treatments are proven to be effective in treatment but still more targeted tools and techniques are required which can specifically target the cause and thus lowers the graph and rating scale of PD.

Alopecia is characterized by hair loss mainly on scalp some time on other resign of the body that... more Alopecia is characterized by hair loss mainly on scalp some time on other resign of the body that has negative psychological and social impact on patients. Androgenetic alopecia and alopecia areata are common disorders. Androgenetic alopecia is the sensitivity of scalp follicles to dihydrotestosterone and alopecia areata is an autoimmune disorder. Current studies have explained the efficacy of corticosteroid therapy or the combination of ultraviolet A therapy and systemic corticosteroids for severe AA. Finasteride opens up new possibilities for the treatment of androgenetic alopecia. Current drug treatment approaches use regrowth stimulators such as minoxidil and finasteride for androgenetic alopecia, as well as corticosteroids, PUVA therapy for alopecia areata. Targeted delivery to the Hair follicle units helps faster targeting to cells that accelerate drug action by faster availability of drug, novel combination treatments combinations like tretinoin with minoxidil shows better results, gene therapy are new approaches that are under developing stage and giving satisfactory results on animal as well as humans.
Bell's palsy is a unilateral, lower motor neuron weakness of the facial nerve. Facial dysfunction... more Bell's palsy is a unilateral, lower motor neuron weakness of the facial nerve. Facial dysfunction has a dramatic effect on a patient's appearance, psychological wellbeing and quality of life. Bell's palsy has been described in patients of all ages, and is more common in adults than in children.The causes of the paralysis still remain unknown. Establishing the correct diagnosis is imperative and choosing the correct treatment options can optimize the likelihood of recovery. Hence this review deals with etiology, signs and symptoms, diagnosis and treatment management for Bell's palsy.
Molecularly targeted agents light at end of tunnel to resolve therapeutics by drawing together mo... more Molecularly targeted agents light at end of tunnel to resolve therapeutics by drawing together morbidity and mortality in patients by the whole of cancer. However, still an urgent has a passion for preferably effective anticancer compounds, state-of-the-art preclinical abused substance evaluations largely overlook to answer a need the demand. New preclinical strategies, including the review of with all the extras mouse models and co-clinical design designs, are for used to boost the predictive price tag of animal-based translational aries research. Here, we saw in a new light the society of born with a silver spoon preclinical antineoplastic agents, their associated limitations, and arbitrary methods to feel in one bones clinical outcomes.

Objective: The objective of the present research was to develop a matrix embedded floating tablet... more Objective: The objective of the present research was to develop a matrix embedded floating tablet of Metoprolol for the sustained activity and prolongation of gastric residence time to improve the bioavailability of the drug. Metoprolol was chosen as a model drug because it is better absorbed in the stomach than the lower gastro intestinal tract. Methods: The experimental work was divided into pre-formulation studies, formulation development, and evaluation. Standardization of drug and excipients confirmed the authentication of the samples. Floating test were conducted for all formulations, In vitro dissolution studies were carried out in a dissolution testing apparatus-II, FTIR study was performed to interpret the drug ,excipient interaction. Results: Floating tests were also performed for 15 formulations and among them five formulations have passed the floating tests (F1, F3, F5, F7, and F14). The In-vitro release kinetics study of this tablet indicated sustained release for Metoprolol and followed zero order release and 95% drug in 8 h in vitro. The drug release profile of formulated product was compared with marketed product Metolar. The floating tablets extended the drug release up to 8 hours. The drug-polymer interaction was evaluated by fourier transform infrared spectroscopy (FTIR). Conclusions: F3 formulation showed the best floating results. The comparative study between F3 and Metolar (Marketed Product) showed the similar in vitro drug release profile. Thus, the optimzed formulation F-3 can be successfully used for the management of hypertension.

Objective: The present work was executed to evaluate the anti-diabetic potency of a polyherbal pr... more Objective: The present work was executed to evaluate the anti-diabetic potency of a polyherbal preparation. The objective of this study is to induce experimental diabetes mellitus using streptozotocin in normal Albino wistar rats and study the antdiabetic activity of polyherbal formulation by comparison of changes in levels of glucose between normal and diabetic rats. Methods: The effect of methanol extract of poly herbal preparation containing aerial parts of Schrebera swietenoides, roots of Barleria montana and aerial parts of Rotula aquatica was investigated in normal and streptozotocin induced diabetic rats. Results: The lowest blood glucose levels were observed at 4 and 8 th hr after the oral administration of 150 and 300 mg/kg b.w polyherbal formulation. The blood glucose levels at 24hrs after the oral administration of 150 and 300 mg/kg b. w of poly herbal formulation was significantly lowers the blood glucose levels. Conclusions: The display of synergy or antagonism by the composite herbal extracts in ameliorating hyperglycemia depended on the type and number of individual herbal extract used in constituting the experimental herbal formulations.

Objective: The Present investigation was performed to find out the effect of synthetic and natura... more Objective: The Present investigation was performed to find out the effect of synthetic and natural polymers on the release properties of glimepiride matrix tablet. Glimepiride is a first third generation sulphonyl urea agent for the treatment of type-II diabetes mellitus. Methocel K15M, Olibanum Gum were used as key release modifying polymers. Methods: Nine formulations were prepared taking different concentration of natural and synthetic polymers, The drug excipient mixtures were subjected to pre-compression studies. The tablets were prepared by direct compression method; all formulations were subjected to physicochemical studies, in-vitro drug release, kinetic studies and stability studies. The physicochemical results were found within the limits. Results: FTIR study interpretation did not show any drug–excipient interaction The drug release from the optimized formulation F-7 was extended for a period of 12 hours. The release kinetics of F-7 formulation showed that the release of drug follows zero order models. The optimized formulations were subjected to stability studies and shown there were no significant changes in drug content, physicochemical parameters and release pattern. Conclusions: Results of the present study indicated the suitability of the above mentioned polymers in the preparation of sustained release formulation of Glimepiride for the management of type-II diabetes mellitus effectively.
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Papers by Pharmaceutical and Biological Evaluations