bluuebunny/crossref_metadata_2025 huggingface dataset:
Investigating Drug Properties of Bioactive Compounds of Cymbopogon citratus by Absorption, Distribution, Metabolism, Excretion/Toxicity and Molecular Docking Analysis Against Apolipoprotein N-Acyl Transferase
Authors: BISWAL R ABHISHEK , Sharif S Riyaz , Pazhamalai Vivek
Published: July 2021

Delivering a potential drug is a predominant challenge in medicinal chemistry.in this study, bio organic compounds of Cymbopogon citratus was screened by analysing physiochemical properties like solubility, permeability, efficacy, toxicity, and metabolic stability. The optimization of drug potential against virulent protein was calculated by using docking algorithm Autodock 4.2.3. Structure based ligand docking reveals that the compounds having better inhibition potential against virulent enzymes with insoluble and impermeable activities. The organic compounds of Cymbopogon citratus were screened using Lipinski rule of five and ADME/T prediction for drug likeliness. The structure based ligand docking was done between bioactive compounds of plant and virulent protein that cause diseases. The interaction was visualized using Discovery studio and was studies. The molecular docking of bioactive compounds resulted in better inhibition potential with controlled lipophilicity level, without causing toxicity that harms the natural habitat of humans. The compounds, 1,3,4-trimethyl -3cyclohexene-1-carboxaldehyde exhibit binding energy -4.70 Kcal/mol followed by β-myrcene – 4.35 Kcal/mol and Geraniol -4.35 Kcal/mol. Hence, structure based ligand docking and in silico ADME/T studies revealed that the compounds have better inhibition potential against Apolipoprotein by improving the prediction of drug compounds.
Antibacterial activity of desiccated cyanobacterium Anabaena sp. isolated from terracotta monuments of Bishnupur, West Bengal
Authors: Bhakat Shailen , Saha Subarna , Mandal Sikha , Rath Jnanendra
Published: July 2021

Anabaena sp. are the dominant cyanobacterial species on terracotta monuments of Bishnupur which exposed to high solar radiation, ultraviolet and in a desiccated condition in most part of the year. In the present study three Anabaena species were isolated from crust samples and its antibacterial activities were evaluated against pathogenic bacteria Bacillus subtilis, Listeria monocytogenes, Staphylococcus aureus, Salmonella typhimurium, Escherichia coli. We observed good antibacterial activity in ethyl acetate and ethanol extract of Anabaena sp. (VBCCA 052002) which having highest antibacterial activity against Staphylococcus aureus, Salmonella typhimurium, Staphylococcus aureus and E. coli respectively. We have validated the antibacterial assay by using resazurin based antimicrobial assay in microtiter plates and calculated the MIC value of ethyl acetate extract of Anabaena sp. (VBCCA 052002) which is found to be 100 µg/ml against Staphylococcus aureus and 150 µg/ml against Salmonella typhimurium.
Green reactants act as natural precursor for facile synthesis of nanoparticles using Withania Somnifera
Authors: Anburaj Rajeswari
Published: July 2021

Nanotechnology includes physical and chemical approaches intended for their phytofabrication of metal nanoparticles. Most of the time, these methods are not as safe as these are associated with the utilization of extremely noxious and hazardous substances that produce biological problems. Due to their manifold applications, various biological methods are gaining admiration for the fabrication of silver nanoparticles (AgNPs). The utilization of vegetative parts in the biosynthesis of nanoparticles (NPs) emerges as a commercial and ecological approach. The spectroscopic profile confirms the occurrence of a functional peak at 360 nm. Fourier transform infrared spectroscopy (FTIR) studies indicate that phenol groups are responsible for phytofabrication of NPs. The results of microbicidal screening confirm that broad spectrum of inhibition was found to be observed in 400 μL of biosynthesized AgNP against E. coli (23 mm) and B. cereus (22.3 mm) Therefore, the progress of simple photosynthesis methods avoid deleterious and harmful properties has fascinated major attention in this field.
Curcumin Reverses the Scopolomine-induced Cognitive Impairment by iNOS and Acetylcholinesterase Inhibition in Rodent Model of Schizophrenia
Authors: Khan Henna , CHAUDHARY AMIT , ALI KHAN RASHID , ALI WAZID
Published: July 2021

Schizophrenia is a severe neuro-developmental psychiatric disorder. Curcumin is a polyphenolic compound extracted from turmeric. It is known for its antioxidant, anti-inflammatory, neuroprotective, and precognitive properties. The purpose of the current study was to evaluate the role of curcumin in scopolamine induced cognitive impairment in animal model of schizophrenia. The elevated plus-maze test was utilised to study the curcumin effect on learning and memory. Curcumin (100 mg/kg, i.p.) was administered daily for 28 days in animals. Behavioural tests such as transfer latency (TL) and spontaneous alteration behaviour was assessed after the last dose of curcumin on the 28th day, followed by biochemical estimations. Present study reported that curcumin showed anti-amnesic effect in animal models of cognitive impairment of schizophrenia. Curcumin reduced the TL compared to toxic control group (scopolamine per se) (P <0.001) in elevated plus maze. In spontaneous alteration behaviour test, curcumin significantly increased percentage alteration and possible alteration as compared to toxic control group (P <0.001). A significant change in acetyl cholinesterase activity, nitrate and oxidative parameters was observed, thus, confirming its anti acetyl cholinesterase, NOS (nitric oxide synthase) inhibition and antioxidant properties (P <0.05). The present study put forward the claim of curcumin as a new and safer therapeutic alternative for the treatment of cognitive impairment in Schizophrenia. The underlying mechanism of this potential effect may be related to anticholinesterase and nitric oxide synthase inhibition activity of curcumin. Further research is warranted for confirming the suggested pathways accountable for memory alleviating effects of curcumin in Schizophrenia.
Design, fabrication and evaluation of microemulsion based gel of essential oil of thymus vulgaris for superficial fungal infections
Authors: Gandhi Jeet V. , Suthar Disha J. , Patel Hetal K. , Shelat Pragna K. , Parejiya Punit J.
Published: July 2021

Although fungus being part of the commensal skin micro-structuring, various pathogenic commensals colonizes on human skin leading to superficial fungal infections.  Owing to the resistance of present therapeutic treatments available, microbial resistance and serious hypoallergic reactions have been a concern to explore the phyto-therapeutic nutrients for treatment of fungal infections. One such plant essential oil-based formulation is thyme oil derived from the leaves of thymus vulgaris. The aim of present work i.e. development of thyme oil based microemulsion for treatment of fungal infections due to candida and trichophyton species. The thyme oil loaded microemulsion based gel was constructed using D-optimal design and the optimized final formulation contains 0.82% of oil, 9.22% of Smix and 89.95% of water. The optimized microemulsions was pale yellow to amber transparent microemulsion with globule size of 14.23 ± 0.3 nm, zeta potential of -0.69 mV and PDI value 0.00143 indicating a stable microemulsion. The microemulsion based gel formed had a pH of 6.03, appreciable viscosity and rheological properties. The drug release of formulation was 100.0 ± 0.22%. The % of drug permeated in skin layers was found to be 15.53 ± 0.22%. While % drug retention on the skin surface was found to be 26.32 ± 0.26% and within skin layers was found to be 58.47 ± 0.22%.  The microemulsion based MBG was found to be safe on the dermis and efficacious then the marketed product and hence, promises its utilization as a safe and efficacious formulation for treatment of dermal infections.
Protective Effect of Diosgenin on Streptozotocin Induced Diabetic Nephropathy in Experimental Rats
Authors: Jain Pankaj G. , Patil Dipali J. , Nayase Priti G. , Surana Sanjay J. , Patil Pramod P.
Published: July 2021

Diabetes mellitus is a multifactorial metabolic disorder associated with the diabetes related vascular diseases. Oxidative stress along with inflammation is the Key factor leading to diabetic complications. Present study was designed to investigate the protective role of diosgenin, a steroidal saponin, in diabetes induced early kidney injury and oxidative stress markers and histopathological changes in kidney of diabetic rats, induced by single intra-peritoneal injection of streptozotocin (55 mg/kg weight (b.w.). After 72 hrs, experimental rats received diosgenin at different doses (10, 20 and 40 mg/kg b.w.) once daily for four weeks. At the end of the experiment, diabetic rats showed a significant increase in the levels of plasma glucose, glycosylated hemoglobin with a significant decrease in insulin and total hemoglobin. The activities of antioxidant enzymes such as superoxide dismutase, catalase, reduced glutathione, and the levels of reduced glutathione were decreased while increases in the levels of lipid peroxidation markers were observed in kidney tissues of diabetic rats. Oral administration of diosgenin to diabetic rats considerably shrivelled the plasma glucose and exaggerated the endocrine level supported a dose dependent manner. Diosgenin at a dose of 40 mg/kg b.w. was more pronounced effect than the other two doses and used for further studies. All the manifestations observed in diabetic rats were significantly reversed to near normal at a dose of 40 mg/kg b.w. of diosgenin. These findings recommend that diosgenin may have a helpful role against excretory organ harm evoked by aerobic stress within the diabetic state.
IN VITRO ANTIDIABETIC ACTIVITY BY GLUCOSE UPTAKE OF YEAST CELL ASSAY AND ANTIOXIDANT POTENTIAL OF ANNONA RETICULATA L. LEAF EXTRACTS
Authors: Pulivarthi Vineela , Josthna Penchalaneni , Naidu Challagundla Varadarajulu
Published: July 2021

The undesirable adverse effects of present available synthetic drugs endorse the modern medicine to search the superior choice for the treatment of metabolic diseases. Herbal medicine turns out to be a hopeful therapy for the effective treatment of diabetes in foreseeable future. In an effort to render a scientific evidence for the antidiabetic potential of Annona reticulata L., the present research, with the objective to evaluate the ability of A. reticulata leaf extracts on antihyperglycemic property under in vitro using yeast cell model was performed. Besides, as the diabetes and its complications are highly associated with the oxidative stress, the current study was also focussed on antioxidant property of A. reticulata leaf extracts. The scavenging ability of plant extracts on free radical 2, 2 – diphenyl- 1- picrylhydrazyl (DPPH), ferric reducing power assay and total antioxidant activity were performed to establish the antioxidant potential of A. reticulata leaf extracts. The in vitro antidiabetic ability of A. reticulata leaves was evaluated by glucose uptake method using yeast cell model. Among the four chosen solvent extracts- aqueous, methanol, ethyl acetate and n-hexane, methanol extract (MeE) exhibited high antioxidant potential. MeE exhibited 62.28% of DPPH inhibition at 200µg/ml, with total antioxidant activity 164.72 ± 2.63µg/ml and higher absorbance in reducing power assay (1.15 ± 0.03).  In vitro antidiabetic activity by glucose uptake of yeast cell assay was evaluated and observed dose dependant rise in % of glucose uptake in methanol, ethylacetate and aqueous extracts of A. reticulata. MeE showed 48.55% of glucose uptake at 500µg/ml concentration. Hence the present study could be concluded as A.reticulata leaves possess potent antioxidant activity and antidiabetic activity under in vitro conditions. With the outcome of the present initial study, research work could be extended further; thereby the exact pharmacological action of the plant compounds could be discovered.
SYNTHESIS AND EVALUATION OF 7-(2-((SUBSTITUTED PHENYL) IMINO)-2-PHENYLETHOXY)-4-METHYL-2H-CHROMEN-2-ONES AS ANTIFUNGAL AGENTS
Authors: Gupta Mohit , Kumar Sushil
Published: July 2021

In the context of the dangerous phenomenon of antimicrobial resistance to the available drugs, we present here the synthesis and evaluation of 7-(2-((substituted phenyl) imino)-2-phenylethoxy)-4-methyl-2H-chromen-2-ones as antifungal agents. Among the compounds, SB-4 was found to be most potent against Candida albicans when compared with the reference drugs Clotrimazole and Terbinafine. The molecular properties of the newly target compounds were performed by online software, and results showed good drug-like properties. The results showed target compounds further optimized as lead compounds as anti-Candida potential.
Development and Evaluation of Novel Bionanoparticles Loaded with Nanosized Lamotrigine by Using the Novel Isolated Biopolymer from Phaseolus vulgaris Seeds
Authors: Kumar Sushant , Satheesh Madhav Nookala Venkala , Verma Anurag , Pathak Kamla
Published: July 2021

The aim of this research was to isolate and characterize the novel biopolymer from Phaseolus vulgaris seeds and to formulate lamotrigine loaded bionanoparticles using this biomaterial. The biopolymer was isolated by simplified and economical process and analysed for different physico-chemical and spectral properties. The nanosizing of lamotrigine was done by bath sonication method and its particle size in nano-range was screened by UV method. The bionanosuspension loaded with nanosized lamotrigine was prepared by bath sonication for 15 cycles (1cycle equal to 3 minutes). The formulated bionanosuspension loaded with lamotrigine using biopolymer was compared with lamotrigine loaded bionanosuspension by using HPMC.  The bionanosuspension was subjected for pH study, dispersibility study, % entrapment efficiency, nanosizing screening, particle size study and in vitro study for drug release and stability study of formulated bionanosuspension. The best formulation LPVu7 showed up to 90.36 ±0.9% drug release in 36 hours. having t 50% of 17 hours and t80% of  29 hours with r2 value of 0.9927 as compared to release from LSP5 with 92.43±0.68%   having t 50% of 16 hours and t80% of  28 hours with r2 value of 0.9951 in  36 hours. The results reveal that isolated biopolymer may be used as an alternative to synthetic polymer because of its novel inbuilt bioretardant cum biostabilizing properties. The formulated bionanosuspension are feasible for delivering the nanosized lamotrigine in sustained manner for prolonged time for long term treatment of epilepsy.
Analyzing the role of phytochemicals in targeting drug transporter protein ABCC6 using molecular docking and molecular dynamics simulations
Authors: Pandya Heena , Patel Chirag N. , Bhavsar Mansi , Pandya Pujan N. , Patel Saumya K. , Rawal Rakesh M.
Published: July 2021

Triple negative breast cancer (TNBC) is an aggressive breast cancer subtype that lacks hormonal receptors. This reduces the therapeutic options for TNBC patients creating more focus on chemotherapy. Drug resistance has posed as a major hurdle in treating TNBC patients. Deregulation of drug transporter proteins is one of major factors that cause resistance to chemotherapeutic drugs. In this study, ABCC6 a drug transporter protein that is found dysregulated in several resistant cancer cells has been docked with natural compounds or phytochemicals with known anti-cancer activities. Subtrifloralactone G, a withanolide extracted from Deprea subtriflora is found to show highest binding energy with ABCC6 protein. Molecular dynamics simulations further prove the stability of the ABCC6 protein- Subtrifloralactone G ligand complex. ADMET analysis shows that phytochemical Subtrifloralactone G can be used as an anti-cancer therapeutic drug in treating resistant cancer cells. The study mainly focuses on the role of phytochemicals in treating resistant TNBC cells.
Enhancement of Solubility And Dissolution Profile of Clopidogrel By Various Solid Dispersion Formulations
Authors: Khader Mohammed Abdul , Salfi Roshan
Published: July 2021

The present research is aimed at enhancing solubility and drug dissolution of clopidogrel (CPG) used as oral antiplatelet agent by employing solid dispersion (SD) technique. Total 40 SDs formulated with  drug: polymers (pluronic F127, poloxamer 407, labrafil PG, PEG 6000, gelucire 50/13), in varying ratios (1:0.5, 1:1, 1:2, 1:3, 1:4) of which CPG1 to CPG20 and CPG21 to CPG40 prepared by adopting solvent evaporation  method fusion (melt) method respectively. The formulation CPG40 containing pluronic F127 as polymer showed highest solubility of 6.57±0.04 mg/ml) that is 45 folds than pure drug. Similar results  reflected in the dissolution studies where CPG40 containing CPG: pluronic F127 in 1:4 ratio showed maximum % drug content, % practical yield and drug dissolution of 99.14% in 60 minutes when compared with other formulations and pure drug (32.76%) obtained  by fusion melt method. From FTIR studies the optimized formulation CPG40 showed the compatibility between drug and polymers. XRD and SEM studies showed CPG40 exists in amorphous form that fetched in better drug release from the SD formulation in comparison to pure drug.
High rate prevalence of asymptomatic SARS-CoV-2 infection: Comparative epidemiology with other pandemic flu and impact on COVID 19 control measures
Authors: Bigoniya Papiya
Published: July 2021

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a novel coronavirus responsible for CODIV 19 pandemic, an international public health emergency. Conventional routes of transmission of SARS-CoV-2 are respiratory droplets and direct surface based contact, similar to SARS-CoV, Middle East respiratory syndrome-related coronavirus (MERS-CoV), and highly pathogenic influenza. Some clinical features of infectivity and viral susceptibility of SARS-CoV-2 are similar to SARS-CoV-1, MERS-CoV, suggesting a difference in the viral tropism despite the phylogenetic homogeneity. The incubation period of SARS-CoV-2 is in line with other coronaviruses, but with lower case fatality rate, although the presence of comorbidities can make it highly lethal. The major concern with SARS-CoV-2 is its ability to spread silently by the asymptomatic and presymptomatic carriers. About 70-80% positive cases of COVID 19 is coming out to be asymptomatic, presymptomatic, or very mild symptomatic which dangerously higher compared to SARS-CoV-1, MERS-CoV, H1N1, and seasonal influenza. Asymptomatic and presymptomatic carriers based silent spreading of SARS-CoV-2 has become a major concern due to short serial interval, and soaring level of virus shedding from the upper respiratory tract. Asymptomatic transmission is making containment measures difficult to implement, now early detection and isolation of asymptomatic and presymptomatic persons can be an effective strategy to control spread. High transmutability and silent infection rate SARS-CoV-2 will hopefully help in the fast development of community herd immunity, assuming to have 12 to 14 months active spread period compared to 18-24 for previous pandemic flu. Mass screening by rapid antibody tests, especially in congregate living conditions, mandatory use face masks, social-distancing, and strict execution of sanitization practices even after the relaxation of lockdown, can effectively help to control the COVID 19 infection rate.
Microarray data analysis, structure prediction and in silico docking of drugs for inhibiting the over expression of High Mobility Group A1 in human malignant neoplasias
Authors: Devgun Manish , Lal Sukhbir
Published: July 2021

The High Mobility Group A1 (HMGA1) gene over expression has been widely observed in various types of cancers. The raw data for microarray data analysis was obtained from the dataset record GDS3525. The SOM and K-means of the Genesis led to the identification of two clusters (each consisting of 30 genes) bearing HMGA1 gene. This on further analysis resulted into identification of 14 similar genes by Easy M-A. The evolutionary similarity of HMGA1 and GORASP2 is clearly observed in the Phylogenetic Tree. Due to the absence of precise structures, the homology modeling was done by using EasyModeller and the resulting models of proteins HMGA1 and GORASP2 were validated by Ramachandran plot. These models were further put to loop optimization by Modloop and the output models were assessed by Ramachandran plot (Rampage) and through SAVS (Procheck). The molecular docking was done by using Autodock, this resulted in two ligands, DB11641 (Vinflunine) and DB12674 (Lurbinectedin), showing potential for the effective treatment of various types of cancers characterized by the over expression of HMGA1 and GORASP2.
Bosentan loaded Microemulsion: A novel formulation and evaluation of their in-vitro and in-vivo characteristic
Authors: Prajapati Bhupendra , Varia Umang
Published: July 2021

The main objective of the research work was to improve the solubility of Bosentan by preparing Microemulsion (ME) for pulmonary artery hypertension therapy. Capmul MCM C8 was selected as oil, Tween 20 as a surfactant and Transcutol HP as a co-surfactant. From Pseudoternary phase diagram ratio of Smix (1:1) selected. From the Microemulsion area of ternary diagram different batches were prepared, but the drug was precipitate from the formulation which can be avoid by adding precipitate inhibitor. Pluronic F 127 was utilized as precipitate inhibitor in the concentration of 1.5%. The optimized formulation ME 8 contain oil (30 %V/V), Smix (60 %V/V) and water (10 %V/V). The prepared Microemulsion evaluated for globule size 96.71±0.11 nm, % transmittance 99.45±0.54 % and >99 % drug content. TEM confirm the spherical shape of globule. The physicochemical parameter of ME 8 was performed and to enhance the stability of Microemulsion it is converted in to solid ME by using adsorbent. Aeroperl 300 was selected as an adsorbent in the drug to adsorbent ratio (1:0.5 %W/W) based on physicochemical properties. From the in-vitro drug release investigation after 7 hours %CDR of ME 8 was found to be 78.87±0.17% and solid Microemulsion (SME 3) shows 76.83±0.29%. The pure drug shows only 27.63±0.23% CDR, which indicate that ME revealed better drug release than pure drug. There was a 2.8 fold increases in solubility compare to pure drug. From the In-vivo data compared to convention formulation, there was significant change in pharmacokinetics data observed.
Stability-indicating Reversed Phase-Ultra Performance Liquid Chromatography Method Development and Validation for Simultaneous Determination of Encorafenib and Binimetinib in Formulation
Authors: Raveendranath Taduvai Venkata , Saravanakumar Rajaiah Thangaraj , Male Anjana
Published: July 2021

A simple, accurate and precise stability indicating method was developed for the simultaneous estimation of the encorafenib (ECRB) and binimetinib (BMTB) in a dosage form by UPLC. Chromatographic elution was processed through a HSS C18 (100 x 2.1 mm, 1.8m) reverse phase column and the mobile phase composition of 0.01N KH2PO4 buffer (3.5 pH) and acetonitrile in the proportion of 55:45 was processed thru a column at a flow rate of 1.0 ml/min. Temperature of the column oven was kept at 30.0°C and the wavelength maximum of detection system was set to 294 nm. Retention times of ECRB and BMTB were found to be 0.767 min and 1.130 min respectively. Repeatability of the method was determined in the form of %RSD and findings were 0.3 and 0.6 for ECRB and BMTB respectively. The percentage recovery of the method was found to be 99.59% and 99.70% for ECRB and BMTB respectively. LOD, LOQ values obtained from regression equations of ECRB and BMTB were 0.51, 1.55mg/ml and 1.47, 4.44 mg/ml respectively. Regression equation of ECRB was y = 6684.x + 18102 and BMTB was y = 13118x + 2159. Two analytes were subjected for acid, peroxide, photolytic, alkali, neutral and thermal degradation studies and the results shown that the percentage of degradation was found between 0.76% and 6.88%. Retention times and total run time of two drugs were decreased and the developed method was simple and economical. So, the developed method can be adopted in industries as a regular quality control test for the quantification of ECRB and BMTB.
Identification of Novel Inhibitors for TG2 (Tissue Transglutaminase) and DJ-1 (Protein Deglycase) against Parkinson's Diseases by Pharmacophore-based Approaches
Authors: VAIDYA GAYATRI S. , NAIK V. UMAKANTH , Parvatikar Prachi
Published: July 2021

Parkinson’s disease (PD) is a one of the most common neurodegenerative disease affecting the central nervous system (CNS) characterized by the multitude of motor and non-motor clinical symptoms. The hallmark of PD motor manifestation include progressive tremor, rigidity, brady kinesia and postural instability. There are many protein involved in the progression of this dieses including TG2 and DJ-1 protein. The present is focused on finding the novel inhibitor based from phytochemicals catagory to inhibit activity of TG2 and DJ-1 protein. The Cheminformatics pipeline used which include ADMET analysis,pharmacophore modeling and molecular docking. Six best hit molecules were mapped with the E-pharmacophore features of TG2 and DJ-1 protein. These pharmacophore were further analysed by molecular docking, protein–ligand interactions and in silico ADMET studies. The molecular docking analysis revealed that hydroxywogonin and 2',3',5,7-Tetrahydroxy flavones had good binding energy and satisfied the Lipinski rule of five and had no toxicity.
A Comprehensive Review on Self-Nano Emulsifying Drug Delivery Systems: Advancements and Applications
Authors: Sokkula Srikanth Reddy , Gande Suresh
Published: July 2021

Lipid-based drug delivery systems are extensively reported in literature for enhancing the drug solubility, permeability and bioavailability. These systems include   simple oil solutions, coarse, multiple and dry emulsions, complex self-emulsifying, microemulsifying or nanoemulsifying drug delivery systems. Self-emulsifying systems are further classified as self-microemulsifying drug delivery systems (SMEDDS) and self-nanoemulsifying drug delivery systems (SNEDDS) are most prevailing and commercially viable oil based approach for drugs that exhibit low dissolution rate and inadequate absorption. Ever since the progress of SNEDDS, they drew the interest of researchers in order to deal with the challenges of poorly water-soluble drugs. SNEDDS is a proven method for enhancing solubility and bioavailability of lipophilic compounds. Considering the ease of large-scale production and the robustness of SNEDDS, several formulations techniques are commercially available. The stability of SNEDDS can be further enhanced by solidifying liquid SNEDDS. Controlled release and supersaturated SNEDDS received patient compliance with larger drug loading. Presence of biodegradable ingredients and ‘drug-targeting opportunities’ facilitate SNEDDS a clear merit and distinction amongst available solubility enhancement techniques. In this article attempt was made to present an overview of SNEDDS, their mechanism, formulation excipients and potentials of SNEDDS, recent advancements, advantages and disadvantages of SNEDDS formulations. The article also focuses on reviewing the application of SNEDDS in enhancing bioavailability of antihypertensive drugs.
Synthesis and Oral Hypoglycemic Activity of Some New Sulphonyl Linkage Thiazolidine-2,4-diones
Authors: Kawale Laxman , Nade Vandana , Deshmukh Rohini , DUMBARE MAHESH
Published: July 2021

Type 2 diabetes mellitus and its complications, decreases the quality of life in diabetic patients. Thiazolidine-2,4-diones are found to be better insulin sensitizing agents, acting on peroxisome proliferator activated receptor-γ (PPAR-γ) and decrease blood glucose level in diabetic patient. Therefore, in the present work, we synthesized 5-[4-(substituted) sulphonylbenzylidene]thiazolidine-2,4-diones and evaluated for their oral hypoglycemic activity. The synthesized compounds were further studied for their find out interactions with 2PRG protein with the help of docking score and also find out their predicated ED25 values. The results of synthesized compounds were showed significant decrease in blood glucose level as compared to positive control group. All synthesized compounds have shown good hydrogen bond interactions with 2PRG protein, docking score and predicted ED25 value as compared with reference drug, pioglitazone and rosiglitazone, respectively. Thus, sulphonyl linked thiazolidine-2,4-diones may be used as promising oral hypoglycemic agent.
Phytochemical, antioxidant and antidiabetic analysis of leaf and stem extracts of Memecylon malabaricum(C.B.Clarke)Cogn.
Authors: Tejavathi D.H. , Sumalatha B. S.
Published: July 2021

Memecylon malabaricum (C.B.Clarke) Cogn. belongs to the family Melastomataceae is one of the important medicinal plants in traditional system of medicine. It has been used to treat diabetes, bacterial infections, and skin disorders including Herpes. Hence, the present study deals with the analysis of stem and leaf extracts through GC-MS to identify the bioactive compounds. 29 in stem and 25 phytochemicals in leaf extract were identified. Based on the results of GC-MS analysis further studies were carried out to estimate phenols, flavonoids and total antioxidant activity. It was found that stem methanolic extract has slightly more quantity of phenolics than the leaf extract. However, leaf extract has shown a considerable amount of flavonoids and better antioxidant activity than stem extract as revealed by DPPH, ABTS and reducing power assay. Further, inhibition of the activity of α-amylase by leaf extract was detected through preliminary studies thereby supporting its traditional use to treat diabetes.
Determination of Spray Pattern and Plume Geometry of Combined Budesonide and Formoterol Fumarate pressurized Metered Dose Inhalation Aerosol
Authors: Kotak Ravindra , Pandya Chintan V. , Pandya Aditee C. , Rajput Avnish , Thakur Brajesh Kumar
Published: July 2021

Budesonide and formoterol fumarate pressurized metered-dose inhaler (pMDI) is combined aerosol dosage form. The label claim of this combined dosage form is 100 mcg of Budesonide and 6 mcg of Formoterol Fumarate per actuation. It is prescribed for the treatment of asthma and chronic obstructive pulmonary disease (COPD). Formoterol fumarate is an anti-asthmatic drug (Bronchodilator), and Budesonide is Anti Inflammatory drug (Glucocortico steroid).The objective of plume geometry and spray pattern study is to monitor the consistency and quality of a device when actuated. The plume and pattern study aims to develop a formulation with robust device which can deliver an accurate amount of drug directly to the lungs of a patient. The chemistry manufacturing and controls (CMC) guideline outlined the basic data required for spray pattern and plume geometry measurement for different pMDI devices. In 2013, draft guidance on bioavailability and bioequivalence (BABE) of pMDI published, which provides details on plume geometry and spray pattern, image collection and evaluation.In the present study, the spray patterns were collected at 2 distances 3 and 6 cm from the actuator device's exit. The spray pattern Ovality results at 3 cm show 2.52% variation and at 6 cm results show 4.31% variation. Method precision, ruggedness and robustness study for Spray pattern also performed at 6 cm distance from actuator orifice. The plume geometry was collected at 6 cm distance from the exit of an actuator device. Plume geometry results show that Plume height is found in the range 16.20 cm to 18.98 cm, Plume angle is found from 17.7–24.9°, and Plume width is found between 3.68 to 4.57 cm.
ANTIUROLITHIATIC ACTIVITY OF NATURAL CONSTITUENTS ISOLATED FROM AERVA LANATA FLOWERS
Authors: Naikal James Prameela Subhashini , Nagula Shilpika
Published: July 2021

A well-known traditional herb Aerva lanata, broadly used in India for treatment of different ailments such as urolithiasis. Pashanabheda is used as antiurolithiatic in Ayurveda. In the present study, flowers of A. lanata were selected for isolation of active constituents and screening for in vitro antiurolithiatic potentials, as literature supports that flowers have the highest quantity of natural components when compared with the other parts. Hydroalcoholic (80%-water, 20%-alcohol) extract of A. lanata flowers was prepared and fractionation with different organic solvents.. The two fractions (ethyl acetate and n-butanol) were subjected to isolation of active constituents using column chromatography technique, followed by purification of the isolated constituents by preparative high performance thin layer chromatography (HPTLC)and then the individual components were characterized by IR spectrophotometery. Finally, in vitro antiurolithiatic activity was screened by nucleation and aggregation assay. In the aggregation assay, gradual decrease in the calcium oxalate (CaOx) crystal nucleation as well as growth was observed by light microscopy. The findings of the nucleation assay indicate that phytoconstituents inhibited the crystallization of CaOx in solution. The size and the number of calcium oxalate crystals decreased with increasing concentration of the phytoconstituents. The increasing concentrations of Quercetin and betulin (100, 200, 300, 400 and 500 μg/mL) inhibited the CaOx crystal growth. The isolated quercetin and betulin from A. lanata have shown antiurolithiatic effect by significantly reducing the CaOx crystal growth.
Formulation and Evaluation of Flurbiprofen Solid Dispersions Incorporated Buccal Patches
Authors: Sadik Mohammed Jaffer , Khan Abdulla
Published: July 2021

Flurbiprofen is an anti-inflammatory drug used in treating rheumatoid arthritis and ankylosing spondylitis. The present work is aimed at overcoming the deprived solubility of flurbiprofen by solid dispersion (SD) technique. The current paper is  the continuance of the published solid dispersion by considering the best final optimized formulation containing flurbiprofen drug: AQOAT AS: SLS as drug: polymer: surfactant in 1:5:2 ratios, and incorporating it into buccal patches to overcome the gastric side effect and attaining  sustained drug release. In this study 15 buccal patches  were formulated  by adopting  solvent casting technique  using polymers like polyvinyl hydroxyethylcellulose (HEC), hydroxypropryl methyl cellulose E15 (HPMC E15), polyvinyl pyrrolidone (PVP), carbopol and analyzed  for the drug content, drug  diffusion, in-vivo dissolution  and stability studies. All SD loaded patches displayed superior drug release (95% to 99.96%) over 12 h. The formulation BP14 showed excellent drug release extended over 12 h with drug release of 99.96% whereas marketed formulation which is sustained release Tablet showed 96.86% drug release within 6 h. The drug release kinetics show that the buccal patches follow zero order release kinetics with correlation coefficient (R2) ranging between 0.905-0.971 and BP14 formulation shown best R2 value. All the formulations exhibited best fit to Higuchi model with R2 ranging between 0.9911 – 0.9962 indicating drug release by diffusion process. The results conclude that buccal patches are superior alternatives for flurbiprofen that facilitates enhanced drug release for prolonged period of time in the effective management of rheumatoid arthritis.
O modelo regulatório brasileiro : comentários à lei geral das agências reguladoras
Authors: Miranda Henrique Savonitti , Gonçalves Jonas Rodrigo , Siqueira Marcus Vinicius Barbosa
Published: July 2021

As agências reguladoras surgiram no Brasil com o propósito de regular as atividades econômicas transferidas à iniciativa privada, a partir de reformas promovidas no cenário econômico nacional, após a implementação de planos de desburocratização da máquina estatal. Para a empreitada, buscou-se a importação de modelos estrangeiros para as agências, em especial a dos países que também tinham laços com uma economia mais liberal que se erguia no Brasil, a exemplo dos Estados Unidos da América. Para tanto, houve um esforço para que se adequasse o modelo das agências ao ordenamento jurídico nacional, em que, apesar das peculiaridades de cada sistema legal no mundo, o Brasil segue com o modelo das agências reguladoras, que já se encontram absorvidas no cenário socioeconômico.
Historia y desarrollo de la participación de la mujer en al ámbito público en México
Authors: Corona Nakamura Luis Antonio
Published: July 2021

El artículo tiene como objetivo principal analizar la importancia de la paridad de género en México. Para lograrlo se observa el contexto histórico de la violencia en contra de la mujer en el ámbito público internacional y nacional; además, se estudian sus conceptos fundamentales a efecto de entender qué es el género, la paridad y cuál la importancia de su aplicación. Se aporta al campo de estudio un verdadero panorama respecto de la exclusión de la mujer a efecto de ser conscientes de ello y modificar el trato hacia ella, en pro de su beneficio mediante la elaboración y adecuación de normas acordes a la realidad que viven, pues de no ser así, éstas serían ineficaces.
El derecho de transformación de la obra musical
Authors: García Trelles Fernández Carmen M.
Published: July 2021

El artículo pretende dar una visión interdisciplinar de la problemática del derecho de trasformación de la obra musical original y su posible conceptuación como obra derivada.  A razón del escaso tratamiento del tema que se hace por el Texto Refundido de la Ley de Propiedad Intelectual española, con frecuencia se generan conflictos cuando el autor de una composición original autoriza la incorporación de ésta en otra nueva, ostentando la facultad para que su obra se mantenga totalmente íntegra sin sufrir menoscabo o deformación, una vez que ha consentido su exhibición o explotación. Dentro del contexto jurídico y musicológico se trata de dar un enfoque transversal y establecer criterios objetivos referidos al ámbito musical que, inmersos en la legislación de propiedad intelectual, consigan dar soluciones a las dudas surgidas respecto a la coyuntura actual e intrincada de la delimitación de la transformación de las obras musicales. La hipótesis de partida es la profusión de imprecisiones, la falta de elementos que delimiten con seguridad la variedad de conceptos atribuibles a las obras musicales originales que puedan ser objeto de obra derivada; así como, la procastinación del legislador a la hora de abordar este problema. Se ponen de manifiesto las lagunas existentes y la falta de estudios al respecto en los dos ámbitos, tanto dentro de los estudios musicológicos, como en el tratamiento de la doctrina y la jurisprudencia nacionales que son escasas, también en relación con el derecho comparado.
La importancia de la ciberseguridad y los derechos humanos en el entorno virtual
Authors: Tapia Hernández Erick Francisco , Ruiz Canizales Raúl , Vega Páez Antonio
Published: July 2021

El presente artículo enfatiza la necesidad de una cultura de la ciberseguridad de los usuarios, ante las amenazas y los riesgos a los que se exponen en el entorno virtual, derivados del desconocimiento y las afectaciones que ello ocasiona, mismas que a simple vista parecen inofensivas, pero que repercuten de forma importante en los derechos humanos de las víctimas como la vida, integridad psicológica, intimidad, privacidad o el patrimonio. Por lo anterior, se mencionan algunas de las amenazas más importantes, se destaca que existen delitos que utilizan como medio de comisión el entorno virtual y que hay delitos que surgen dentro de dicho entorno. Así mismo, se señalan algunos derechos humanos originados desde el entorno virtual, y cuyo reconocimiento por parte de los Estados es necesario para así garantizarlos.
El deber de información en un contrato de cesión de contrato
Authors: Abondano Almeida Paula Andrea
Published: July 2021

El deber de información es derivado del principio de la buena fe, aplicable en los contratos y exigible para el contratante poseedor de la información y para el que la desconoce, quien debe evitar estado de ignorancia. Este artículo pretende responder porqué, en un evento de responsabilidad en una cesión de contrato, merece mayor reproche la conducta del cesionario negligente, quien no solicita la información pertinente respecto del contrato cedido, frente a su co-contratante poseedor de dicha información, y que no la entrega intencionalmente. Para determinar el alcance del deber de información a cargo de los contratantes, se hace una revisión de normas jurídicas, doctrina, jurisprudencia y el estudio de los deberes de información, diligencia, lealtad, prohibición de ir en contra de los actos propios, concluyendo que la negligencia y la violación del deber de auto-información no merecen protección jurídica.
Study on Adsorption of Methylene Blue from Aqueous Solution by Biochar Derived from Mimosa Pigra Plant
Authors: Xuan Cuong Nguyen
Published: July 2021

Biochar from mimosa pigra was studied to remove methylene blue (MB) from aqueous solution. The properties of biochars were determined using Fourier Transform Infrared, scanning electron microscope, and Brunauer–Emmett–Teller. The biochar achieved the yield of 24.62 % at 500 oC pyrolysis. The specific surface area of ​​the biochar is 285.53 m2/g, the total pore size is 0.153 cm3/g and the ash content is 2.79%. The optimal dose of removing MB of the biochar is 5 g/L and the optimal pH is 2 - 10. MB removal reached over 80% in the first 30 min, followed by a stable period of 120 to 360 min reaching over 90% of removal. Maximum adsorption capacity reached 20.18 mg/g at 25 oC. MB adsorption data is suitable for kinetic models in order: Avrami > Elovich > PSO > PFO. The adsorption process may comprise physical and chemical adsorption andmultiple stages.
Neutron Cross Section Generation for PWR MOX Fuel Assemblies with SCALE and Serpent
Authors: Thanh Mai Vu , Hartanto Donny , Anh Tran The , Thi Lan Luu , Viet Phu Tran , Viet Ha Pham Nhu
Published: July 2021

In this study, the SCALE/TRITON code (based on deterministic method) and the Serpent 2 code (based on Monte Carlo method) were utilized to prepare the group constants of the pressurized water reactor (PWR) mixed-oxide (MOX) fuel assemblies for transient analyses of PWR MOX fueled cores in normal operation and control rod ejection accident condition with 3D reactor kinetics codes. The PWR MOX fuel assemblies were modeled with TRITON and Serpent, and their infinite neutron multiplication factors (k-inf) versus burnup and respective two-group neutron cross sections were calculated and compared against the available benchmark data obtained with the HELIOS code. The comparative results generally show a good agreement between TRITON and Serpent with HELIOS within 643 pcm for the k-inf values and within 5% for the two-group neutron cross sections. Therefore, it indicates that the TRITON and Serpent models developed herein for the PWR MOX fuel assemblies can be applied to group constant generation to be further used in transient analyses of PWR MOX fueled cores.
EXAFS Debye-Waller Factors of B2-FeAl Alloys
Authors: Hong Nguyen Thi , Duc Nguyen Ba , Khac Hieu Ho
Published: July 2021

This work develops the anharmonic correlated Debye model to study the temperature-dependent extended X-ray absorption fine structure (EXAFS) Debye-Waller factors (DWFs) of B2-FeAl alloys. We derived the analytical expressions of the EXAFS DWF and Debye frequency as functions of temperature. Numerical calculations were performed for Fe1-yAly alloys with various Al concentration (y = 0.35, 0.40, 0.45 and 0.50) in which Fe-Al alloys still maintained B2 structure. The good agreement between our theoretical results with previous data verifies our developed theory. Our calculations show that DWFs of Fe1-yAly alloys increase robustly when temperature and/or Al concentration in Fe1-yAly alloys increase. The increasing of DWF will cause the reduction of the amplitude of EXAFS.
Piper Ribesioides Wall., a Newly Recorded Species for the Flora of Vietnam
Authors: Ngoc Anh Luu Dam , Hung Nguyen Quang , Thanh Nguyen Trung , Truong Do Van
Published: July 2021

We here reported a newly recorded Piper species for the flora of Vietnam, namely Piper ribesioides Wall. (Piperaceae). This species is most morphologically similar to P. politifolium C.DC. by sharing glabrous plants and fruits with a stipe, but it differs from the latter having a monoecious habit (vs. dioecious), stamens 4 (vs. 2), and a cordate leaf base with equal or subequal lobes (vs. oblique with unequal lobes). Descriptions, illustrations, information on ecology, and taxonomic notes of the species is provided.
Isolation and Selection of Purple Non-Sulfur Bacteria for Nutrient Rich Biomass Production from Wastes
Authors: Minh Do Binh , Hai Pham The
Published: July 2021

Purple nonsulfur bacteria (PNSB) are anoxygenic photosynthetic bacteria, which are able to photoheterotrophically grow in the presence of excessive nutrients. Hence, PNSB can convert organic components, in waste waters into nutrient rich biomass. This suggests the feasibility of converting wastes into valuable products. In this research, method for isolation of PNSB was optimized, and subsequently used for the isolation of  PNSB from domestic waste and pond water samples taken in Hanoi. In addition, the effects of carbon and nitrogen sources and types of waste on biomass and nutrients (protein and carotenes) were also investigated. Four PNSB strains were isolated and based on comparative 16S rDNA analysis and their morphological characteristics, they were identified as Rhodobacter (Rb.) capsulatus, Rhodobacter (Rb.) sphaeroides, Rhodobacter (Rb.) sediminis and Rhodopseudomonas (Rp.) palustris. In terms of the effects of carbon and nitrogen sources on their biomass and nutrient production, glucose or maltose and ammonium chloride or urea were found to be more enhancive than starch and peptone, respectively. Among the studied strains, Rb. capsulatus MD1 and Rb. sphaeroides MD3 showed significantly higher biomass production (up to 0.7 g/l) when growing with various carbon and nitrogen sources, in comparison with the other strains. Moreover,  MD1 and MD3 also produced at least four-fold more carotenoid and up to two-fold more protein in tofu processing wastewater compared with the other wastewater. The results suggest potential applications of the PNSB strains for efficient conversions of organic compounds in wastes into biomass of high nutritional values.
Taxillus Thibetensis (Lecomte) Danser (Loranthaceae) a New Record Species For Flora of Vietnam
Authors: Le Chi Toan , Nguyen Van Du , Pham Thu Lan , Le Thi Ngat , Liu Bing
Published: July 2021

Taxillus thibetensis (Lecomte) Danser (Loranthaceae), a species previously known only from China, is newly recorded from Vietnam. A specimen discovered in the rainforest of Lao Cai province, Northern Vietnam was identified as Taxillus thibetensis based on both morphological and molecular data. The Vietnamese individuals of Taxillus thibetensis are closely related to T. thibetensis in China. A detailed description,  illustration and data on distribution, ecology, phenology of Vietnamese Taxillus thibetensis are provided