bluuebunny/crossref_metadata_2025 huggingface dataset:
Development and In Vitro – In Vivo Evaluation of Gastro-retentive Floating Tablets Containing Repaglinide
Authors: P Poornima , K Abbulu , K Mukkanti
Published: August 2020

The present investigation concerns the development of the repaglinide floating matrix tablets, which after oral administration are designed to prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. Among all the formulations F21 containing HPMC K1500 PH PRM, Polyox WSR-303 and Sodium bicarbonate, as gas generating agent was selected as optimized formulation based on physico chemical properties, floating lag time (36 sec) and total floating time (>24 h). From in vitro dissolution studies, the optimized formulation F21 showed drug release of 98.92±5.19% within 24h whereas 95.09±5.01% of the drug was released from the marketed product within 1h. The major mechanism of drug release follows zero order kinetics and non-Fickian transport by coupled diffusion and erosion. In vivo experiments supported the expectations in prolonging the gastric residence time in the fasted state in beagle dogs. The mean gastric residence time for the tested tablets was 270 min±60. This result is encouraging, because a longer gastric residence time is an important condition for higher bioavailability of the drugs included in the prolonged or controlled release dosage forms.
Design and Characterization of Self-Nanoemulsifying Drug Delivery Systems of Rosuvastatin
Authors: D. V. R. N. Bhikshapathi , Keerthi Priya
Published: August 2020

Development of self-emulsifying drug delivery systems (SEDDS) are becoming more popular to improve the oral bioavailability of poorly water-soluble drugs. Rosuvastatin is a lipid-lowering agent used in patients suffering from dyslipidemia. It is a competitive inhibitor of 3-hydroxy 3-methyl glutaryl coenzyme A, which converts mevalonate to cholesterol. Rosuvastatin is a BCS class II (poor solubility) drug; hence, SNEDDS are being formulated to enhance oral bioavailability of the drug. In the present study, rosuvastatin SNEDDS were formulated using different oils, surfactant and co-surfactant. The optimized formulation F9 has composition of Las (PEG-8-Caprylic glycerides), Maisine 35-1 and Tween 20 as oil phase, surfactant and co-surfactant respectively. Composition of SNEDDS was optimized using Pseudo-ternary phase diagram, where the formulations showed increased self-emulsification with increased concentration of surfactants. Formulation F9 was found to be best formulation based on evaluation parameters. The particle size of the optimized SNEDDS formulation was found to be 10.9 nm & Z-Average of 55.6 nm indicating all the particles were in the nanometer range. The zeta potential of the optimized SNEDDS formulation was found to be -11.2 mV, which comply with the requirement of the zeta potential for stability. The developed rosuvastatin SNEDDS have the potential to minimize the variability in absorption and provide rapid onset of action of the drug.
Formulation and Evaluation of Spray Dried Microspheres of Controlled Release Ramipril
Authors: Mutagond Chetankumar , M R Vinod , V M Vijapure , S C Marapur , Patil R G , P N Jorapur , Biradar PN
Published: August 2020

The present study sought to develop and evaluate spray-dried microspheres of chitosan and xanthan gum for controlled release of ramipril, a widely used antihypertensive drug. The prepared microspheres were characterized by particle size analysis, scanning electron microscopic studies, differential scanning calorimetric analysis, Fourier transform infrared spectroscopy analysis, X-ray diffraction studies, drug entrapment efficiency, and in-vitro drug release study. The prepared microspheres were spherical in shape and freely flowing. The size of the microspheres was in the range of 25.7 to 47.4 µm and the drug entrapment efficiency was in the range of 74.68% to 90.44%. TheDSC analysis and X-ray diffraction studies indicated that the drug was uniformly dispersed in amorphous state in the microspheres. The in-vitro drug release indicated that the spray-dried microspheres prepared with chitosan alone were not suitable for controlled released delivery of drug as maximum amount of drug was released within 5 hrs. Whereas microspheres prepared by xanthan gum released small amount of drug within 5 hrs and more amount of drug was controlled released that fit the therapeutic needs. Drug release mechanism followed non-Fickian transport. These suggest the formulation potential of chitosan and xanthan gum for spray-dried microspheres for controlled release of ramipril
Comparitive Antiobesity and Hypolipidemic Activity of Various Extracts of Tecoma gaudichaudi flowers in Monosodium Glutamate Dietary Model in Rats
Authors: G V N Kiranmayi , K Ravishankar , Y Rajendra Prasad , K Surya Tejaswi
Published: August 2020

In the present study, we evaluated the antiobesity and hypolipidemic activities of ethanolic, ethyl acetate and hexane extracts of Tecoma gaudichaudi flowers in rat models.Anti-obesity activity of ethanolic, ethyl acetate and hexane extracts (200 & 400 mg/kg)of Tecoma gaudichaudi flowers were evaluated in rats fed with monosodium glutamate (8 mg/gm) diet. Experimental parameters like body weight, food consumption, locomotor behavior, serum glucose, triglyceride, total cholesterol, high density lipoprotein (HDL), low density lipoprotein (LDL) and very low density lipoprotein (VLDL)  were studied for evaluating the anti-obesity activity of ethanolic extract (EE), ethyl acetate extract (EAE) and hexane extracts (HE) of Tecoma gaudichaudi flowers and orlistat (5mg/kg). There was a significant decrease of total cholesterol, total triglycerides and LDL-C and a significant increase of HDL-C level in hyperlipidemic rats after four-week administration of different extracts of Tecoma gaudichaudi flowers. Treatment with  ethanolic extract (EE), ethyl acetate extract (EAE) and hexane extracts (HE) of Tecoma gaudichaudi exhibited antihyperlipidemic properties which might lead to improvement of serum lipid profile.
Nanotechnology-based Strategies for Ocular Drug Delivery Systems
Authors: Misra Manju , Gupta Aashu , Nayak Kritika
Published: August 2020

This review describes current nanotechnology-based delivery systems for ocular targeting. Amongst all the drug delivery systems existing today, ocular drug delivery is one such delivery approach which is having great endeavours due to the challenges faced by it. Many new as well as exciting treatment options have emerged in this field. The major cause behind development of new treatment alternatives in this field are the limitations raised by the conventional approaches. Currently, researchers are working on development of novel nano techniques to overcome these challenges. The major hurdle is associated with the complicated anatomy and physiology of eye having various static (cornea, conjunctiva, retinal pigmental epithelium) as well as dynamic barriers (blood aqueous barrier, blood retinal barrier) which reduce the overall bioavailability of the drugs. These membranous and fluidic barriers make drug delivery to eye a very challenging task. Hence, current research focuses on developing a system, which is least invasive and able to surpass ocular barriers to maintain sufficient drug levels within the ocular tissue. Nanotechnology based delivery systems play a vital role in this. Many vesicular as well as particulate systems are attempted for the same for anterior as well as posterior segment targeting which can easily overcome limitations of conventional drug delivery systems. Current momentum and ongoing research in this field holds a significant level of promise towards development of improved therapies for treating vision related ailments.
Formulation and In Vivo Evaluation of Mucoadhesive Micro-spheres of Rebamipide, a Mucoprotective Drug for GIT Disorders
Authors: D. V. R. N. Bhikshapathi , P Kanteepan
Published: August 2020

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. The current research study aimed to develop novel gastro-retentive mucoadhesive microspheres of rebamipide using ionotropic gelation technique. Studies of micromeritic properties confirmed that microspheres were free flowing with good packability. The in vitro drug release showed the sustained release of rebamipide up to 99.23 ± 0.13% within 12 h whereas marketed product displayed the drug release of 95.15 ± 0.23% within 1 h. The release mechanism from microspheres followed the zero-order and Korsmeyer-Peppas (R2 = 0.915, 0.969), respectively. The optimized M12 formulation displayed optimum features, such as entrapment efficiency 97%, particle size 61.94 ± 0.11 µm, percentage yield 98%, swelling index 95% and mucoadhesiveness was 97%. FTIR studies revealed no major incompatibility between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M12) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, and Kel  were calculated. The marketed product Cmax (3.15 ± 0.05 ng/mL) was higher than optimized formulation (2.58 ± 0.03 ng/mL). The optimized formulation AUC0-t (15.25 ± 1.14 ng.hr/mL), AUC0-∞ (19.42 ± 1.24 ng.hr/mL) was significantly higher than that of marketed product AUC0-t (10.21 ± 1.26 ng.hr/mL) and AUC0-∞ (13.15 ± 0.05 ng.hr/mL). These results indicate an optimized formulation bioavailability of 2.5-fold greater than marketed product.
Formulation and Evaluation of Lercanidipine Loaded Self-Nanoemulsifying Drug Delivery System
Authors: Rao J. Venkateswara , Reddy T. Rama Mohan
Published: August 2020

In the present study, we sought to improve the solubility and bioavailability of lercanidipine HCl using self-nanoemulsifying drug delivery systems (SNEDDS). The extent of self-emulsification was checked with various oils with suitable surfactants and co-surfactants. The final optimized formulation contained Caproyl 90, Tween 80 and Labrosol as oil, surfactant and co-surfactant respectively. Based on lercanidipine solubility analysis, ternary phase diagrams were constructed for optimizing the system. The formulations were evaluated for FTIR studies, scanning electron microscopy (SEM), solubility, droplet size determination, zeta potential and stability studies. The droplet size was found to be 5.1 nm and Z-Average of 14.6 nm. The zeta potential of the optimized formulation (F16) was found to be -19.7 mV. In vitro drug release from SNEDDS was significantly higher than pure drug. Hence, lercanidipine SNEDDS is an optimum formulation strategy to enhance the solubility and oral bioavailability of this poorly water-soluble drug.
Improvement of Solubility and Dissolution of Rilpivirine Solid Dispersions by Solvent Evaporation Technique and Novel Carriers
Authors: D. V. R. N. Bhikshapathi , M Vishwa
Published: August 2020

Rilpivirine benzonitrile is a pharmaceutical drug used for the treatment of HIV infection it is characterized with poor solubility that limits its absorption and dissolution rate, which delays onset of action. In the present study, immediate release solid dispersion of antiretroviral Rilpivirine was formulated by solvent evaporation technique. Eighteen solid dispersions were prepared with 1:1:1, 1:2:1 and 1:3:1 ratios of drug: carrier: surfactant. There was significant improvement in the rate of drug release from all 18 solid dispersions and the formulation (SE12) comprising Rilpivirine: Kolliwax GMS II: SLS in 1:3:1 by solvent evaporation process has shown enhanced solubility about 30 folds and significant improvement in the rate of drug release. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of Rilpivirine has been converted into an amorphous form from crystalline within the solid dispersion formulation. The obtained results suggested that developed solid dispersion by solvent evaporation method might be an efficacious approach for enhancing the solubility and dissolution rate of Rilpivirine.
Evaluation of the Activity of Leea Indica Merrill in Inflammatory Bowel Disease using Experimental Models
Authors: Shah Samir K , Patel Kruti M , Rathod Nitiraj P
Published: August 2020

Leea indica is traditionally well-known for its versatile uses. The present study was carried out to evaluate the protective effect of methanolic extract of Leea Indica on DNBS (2, 4 dinitrobenzene sulfonic acid) induced inflammatory bowel disease in rats. Adult Wistar rats of either sex weighing 150-200 g were selected. Thirty animals were randomly divided into 5 groups each consisting of 6 animals. The period of experiment was of 12 days. Animals of Group I, Group-III, Group-IV & Group-V were given water, methanolic extract of Leea indica (200mg/kg & 400mg/kg) and sulfasalazine (360 mg/kg body weight) respectively once a day orally for 1st to 7th days. On 8th day of the study, DNBS solution (30 mg dissolved in 0.25 ml of 50% ethanol) was administered intrarectally to induce IBD in animals of Group-II to V, on same day & no treatment was given. Then from 9th to 11th day, they were again given treatment. On 12th day, blood was collected from all animals and sacrificed and dissected to isolate colon. Finally, macroscopic, microscopic and biochemical studies were carried out. At all the two doses, the methanolic extract of Leea Indica showed significant anti-inflammatory activity in experimental models. Results obtained in this study substantiate the anti-inflammatory effect of methanolic extract of Leea Indica roots.
Synthesis and Evaluation of 2, 3, 4, 6-Tetra-Substituted-2, 3-Dihydropyridine Derivatives as Novel Antimicrobial Agents
Authors: M Bhagavaan Raju , A A. Ramesh , Rao A Raghuram
Published: August 2020

The present study has been carried out to synthesize and screen certain heterocyclic antimicrobial compounds with clues from the biologically potent activities of heterocyclic compounds containing pyridine. With a view to synthesize some biologically active compounds, it has been felt worthwhile to study the synthesis of 2, 3, 4, 6-tetra-substituted-2,3-dihydro pyridine derivatives (7a-t). They were synthesized by the condensation of respective 2-amino-2,3-dihydropyridines with different aromatic aldehydes. 7a-t were purified and characterized by physical and spectral methods (IR, 1HNMR & MS). All the compounds were evaluated for their antimicrobial activity by the agar diffusion method against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Proteus vulgaris, Candida albicans and Saccharomyces cerevisiae. All the compounds exhibited mild to moderate antibacterial & antifungal activity. Among these compounds, compound 7h (R= Cl, R1=Cl) showing greater inhibitory activity against all tested organisms employed with zones inhibition of 20 to 15 mm at a concentration of 150 μ g/mL. Compounds 7g, 7c, 7i and 7j have been found as the next in the order of its antimicrobial potency. These compounds have the potential as novel antimicrobial agents.
Formulation, Optimization and Evaluation of Rasagiline Mouth Dissolving Films
Authors: Rao Pingali Srinivasa , Reddy T Rama Mohan
Published: August 2020

The oral route is the most preferred route, though preoral administration of drug has disadvantage like hepatic first pass metabolism and enzymatic degradation within the GI tract. Trans-mucosal routes of drug delivery offer distinct advantage over preoral administration. The aim of present investigation was to formulate the fast-dissolving oral films (FDOF) of rasagiline, an anti-Parkinson drug. In the present study, rasagiline fast dissolving films were formulated by solvent-casting method containing HPMC 5cps, 15 cps and 50 cps as polymers and PEG 400 as plasticizer, Crospovidone and SSG as superdisintigrating agents. All films prepared were smooth and elegant in appearance and showed no visible cracks, were even in weight, thickness and drug content. Formulation F16 is considered as the optimized formulation as it showed the faster disintegration time i.e., 8±0.18 sec, good percentage elongation (9.4%), good folding endurance (120±4), and the in vitro drug release is 99.39±5.28% within 9 min. It can be concluded that from the study that the mouth dissolving film can be potential novel drug dosage for treatment of Parkinson’s disease.
Formulation and Evaluation of Sustained Release Dosage Forms of Norfloxacin
Authors: Suja C , C Sismy
Published: August 2020

The goal of this study was to formulate and evaluate norfloxacin sustained release tablets. Norfloxacin sustained release tablets were prepared by wet granulation method using two polymers such as HPMC K 100 M (hydrophilic polymer) and guar gum (natural polymer) and with three polymer ratios (0.5, 1.0 and 1.5). The prepared granules were evaluated to preformulation studies such as angle of repose, bulk density, tapped density, bulkiness, compressibility index and Hauser’s ratio. All the parameters shows that the granules having good flow properties. Then the formulated tablets were taken to evaluation studies such as hardness, weight variation, friability, drug content and thickness. All the parameters were within the acceptable limits. IR spectral analysis showed that there was no interaction between the drug and polymers. The in vitro release study was performed in phosphate buffer pH 7.4 at 293 nm. The in vitro release study showed that if the polymer ratio is increased, then the release of the drug is prolonged. HPMC K 100M shows a prolonged release when compared to guar gum.
Formulation Design and Optimization of Repaglinide Solid Dispersions by Central Composite Design
Authors: D. V. R. N. Bhikshapathi , I Srinivas
Published: August 2020

Repaglinide is a pharmaceutical drug used for the treatment of type II diabetes mellitus, it is characterized with poor solubility which limits its absorption and dissolution rate and delays onset of action. In the present study, immediate release solid dispersion of repaglinide was formulated by solvent evaporation technique. Repaglinide solid dispersions were prepared using PEG 8000, Pluronic F 127 and Gelucire 44/14 by solvent evaporation method. A 3-factor, 3-level central composite design employed to study the effect of each independent variable on dependent variables. FTIR studies revealed that no drug excipient interaction takes place. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of repaglinide has been converted into an amorphous form from crystalline within the solid dispersion formulation. The correlation coefficient showed that the release profile followed Higuchi model anomalous behavior and hence release mechanism was indicative of diffusion. The obtained results suggested that developed solid dispersion by solvent evaporation method might be an efficacious approach for enhancing the solubility and dissolution rate of repaglinide.
Endocrine and Therapeutic Basis of Diabetes Mellitus Therapy
Authors: Kulshreshtha Mayank , Srivastava Pragati , Panjwani Dharamveer
Published: August 2020

This review article describes the role of hormones, microvascular complications, pharmacological and non-pharmacological treatments and precautions of diabetes therapy. Diabetes mellitus (DM) is a chronic, lifelong condition that affects ability to use the energy found in food. According to World Health Organization (WHO), it is estimated 422 million adults are suffered with DM up to latest 2016 data.  It occurs throughout the world but is more common in the more developed countries. Increase in prevalence is occurring in low- and middle-income countries including in Asia and Africa, where most patients will probably be found by 2030. The WHO estimates that diabetes resulted in 1.5 million deaths in 2012, making it the 8th leading cause of death. We summarized the published scientific data and new development in the field of diabetes with a search of PubMed, Google scholar, med know and other online resources.  Various hormones play an important role in which insulin has a more importance in DM. Pharmacological treatment included various side effects while herbal drugs are found to be safe. Diet and exercise are the excellent key points to cure the disease. Avoid high sugar diet and various foods whose sugar levels are high should be avoided at the age 40.  Overall, better knowledge, balanced life style, and daily exercise are the excellent treatment of diabetes and effective glucose control.
Biopharmaceutical and Pharmacodynamic Characteri-stics of Telmisartan Oral Disintegrating Films
Authors: Kaza Rajesh , M Sujatha Kumari , M Kishore Babu , A Avinash , R Nagaraju
Published: August 2020

This research work was aimed to develop the telmisartan fast dissolving films. Fast dissolving films allow rapid drug dissolution in the oral cavity and thereby bypass the first pass metabolism. Solid dispersions of telmisartan using natural polymers such as hupu gum (HG), guar gum (GG) and xanthan gum (XG) were prepared by kneading technique and the optimized solid dispersion was exploited in the development of rapidly dissolving film. Telmisartan films were prepared by solvent casting method using different grades of HPMC (E5, 50 cps and K4M). Six formulations (FT1-FT6) of telmisartan films were prepared and evaluated for their physical characteristics such as thickness, tensile strength, percentage elongation, weight variation, folding endurance, drug content uniformity and surface pH and gave satisfactory results. The compatibility of the drug in the formulation was confirmed by FTIR and DSC studies. The formulations were subjected to disintegration, in vitro drug release and pharmacodynamic studies on spontaneous hypertensive rats (SHR). Amongst the formulations of FT1-FT6, FT6 was found as best formulation which contains HPMC E5 and telmisartan solid dispersion with guar gum at weight ratio of 1:2 and showed excellent film forming characteristics such as disintegration time at 42 sec and percentage drug release 97.98% within 10 minutes. The optimized film formulation (FT6) showed excellent stability over 45 days when stored at 40°C/60% RH. The pharmacodynamic study in SHR proved that fast dissolving films of telmisartan produced a faster onset of action.
Role of Genetic Variations in the CYP2C9 Gene in Determining the Optimal Dose of Warfarin in a Group of Syrian Patients
Authors: Shayah Kamar , Ghrewati Abduljalil , Mohammad Yaser Abajy , Hadid Ibrahim
Published: August 2020

Genetic variations in drug metabolizing hepatic CYP2C9 gene determine the optimal dose for many drugs including anticoagulants such as warfarin.  Here we sought to detect the frequency distribution of genetic variations of CYP2C9 gene and to determine its potential role in the control of warfarin dose in Syrian patients. The study included 125 patients with high risk of thrombosis of adults who visited the Heart Disease & Surgery Hospital (HDSH) and Aleppo University Hospital (AUH) and treated with warfarin as oral anticoagulant therapy, and the dose-corrected by the international normalized ratio (INR) at least three months ago. Genomic DNA was extracted from blood samples, and genotype analysis for CYP2C9*2 and  CYP2C9*3 variant alleles was done by polymerase chain reaction-restriction fragment length polymorphism assay (PCR-RFLP). Data were analyzed using SPSS version 20. The results obtained in this study suggest that Genotype frequency distribution of CYP2C9*2 and CYP2C9*3 variant alleles was found to be different from other populations and has significant effect on warfarin dose requirement (p<0.05). It is concluded that there is a need to include CYP2C9 genetic variations detection tests in the warfarin dosing algorithm, as this has an important role in reducing serious hemorrhagic complications, especially in patients with the CYP2C9*2/*2 and CYP2C9*3/*3 homozygous mutant genotypes.
Recent Developments and Novel Drug Delivery Strategies for the Treatment of Tuberculosis
Authors: Brhane Yonas , Gabriel Tesfaye , Adane Tigist , Negash Yemisrach , Mulugeta Henok , Ayele Mulugeta
Published: August 2020

Tuberculosis (TB) is a contagious infectious illness caused by species having a place with the Mycobacterium tuberculosis complex. The clinical management of tuberculosis still remains a difficult task. Treatment of TB with anti-tubercular drugs becomes the only option available. Hence, the goals of treatment are ensure cure without relapse, prevent death, impede transmission, and prevent emergence of drug resistant strains. This review describes the latest developments and innovative drug delivery strategies for treatment of TB in order to improve the therapeutic efficacy and reduce toxic effect of anti-tubercular agents and enhance patient compliance with concomitant decrease in drug interaction. Among different novel drug delivery systems Niosomes, Liposomes, Dendrimers, Cyclodextrins, Microencapsulation, Alginates and Hydrogels have been described as new drug delivery strategies of anti-tubercular agents.
Antidiabetic Activity of Aqueous and Methanolic Extract of Dried Pericarp (Shell) of Juglans Regia L.
Authors: Agrawal Krishn Kumar , Agrawal Nitin , Gupta Jyoti , Gupta Tripanshu
Published: August 2020

The aim of the present study was to investigate the in-vitro anti-diabetic activity of aqueous and methanolic extract of dried pericarp (Shell) of Juglans regia L. The preliminary qualitative phytochemical screening was also undertaken to reveal the presence of Phyto-constituents in the extracts. Phytochemical screening of aqueous extract shows the presence of polyphenols, flavanoids, cardiac glycosides, carbohydrates and reducing sugar while methanolic extract show the presence of alkaloids, polyphenols, cardiac glycosides, carbohydrates and reducing sugar. Pharmacological evaluation of Juglans regia was performed by α-amylase inhibition assay method. Percentage inhibition of α amylase at dose of 50mg/mL, 100 mg/mL and 150 mg/mL of aqueous and methanolic extract was found to be 33.33, 66.67, 93.34 and 32.27, 59.64, 90.74 respectively. Among the extracts the aqueous extract showed highest activity as compared to control and methanolic extract.
Development and Validation of Stability-indicating Reverse Phase HPLC Assay for Tramadol in Bulk and Tablet Formulations
Authors: Nerkar Pankaj Padmakar , Badjuar Vaishali , Ige Pradyum , Mahajan Hitendra , Ansari Sameer
Published: August 2020

This manuscript describes the development and validation of a simple, isocratic, and accurate reversed-phase HPLC method for the assay of tramadol in bulk powder form and tablet formulations. The chromato-graphic separation was achieved on an Qualisil BDS C18 (250 mm x 4.6mm, 5μm) column using acetonitrile: methanol: phosphate buffer pH 3.4 adjusted with orthophosphoric acid: (20:10:70, v/v) as a mobile phase, at a flow rate of 1 mL/min and detection at 271 nm. The linear range for tramadol were 2.0 to 10 μg/mL was obtained with correlation coefficients ≥ 0.999. The retention time was found to be 4.47 min for tramadol that was subjected to stress conditions, such as hydrolysis, oxidation, photolysis and thermal degradation, and the stressed samples were analyzed using the above methodology. The method was validated for the precision, accuracy, linearity and robustness. The developed stability-indicating method for tramadol was validated as per ICH guidelines.
Role of Temperature on the Size of Niosomes Formed by the Ether Injection Method
Authors: Agarwal Shweta , Tempta Pallavi , Kaushik Poonam , Kaushik Kusum
Published: August 2020

Niosomes are lamellar vesicles formed by self-association of non-ionic surfactants and cholesterol having good compatibility with the biological system and low toxicity. Their ability to encapsulate both hydrophilic and hydrophobic drugs, their potential use in protection of drugs, controlled release and targeted drug delivery makes them a promising drug delivery system. Various factors like nature of drug, amount and type of surfactant used, method of preparation, amount and charge of cholesterol used, type and volume of hydrating medium, speed of agitation, time and temperature of hydration medium affect the type and characteristics of niosomes formed. Therefore, a study was conducted to determine the effect of hydration temperature on the size of niosomes formed by ether injection method. Aceclofenac was used as the model drug as it is lipophilic and shows good encapsulation in niosomes. Span 20 was used as the non-ionic surfactant. The study was conducted at three temperatures of hydration and all the other variables were kept constant. The niosomes formed at the different hydration temperatures were evaluated for shape and size by optical microscopy and mean vesicle size determined at each temperature. The data obtained for size was statistically analysed by the software Graphpad prism version 7 using ordinary one-way ANOVA. The p value obtained (at 95% confidence interval: p< 0.05) was used to determine significant difference between the mean vesicle sizes at the three temperatures. The study showed that hydration temperature played a major role in the size of niosomes formed by ether injection method.
Antifungal Activity of Peppermint Oil against Candida Albicans Isolated from Urine Samples
Authors: Berakda Noura , Radwan Abdulkarim
Published: August 2020

Fungal infections with candida species are an important cause of morbidity and mortality. Situation is further worsened by increasing resistance to antifungal drugs. In this study, we sought to investigate the antifungal activity of peppermint oil against candida albicans of urinary tract candidiasis in females from Syria. An in vitro study was carried out using the following Candida albicans strains involved in urinary tract candidiasis using well diffusion (WD) testing: Candida albicans (ATCC 90028) and 15 strains were compiled from Aleppo university Hospital. It was taken from women having urinary tract candidiasis. The antifungal activity of peppermint oil was determined in the form of inhibition zone using antifungal assay agar WD testing. In all experiments, the obtained results indicated that peppermint oil has inhibitory effects on Candida albicans (ATCC 90028) and some 15 strains. This study showed that peppermint oil was active against the tested Candida albicans strains. Peppermint oil was more effective against Candida albicans compared to fluconazole. Peppermint oil may have potential for use in the development of clinically useful antifungal preparations. Therefore, peppermint oil might be highly effective in the natural prevention treatment of urinary tract candidiasis.
Cashew Nut Starch as Natural Excipient for Improved Bioavailability of Drugs
Authors: Kushwaha Anjali
Published: August 2020

The bioavailability of drug is affected by various excipients present in the formulation. In case of tablets, the role of binders is very important for release of drug and bioavailability. In the present study, starch was extracted from the cashew nuts and used as binding agentat a concentration of 2% w/v, 4% w/v, 6% w/v and 8% w/v. The tablets were formulated by using famotidine drug and they were further evaluated for various parameters like weight variation, hardness, friability, disintegration time, in vitro and in vivo drug release. The results show that all parameters were found within the given Indian Pharmacopeial limits. The in vitro release studies were performed in 0.1 N HCl using dialysis methods. This shows that tablets containing 2 % of cashew starch showed maximum drug release (89%) then other formulations. Then optimized formulation was further used for in vivo study and results shows better bioavailability as compared to marketed products.
Formulation and Evaluation of Metoprolol Tartrate Sustained Release Matrix Tablets
Authors: Y Shravan Kumar , G Shireesha , S Harika
Published: August 2020

The objective of the present work was to develop sustained release matrix tablets of Metoprolol tartrate using different polymers viz. Guar gum, Xanthan gum, Kondagogu gum and HPMC K100M. The release rates were modulated by combination of two different rates controlling material and triple mixture of two different rate controlling materials. After evaluation of physical properties of tablet, the in-vitro release study was performed in phosphate buffer pH 6.8 up to 12 hrs. Dissolution data was analyzed for release kinetics. It was observed that matrix tablets contained polymer Xanthan gum was successfully sustained the release of drug up to 12 hrs. Among all the formulations, F6 which contains 45 % of Xanthan gum, release of drug which follows zero order kinetics via, swelling, diffusion and the release profile of formulation F6 was compared with marketed product. The FTIR study revealed that there was no chemical interaction between drug and excipient.
Evaluation of Carboxymethylated Plectranthus edulis Starch as Suspending Agent in Metronidazole Benzoate Suspension Formulation
Authors: Brhane Yonas
Published: August 2020

Carboxymethylated Plectranthus edulis, Vatke (P. edulis) [fam., Lamiaceae] starch was evaluated as a suspending agent in metronidazole benzoate suspensions in comparison with sodium carboxymethyl cellulose (NaCMC) at concentration range of 1-4% (w/v). The resulting suspensions were evaluated for their sedimentation volume (%), degree of flocculation, rheology, redispersibility, and dissolution rate. Stability studies were performed for 3 months. The apparent viscosities of the formulations prepared with carboxymethylated P. edulis starch at reaction condition E (CMPS-E) was significantly lower than that of NaCMC (p < 0.05). The flowability of the suspensions, at all concentration levels of the suspending agents, were in the order of CMPS-E > NaCMC. AT 1% concentrations, carboxymethylated P. edulis starch (76 ± 1.5%) provided significantly higher (p < 0.05) sedimentation volume than NaCMC (40 ± 1.5%). At 3% and 4%, both gave comparable sedimentation volume (100%). Potassium dihydrogen phosphate (KH2PO4) employed as a flocculating agent significantly increased (p < 0.05) the sedimentation volume of the suspensions prepared with carboxy-methylated P.edulis starch and NaCMC. The redispersibilities of CMPS-E was better than those of NaCMC. All suspensions showed a release of greater than 85% of drug within 1 h. The results of stability studies showed that all suspension formulations were stable. From the foregoing, it can be concluded that carboxymethylated P. edulis starch could be used as an alternative suspending agent.
Influence of Solid Lipid Nanoparticles on Pharmaco-dynamic Activity of Poorly Oral Bioavailable Drugs
Authors: Dudhipala Narendar
Published: August 2020

In the recent scenario, lipid nanoparticles gain much attention on the oral absorption of drugs to enhance therapeutic effectiveness after oral administration. Pharmacodynamic activity of drug mainly describes the pharmacological and therapeutic activity of drug to the biological system. Lipid nanoparticles especially solid lipid nanoparticles are made of physiological inert lipid molecules and promotes the lymphatic transport. Abundant literature is available on the effect of lipid nanoparticles and other colloidal carrier systems on the pharmacokinetic parameters of poorly bioavailable drugs, to improve their oral absorption and also respective mechanisms for the improved oral bioavailability. However, little literature is reported on the pharmacodynamic activity and the effect of dose on the pharmacodynamic activity. It is of paramount importance to assess the influence of lipid nanoparticles on pharmacotherapeutic actions of specific drug classes. Therefore, current review is mainly focused on the role of solid lipid nanoparticles on the pharmacodynamic action and advantages of the developed delivery systems with respect to pharmacodynamic activity.
Nanosuspension Technology for Delivery of Poorly Soluble Drugs and Its Applications: A Review
Authors: Godge Ganesh R , Garje Mahesh A , Dode Aniket B , Tarkase Kailas N
Published: August 2020

Now a days, many drug candidates are water insoluble hence they show a limited drug release and poor bioavailability. It is difficult to formulate these drugs by conventional dosage form. Nanosuspension technology is a promising approach to solve the problems of poorly soluble and less bioavailable drugs. Nanosuspension is a very finely colloidal, biphasic, and uniformly dispersed solid drug particles in a suitable aqueous vehicle, having a particle size below 1 μm stabilized by suitable surface active agents and polymers. Nanosuspensions are prepared by various suitable techniques for drug delivery applications. Due to reduced particle size at the nano scale, surface area, saturation solubility, dissolution velocity and bioavailability of BCS class II and class IV drugs are increased sufficiently. Nanosuspension is suitable to administration via various routes such as oral, intravenous, topical, pulmonary and ocular delivery systems. Nanosuspension can be also used for targeting purpose in various diseases such as cancer, HIV and production of sustained and extended release products by choosing suitable polymers. Production and manufacturing are not complicated, easy to scale up. Top down and bottom technologies are used for the preparation of nanosuspensions. It includes methods such as high-pressure homogenization, by milling media method, precipitation method, probe sonication, dry-co-grinding, supercritical fluid method, and lipid emulsion method. Formulation consists of stabilizers, surfactant, and solvents. Nanosuspension can be stored in the form of dry powder using spray drying, freeze drying techniques. This review describes the advantages, various methods of preparation, formulation consideration and characterization of nanosuspension.
Mesoporous Silica-Based Nanoparticles in Pharmaceutical Sciences: A Mini-Review
Authors: Bhattacharya Sankha , Prajapati Bhupendra G
Published: August 2020

The sustained and comprehensive need in the field of materials having immense thermal, chemical, and mechanical stability lead to the evolution of mesoporous silica nanoparticles (MSNs). Due to higher surface area and ridged tuneable particular size, silica-based mesoporous (2-50nm) drug delivery system recently becomes a prime orb for loading different guest molecules such as peptides, proteins, anticancer drugs. The most common type of mesoporous nanoparticles is MCM-41 and SBA-15. MSMs has a wide range of applications in drug delivery, imaging, and catalysis. It was in the 1970’s, when the first patent was field related to MSMs, however during 1990, the full-fledged research started for MSMs. During that era, Mobil Corporation Laboratories, Japan started synthesizing of MSMs. Yet, the University of California also pioneered in MSMs synthesis, as they claimed to prepare 4.6-30 nm MSMs with a hexagonal array of pores; they further named it as SBA-15. MSMs has huge application in drug delivery system. Because of its larger surface area of the pores, the cytotoxin or drug can be filed within the pores like a Trojan Horse. Within the intercellular environment, by the endocytosis process, the small particles will be engulfed by biological cell membranes depending on what ligands attached within MSMs i.e., loaded RNA, loaded DNA, surface protein, PEG, and monoclonal antibody. Surprisingly, advanced research on MSMs concluded that cancerous cells have the tendencies to take MCM-41 than the healthy cells of the host; giving scientists a new hope that MCM-41 will one day be used commercially to treat a certain type of cancers. Modern research also shows that for the poorly water-soluble drug, SBA-15, TUD-1, HMM-33 and FSM-16 of MSMs has tremendous potential to improve in-vitro dissolution profiling i.e., upon loading of itraconazole (a poorly water-soluble drug) within SBA-15, it can able to stimulate GI fluid and facilitate transepithelial intestinal transport which ultimately results in higher drug absorption. In this mini-review, we attempted to discuss MSNs synthesis methods, morphology, preparations, mechanisms and recent research in the MSNs Drug delivery system. Thus, we concluded that more in vivo biocompatibility studies, biodistribution studies, toxicity studies, and clinical research is the fundamental prerequisite for further advancement in mesoporous silica-based nanoparticles (MSNs).
Human and machine validation of 14 databases of dynamic facial expressions
Authors: Krumhuber Eva G. , Küster Dennis , Namba Shushi , Skora Lina
Published: August 2020

With a shift in interest toward dynamic expressions, numerous corpora of dynamic facial stimuli have been developed over the past two decades. The present research aimed to test existing sets of dynamic facial expressions (published between 2000 and 2015) in a cross-corpus validation effort. For this, 14 dynamic databases were selected that featured facial expressions of the basic six emotions (anger, disgust, fear, happiness, sadness, surprise) in posed or spontaneous form. In Study 1, a subset of stimuli from each database (N= 162) were presented to human observers and machine analysis, yielding considerable variance in emotion recognition performance across the databases. Classification accuracy further varied with perceived intensity and naturalness of the displays, with posed expressions being judged more accurately and as intense, but less natural compared to spontaneous ones. Study 2 aimed for a full validation of the 14 databases by subjecting the entire stimulus set (N= 3812) to machine analysis. A FACS-based Action Unit (AU) analysis revealed that facial AU configurations were more prototypical in posed than spontaneous expressions. The prototypicality of an expression in turn predicted emotion classification accuracy, with higher performance observed for more prototypical facial behavior. Furthermore, technical features of each database (i.e., duration, face box size, head rotation, and motion) had a significant impact on recognition accuracy. Together, the findings suggest that existing databases vary in their ability to signal specific emotions, thereby facing a trade-off between realism and ecological validity on the one end, and expression uniformity and comparability on the other.
Magnetic-field-assisted synthesis of anisotropic iron oxide particles: Effect of pH
Authors: Shibaev Andrey V , Shvets Petr V , Kessel Darya E , Kamyshinsky Roman A , Orekhov Anton S , Abramchuk Sergey S , Khokhlov Alexei R , Philippova Olga E
Published: August 2020

The synthesis of magnetite (Fe3O4) nanorods using reverse co-precipitation of Fe3+ and Fe2+ ions in the presence of a static magnetic field is reported in this work. The phase composition and crystal structure of the synthesized material were investigated using electron diffraction, Raman spectroscopy, and transmission electron microscopy. It was shown that the morphology of the reaction product strongly depends on the amount of OH− ions in the reaction mixture, varying from Fe3O4 nanorods to spherical Fe3O4 nanoparticles. Fe3O4 nanorods were examined using high-resolution transmission electron microscopy proving that they are single-crystalline and do not have any preferred crystallographic orientation along the axis of the rods. According to the data obtained a growth mechanism was proposed for the rods that consists of the dipole–dipole interaction between their building blocks (small hexagonal faceted magnetite nanocrystals), which are formed during the first step of the reaction. The study suggests a facile, green and controllable method for synthesizing anisotropic magnetic nanoparticles in the absence of stabilizers, which is important for further modification of their surfaces and/or incorporation of the nanoparticles into different media.
Effect on antimicrobial activity of antifungal agents-silver nanoparticles combined treatments
Authors: Pérez Arriola Yarithza , Vázquez Muñoz Roberto , Bogdanchikova Nina , Huerta Saquero Alejandro
Published: August 2020

Infectious diseases are a global public health problem; they are among the leading causes of death worldwide and consume a significant amount of resources. Fungi are the most common pathogens in humans and animals. Fungal infections incidence has increased more than 200%. Currently, antifungal agents are used for combating fungal infections, but there are many problems associated with their use, such as the emergence of resistant organisms, as well as the complexity related to the development of new antibiotics. In that sense, silver nanoparticles have proven to be an alternative solution to fight fungal infections due their capacity to inhibit fungal growth. In this work, we studied the antimicrobial activity of silver nanoparticles (AgNPs), antifungal agents (Amphotericin B and Fluconazole) and combinations of both, AgNPs-antifungals over the pathogenic dimorphic yeast Candida albicans. The antimicrobial tests were performed according to the CLSI ́s M27-A3 protocols. Combined AgNPs-antifungal treatments showed a different effect on antimicrobial activity. We found a synergistic effect of specific combined treatment, whereas antagonistic effect was observed with other combination.
Tracking the Quality of Addiction Treatment Over Time and Across States: Using the Federal Government’s “Signs” of Higher Quality
Authors: Mark Tami L. , Dowd William N. , Council Carol L.
Published: August 2020

The objective of this study was to track trends in the signs of higher-quality addiction treatment as defined by the National Institute on Drug Abuse, the National Institute on Alcohol Abuse and Addiction, and the Substance Abuse and Mental Health Services Administration. We analyzed the National Survey of Substance Abuse Treatment Services from 2007 through 2017 to determine the percent of facilities having the characteristics of higher quality. We analyzed the percent by state and over time.

• We found improvements between 2007 and 2017 on most measures, but performance on several measures remained low.

• Most programs reported providing evidence-based behavioral therapies.

• Half or fewer facilities offered medications for opioid use disorder; mental health assessments; testing for hepatitis C, HIV, and sexually transmitted diseases; self-help groups; employment assistance; and transportation assistance.

• There was significant state-level variation across the measures.
Return on Investment Analysis of Private Sector Facilitation Funds for Rwandan Agribusinesses
Authors: McGill Karis , Turner Eleanor
Published: August 2020

This study analyzes the return on investment for an agribusiness facilitation fund implemented in Rwanda. Combining project monitoring data with supplementary surveys and interviews of recipient agribusinesses, we find a positive return on investment in terms of farmer income generated per dollar spent by the US government. To determine the commercial viability of the investments, we estimate the payback period and find the median time it will take a firm to recoup the entire investment through profits is 3.7 years. We estimate the net present value of the entire fund portfolio to be $12.5 million. These estimates rely on conservative assumptions and likely underrepresent the profitability of the investments. Given the positive returns and commercial viability of the agribusinesses, we examine the fund’s role as a first step to “graduate” firms toward investment readiness. Although three firms did access equity investment, we find that the majority of the businesses in the portfolio do not meet investor requirements for deal size and management capacity and are more appropriately financed by commercial lenders. We conclude with recommendations for the implementation and measurement of similar funds.