bluuebunny/crossref_metadata_2025 huggingface dataset:
Optimization of Gastroretentive Delayed Release Drug Delivery using Design of Experiment Approach
Authors: PATEL DASHARATH MULJIBHAI , Patel Preeti B.
Published: July 2024

Gastroretentive drug delivery with delayed release of propranolol hydrochloride for chronotherapy of hypertension was formulated. The drug delivery in the form of compression coated tablet was developed using Indian Pharmacopoeia grade hydroxypropyl methyl cellulose K100M and carbopol 934P as matrix forming polymers and polyvinyl pyrrolidone K30 as channelling agent. Drug-excipient compatibility study revealed no interaction between drug and the excipients. Prepared tablets were evaluated for floating lag time, total floating time and lag time before drug release. Drug delivery was optimized by using 32 full factorial design. The concentrations of matrix forming polymers were selected as independent variables whereas lag time before drug release, drug release at 8, 12 and 20 h were selected as response variables. Tablets of optimized batch F5 containing 25% hydroxypropyl methyl cellulose K100M and 9% polyvinyl pyrrolidone K30 exhibited the maximum similarity with predicted drug release profile for an ideal formulation with similarity factor of 80.69. The lag time before drug release (5 h), drug release at 8 h (27.39%), 12 h (49.48%) and 20 h (86.69%) of optimized batch were close to predicted drug release profile for an ideal formulation. Drug release from optimized batch followed zero order kinetics with super case II transport. Optimized formulation was stable for 1 mo at environmental conditions of 40±2°C temperature and 75±5% relative humidity. Prepared drug delivery of propranolol hydrochloride may be useful to provide sustained drug release for 24 h at the site of absorption for chronotherapy of hypertension.
EFFECT OF DAIDZEIN, NARINGENIN AND ICARIIN ON CISPLATIN-INDUCED NEPHROTOXICITY IN EXPERIMENTAL MICE
Authors: Jadon Arvind Singh , Sharma Manoj
Published: July 2024

Cisplatin is one of the most widely used and most potent chemotherapy drugs. However, side effects in normal tissues and organs, notably nephrotoxicity in the kidneys, limit the use of cisplatin and related platinum-based therapeutics. Renoprotective approaches are being discovered, but the protective effects are mostly partial, suggesting the need for combinatorial strategies. The cytoprotective efficacy of Daidzein, Naringenin, and Icariin against Cisplatin-induced nephrotoxicity in female Swiss mice was examined in this work. All animals were divided into two sets i.e. pre-cisplatin (BA) and post-cisplatin (AA) administration and treated with Daidzein, Naringenin, and Icariin. Nephrotoxicity was assessed by body weight and biochemical parameters i.e. Serum Creatinine, Urea, uric acid During this study body weight of the experimental animal changed by 5% maximum observed in both sets. Biochemical tests of kidney showed that pre-treated and post-treated with Daidzein groups were most effective against nephrotoxicity. These findings are also confirmed by histopathology. The study has proven that pre-treatment with flavonoids was found more effective against cisplatin-induced cytotoxicity as compared to post-treatment.
Hepatoprotective activity of different leaves extracts of Convolvulus pluricaulis against CCl4 induced liver damage
Authors: Tamboli Ashpak M. , Wadkar Kiran A.
Published: July 2024

The study was designed to assess the hepatoprotective activity of various extracts (Pet. ether, chloroform, ethyl acetate, ethanol & aqueous) of leaves of Convolvulus pluricaulis in carbon tetrachloride (CCl4)-induced hepatotoxicity in rats. Amongst all the extracts, ethyl acetate extract (200 and 400 mg/kg) significantly normalized the CCl4-elevated levels of serum SGPT, SGOT, ALP and TB and GSH, CAT and considerably reduced the serum levels of MDA compared to CCl4 group (**p<0.01) and also decreased the histological injuries (inflammation and fatty degeneration) due to CCl4. The results revealed that the Convolvulus pluricaulis extracts could provide considerable protection against CCl4 hepatotoxicity in rats that may be related to its antioxidant properties. The protective nature of the Convolvulus pluricaulis leaves extract might be due to enhanced scavenging antioxidant properties in the presence of unique secondary metabolites such as glycosides, alkaloids and flavonoids. These compounds are known to have antioxidant properties and have applications in treatment of liver diseases.
Designing of multi-epitope based vaccine against SARS COV-2, using reverse vaccinology approach
Authors: Ganguly Rik , Ngoruh Angneh , Ingty Prosperwell , Bhattacharjee Atanu
Published: July 2024

SARS Coronavirus-2 (SARS-CoV-2) pandemic has shown a devastating effect worldwide. More than 1.62 million people have lost their life due to this dangerous virus and it has become one of the major concerns worldwide. It has become an emerging global issue concerning different scientific communities. Here an attempt has been made to develop a vaccine against the SARS-CoV-2 virus using epitope-based subunit vaccines and reverse vaccinology and immunoinformatics methods. With the help of computational experimentations and multi-epitope-based drug designing studies, we have successfully designed 5 different vaccine structures which were further analyzed for insilco toxicity as well as molecular interaction studies.  Significant interacting candidates were further subjected to insilco immuno simulation for the data point of about a year time. This work could provide new hope for development of effective vaccine in the face of global threat arising from the emerging virus.
Evaluation of total phenolic content and antioxidant activities of three species of marine algae from Thirumullavaram, Kerala, Southwest coast of India
Authors: Sharma Gayathri , John Jose
Published: July 2024

Antioxidants from natural sources are gaining demand in various industries since they are the safest alternatives to synthetic antioxidants. Marine macroalgae are rich sources of antioxidants and polyphenols. In the present study, in vitro antioxidant activities of the acetone extract, aqueous extract, and acetone: water extracts (7:3 v/v) of three macroalgae (Ulva fasciata, Gracilaria corticata, and Hypnea valentiae) collected from Thirumullavaram, Kerala, Southwestern coast of India were evaluated using three in vitro assays, viz., DPPH, ABTS+, NO* radical scavenging activities. The total phenolic content of the extracts was determined using the Folin-ciocalteau method and the results are expressed in milligrams of phloroglucinol equivalents per gram of dry weight (mg PGA g-1 DW). The highest DPPH radical scavenging was shown by acetone: water extract of U. fasciata (IC50 2.21 mg ml-1) and the highest ABTS+ radical scavenging was shown by the aqueous extract of G. corticata (IC50 0.13 mg ml-1) followed by the acetone extract of H. valentiae (IC50 0.14 mg ml-1). The highest NO* radical scavenging was exhibited by H. valentiae (IC50 0.06 mg ml-1). The acetone: water extracts of U. fasciata and G. corticata exhibited very high phenolic content (59.13 mg PGA g-1 DW and 59.85 mg PGA g-1 DW, respectively). The study indicated that all three species showed increasing radical scavenging activities corresponding to the concentration of the extract and the solvent used for extraction. The presence of secondary metabolites like phenols, and terpenes also seem to have contributed to the radical scavenging activities.
Development, Optimization and Characterization of Sterically Stabilized Liposomes of Irinotecan
Authors: Thacker Krupali A. , Prajapati Bhupendra G.
Published: July 2024

The present investigation work summarizes the development of irinotecan liposome injection for intravenous infusion, 4.3 mg/mL (10 mL fill), a generic equivalent of reference product onivyde irinotecan liposome injection for intravenous infusion, 4.3 mg/mL (10 mL fill), which is indicated for colorectal cancer dosing for camptosar. Quality by design (QbD) approach has been used to develop generic irinotecan liposome injection and manufacturing process that ensures the quality, safety and efficacy of irinotecan liposome injection. Preliminary screening trials for drug (API) loading suggest that active loading process with extrusion process using ammonium dihydrogen phosphate shows better drug entrapment with less free drug. A 2(5-1) fractional factorial design of experiments (DoE) adopted to evaluate the effect of lipids concentration in ethanol, hydration temperature, hydration time, extruder temperature and extruder pressure on particle size. Based on design space, optimized process parameters were defined for maintaining the required particle size. A 2(4-1) fractional factorial DoE adopted to evaluate the drug loading heating temperature, drug loading heating time, drug loading cooling temperature and drug loading cooling time on particle size and free drug. Based on design space, optimized process parameters were defined for maintaining the required particle size and % free drug. Stability study of the final formulation suggest no any degradation of impurity and no any % free drug is increasing with respect to stability time. Also all characterization was performed on final formulation and all data is comparable with the reference formulation. The developed formulation of irinotecan liposome injection for intravenous infusion, 4.3 mg/mL (10 mL fill) shows less free and high entrapped drug compared to reference product with new remote loading agent except patent of onivyde.
Formulation and Characterization of Imatinib Mesylate Liposomes in Gel for Intraarticular administration
Authors: Gorajiya Amruta , Shelat Pragna , Lalwani Anita
Published: July 2024

Intra-articular administration of drug loaded in liposomal gel directly in joints provides spatial and prolonged local action by minimizing drug particle clearance from the synovial cavity. The objective of the present study was to prepare imatinib mesylate (IMT) containing liposomes, which were further loaded in xanthan gum gel for intraarticular administration to increase the duration of drug release. Liposomes were prepared by using different ratios of 1,2-Dierucoyl-sn-glycero-3-phosphatidylcholine, 1,2-Dipalmitoyl-sn-glycero-3-phospho-rac-glycerol and cholesterol using thin film hydration method. The liposomes were evaluated for entrapment efficiency, surface charge potential and size distribution to establish formulation composition and process parameters. Light microscopy and scanning electron micrographs of the liposomes showed the spherical topography of the prepared liposomes. Viscosity and gel strength of the gel loaded with IMT containing liposomes was evaluated. In-vitro release study showed that liposome gel formulations could significantly extend the drug release compared with conventional gel and liposome formulations. The formulation was studied for stability over a period of 6 months for pH, viscosity, drug release up to 7 days at two different conditions i.e. 2 to 8°C and 25 ± 2°C and 60% RH ± 5% RH. Analytical results are more promising and no significant difference was observed in these parameters when the formulation was stored at 2 to 8℃. In summary, liposome gel is expected to be an efficient cargo for intra-articular drug delivery of Imatinib mesylate.
A CROSS-SECTIONAL OBSERVATIONAL STUDY TO ANALYSE PRESCRIPTION PATTERN OF PROTON PUMP INHIBITORS IN A TERTIARY CARE TEACHING HOSPITAL
Authors: Singh Mehtab , Sidhu Shabir
Published: July 2024

The approved indications of proton pump inhibitors (PPIs) do not include generalized acid suppression. Rather these agents should be used for various forms of gastroesophageal reflux disease (GERD), patients receiving non-steroidal anti-inflammatory drugs (NSAIDs) with high bleeding risk. Several reports are available which show that chronic inappropriate use of PPIs results in severe adverse effects. Recent systemic reviews and meta-analyses studying the prescription pattern of PPIs in India over the last two decades revealed that the PPIs are being overprescribed, and prescribed for indications other than the approved indications. With this background, the current study was planned to explore the prescription and usage pattern of PPIs in a tertiary care teaching hospital. The present study was a cross-sectional observational study conducted at the punjab institute of medical sciences, Jalandhar after obtaining Institutional Ethics Committee (IEC) approval. The prescriptions received at the pharmacy department of the hospital from different open publication distribution system (OPDs) were screened.The data regarding demographics of the patient (gender, age), the prescribing department, and the total number of drugs prescribed per prescription was collected. Further, the prescriptions were analysed according to World Health Organization (WHO) prescribing indicators. It was observed that every second prescription received in the pharmacy department was of PPIs. In total 1000 prescriptions were screened and 500 prescriptions were for PPIs. 63% of the prescriptions were from female patients and the rest of the prescriptions were from male patients. The majority of the patients (58.4%) were in the age group of 18 to 40 years. 95.2% of the prescriptions contained PPIs in fixed-dose combination (FDCs) formulation. The most frequently prescribed PPI as a mono drug was pantoprazole (2.4%).The second active pharmaceutical ingredient (API), in all the FDCs, was observed to be a prokinetic agent, either domperidone or itopride. Only 4.8% of the prescriptions were from the gastroenterology clinic. The analysis of the prescription using WHO prescribing criteria showed that the average number of drugs prescribed per encounter was 4.63 and only 0.4% of the drugs were prescribed from National List of Essential Medicines (NLEM). The drugs prescribed by generic name were 81.4% against the optimal level of 100%. It can be concluded that PPIs are being prescribed without appropriate indication in most cases. These findings suggest the need for sensitization programs for practitioners for prescribing practices and appropriate use of PPIs.
Bee Venom Apitoxin Alleviates Collagen-Induced Arthritis In DBA-1J Mice
Authors: Jeon Ha-Young , You In-Soo , Koo Ja-Kap , Kim Sokho
Published: July 2024

The anti-inflammatory, antibacterial effect, and anti-aging properties of the venom of honey bee Apis mellifera L. have been investigated and exploited for pharmaceutical and cosmetic applications for decades. Apitoxin, a drug based on bee venom, is administered via injection and is permitted for use in humans for its antipyretic, analgesic, and anti-inflammatory properties. This study was conducted to expand the scope of apitoxin application to arthritis. We used a DBA-1J mouse model of collagen-induced arthritis (CIA). Apitoxin was injected intradermally into the mice twice a week, and the body weight, arthritis score, and hindlimb paw edema were recorded once a week for 4 weeks in mice with CIA. The body weight of the groups with CIA was significantly lower than that of the group without CIA during the experimental period. Although the arthritis scores of all groups with CIA were higher than those of the group without CIA, the high dose apitoxin-treated group had a significantly improved arthritis score than the vehicle group on days 14 and 28. A significant reduction in edema was observed in the hindlimb paws in the apitoxin-treated group compared with that in the vehicle group. Additionally, inflammatory cytokines, such as IL-6 and IL-1β, and IgG antibodies to type II collagen, were detected in the articular tissue of mice with CIA on day 28. Both IL-6 and anti-type II collagen IgG levels significantly decreased in the apitoxin-treated group compared with those in the vehicle group. Histopathological analysis of the articular tissue also revealed similar improved results in the apitoxin-treated group. In conclusion, these results suggested that apitoxin has potential therapeutic application in patients with arthritis.
PHYTOCHEMICAL SCREENING AND EVALUATION OF DIURETIC ACTIVITY OF SETARIA GLAUCA
Authors: Singh Feran , Sharma Pankaj , Jain Vinay , Bhargava Sarvesh
Published: July 2024

This study aims to research the diuretic properties of ethanolic extract of whole plant of Setaria glauca by Lipschitz model in albino rats. Ethanolic extract of S. glauca was administered to experimental albino rats orally at 2000 mg/kg p.o. The acute toxicity of the extract was evaluated as per OECD guideline 420–425. The LD50 of the extract was found to be between 2000 mg/kg p.o. male albino rats (n=6) were divided up into four groups. the control group was given saline as usual albino rats were divided into four groups to assess the diuretic activity of ethanolic extract of whole plant of S. glauca metabolic cages are used. group II contains furosemide (10 mg/Kg, p.o.) while groups III and IV receive saline as the control group’s vehicle. (100 mg/kg), medium (200 mg/kg), dosing of ethanolic extract of whole plant of S. glauca, respectively. Immediately following the methanolic extract of S. glauca, treatment Three rats were placed in each metabolic cage and kept at 21°C ± 0.5°C while all the rats were hydrated with saline (10 mL/kg, p.o.). urine the volume was measured. Each hour until the conclusion of the 5th hour and of each creature was calculated. The diuretic action and diuretic activity were decided based on the urine yield. Moreover, concentration of urinary sodium, chloride, and potassium particles was decided. The urinary Na+/K+ proportion and carbonyl anhydrase movement (Cl-/(Na+/K+)) where moreover surveyed. Animals were denied access to nutrient and water for a period of 5 hours. At the conclusion of the 5 hours, the total amount of urine accumulated with each metabolic cage has been measured. The volume of urine as well as the levels of the different ions, such as sodium, potassium, and chloride, were evaluated. Rats’ urine volume and concentration of urinary electrolytes increase because of the aqueous crude extract and of S. glauca.
Microwave Assisted Synthesis of some 3-(substituted benzylidine)-amino-2-phenylquinazolin-4(3H)-ones and Evaluation of their anticonvulsant activity
Authors: Rishipathak Dinesh D. , Karanjikar Chaitrali V. , Udavant Pavan B.
Published: July 2024

Quinazolin-4(3H)-one derivatives are recognized as central nervous system (CNS) depressants. Epilepsy, the second most common neurological condition after headache, is characterized by recurrent seizures of cerebral origin. Fifty million people worldwide and an estimated 6 to 10 million people in India suffer from epilepsy. It is of concern that the diagnosis and management of epilepsy is often suboptimal in developing countries. There is a growing need for better, stronger, and safer therapeutic treatments for epilepsy. Quinazoline-4(3H)-ones were investigated as a potential next step in creating effective antiepileptic drugs. Herein, we report the synthesis of 3-(substituted benzylidine)-amino-2-phenylquinazolin-4(3H)-ones from 3-amino-2-phenylquinazolin-4(3H)-one under microwave irradiation as heating source wherever required. The compounds were evaluated for anticonvulsant potential using maximal electro-shock induced convulsions in mice. The chemical structures of the synthesized compounds were confirmed by fourier transform infra-red (FTIR), proton nuclear magnetic resonance (1H-NMR), and carbon-13 nuclear magnetic resonance (13C-NMR) studies. All the compounds were subjected to toxicity studies and then evaluated for their anticonvulsant activity against the maximal electroshock (MES) seizure method. LD50 was found to be 1098 mg/kg and the duration of tonic phase was reduced upto 1.1 sec and that of stupor phase was reduced upto 80 seconds. Most of the animals were protected from death after induction of convulsions. The structure-activity relationship of the compounds revealed that the 4(3H)-quinazolinone schiff bases; viz. 3-(N,N-dimethylamino-benzylidine)-amino-2-phenyl- quinazolin-4(3H)-one, 3-(p-chlorobenzylidine)-amino-2-phenyl-quinazolin-4(3H)-one and 3-(furan-2-yl methyleneamino)-2-phenylquinazolin-4(3H)-one; by significantly shortening the tonic and stupor phases of convulsions compared to controls, these compounds demonstrated strong anticonvulsant potential.
AN LC-MS/MS METHOD FOR SIMULTANEOUS QUANTIFICATION OF PARACETAMOL AND PAMABROM IN HUMAN PLASMA
Authors: Thummar Kashyap N. , Patel Falgun , Pethani Trupesh , Dudhatra Bhumika
Published: July 2024

Back pain and menstruation pain are generally treated with a combination of paracetamol (PCM) and pamabrom (PAMA). In this study, a liquid chromatography/tandem mass spectrometry (LC-MS/MS) method for the simultaneous quantification of PCM and PAMA from human plasma is developed and validated for the first time. The analytes and the internal standard (IS), diclofenac, were eluted on a kromasil C18 (100 x 4.6 mm, 5 μm) column using a simple optimized mobile phase after being treated by liquid-liquid extraction. Using the electrospray ionization technique, quantification was carried out using a hyphenated tandem mass spectrometer with a flow rate of 0.4 mL/min and completing the entire run time within 4 minutes. For PCM and PAMA, the calibration curve was linear (r > 0.995) for the range of 40–8000 ng/mL and 20–4000 ng/mL, respectively. This method produced reliable findings since it was verified for specificity, accuracy, recovery, linearity, precision, matrix effect, and stability investigations, and the results were determined to be within acceptable parameters. The current study’s findings demonstrated that this technology’s simplicity, rapidity, and sensitivity allow for routine usage in exploratory or clinical monitoring of both medications in human plasma.
Development and Characterization of Methotrexate Bearing Emulsomes for Management of Skin Cancer
Authors: SAHU BHARTI , Kori Mohan L.
Published: July 2024

The present study is aimed to manage skin cancer via topical route, because of conventional chemotherapy having lots of drawbacks like drugs introduced into the body through an injectable route thus drugs are distributed between normal cell and cancerous cell than its leading to unaccepted side effects and requires high dose of drug. In this paper, main focus onto overcome these drawbacks, emulsomes were developed loaded with methotrexate bio-active agent. A 32 factorial design approach was employed firstly for the formulation development of emulsomes for different concentration of lipid content which was phosphatidyl choline, cholesterol and solid core lipid. Developed methotrexate loaded emulsomes were characterized for particle size, polydispersity index, zeta potential and entrapment efficiency and results revealed 127.21 ± 1.11 nm, 0.216, -24.21 ± 1.09 mv, and 81.37 ± 0.8%, respectively. Thus optimized lipid content was further used for optimization of type and concentration of surfactants9 and sonication time. Hence 18 formulations of emulsomes were developed and characterized for particle size, polydispersity index, zeta potential and entrapment efficiency and result 126 ± 1.09 nm, 0.215, -24.81 ± 1.19 mv, and 85.17 ± 0.3%, respectively. These formulations were tested for their in-vitro drug release studies and release data show the value of t½ for formulations EM4F11, EM4F18 and EM4F8 was more than 12 h and they were retarded drug release up to 85% till 24 h to get better-sustained drug release profile. Then stability study was performed for formulation EM4F11 at 2 ± 2°C, 25 ± 2°C and 60% RH and 40 ± 2°C and 75% RH and data identified that the formulations stored at temperature 25 ± 2°C and 60% RH and it was less than 2% degradation at the end of six months. Hence developed emulsomes formulation might represent a promising system for improving the bioavailability of lipophilic drugs. Moreover, emulsomes produce sustained drug release, which is beneficial clinically. Thus the presented system adds additional benefits to the well-known opportunities to the conventional delivery system and is helpful in minimizing the side effects of anti-cancerous drugs and well suited for the management of skin ailment.
Ethanolic Extract of Momordica dioica Roxb. Leaves Show Potent Anti-diabetic Activity on Experimental Wistar Albino Rats
Authors: ADLAK PRADEEP , Sagar Rakesh , KORI MOHAN LAL
Published: July 2024

Diabetes mellitus is one of the most common endocrine metabolic disorders and significantly impacts the health, quality of life, and life expectancy of patients as well as on the healthcare system. Herbal remedies are convenient for managing diabetes due to their traditional acceptability and availability, low cost, and fewer side effects. The study aimed to evaluate the anti-diabetic effects of ethanolic extract of Momordica dioica leaf in normal and streptozotocin (STZ)-induced diabetic rats. In the study, two doses of ethanolic extracts of Momordica dioica leaf (MDL) were administered to normal rats for an oral glucose tolerance test. For anti-diabetic studies in STZ-induced diabetic rats, the effects of extracts were observed for duration of 28 days for blood glucose alterations. After the completion of the experimental period, the experimental rats were sacrificed and the collected serum samples were subjected to various biochemical parameter studies, including lipid profile, glycosylated hemoglobin (HbA1c), urea, and creatinine level studies. Whereas the tissues collected were subjected to antioxidant studies followed by histopathological studies of the pancreas. In this research study, it was observed that the MDL extracts showed a significant reduction in blood glucose level, reverted the altered lipid profile, and increased HbA1c to normal. It significantly normalized the urea and creatinine levels, as well as levels of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH). Thus, from this study, it could be concluded that MDL extract exhibited potent anti-diabetic activity in STZ-induced diabetic rats. This significant activity may be due to the presence of gallic acid, rutin, charntin, ferulic acid, and ellagic acid.
A Comprehensive Review on the Nanocarrier-based Drug Delivery of Cabazitaxel
Authors: Uddin Rehan , Rajawat Jitendra S.
Published: July 2024

Drug resistance significantly impacts the anticancer activity of several taxane-based formulations, i.e., docetaxel (DTX) and paclitaxel (PTX) formulations in clinical research. Cabazitaxel is a second-generation taxane with high anticancer efficacy than paclitaxel and docetaxel. The structure of cabazitaxel depicts low P-glycoprotein (p-gp) efflux pump affinity, which could help overcome the taxane resistance. Cabazitaxel’s clinical use is limited to metastatic castration-resistant prostate cancer (mCRPC) who have progressed after the chemotherapy from the docetaxel because of its hydrophobicity and high toxicity as the less stability of its marketed formulation, Jevtana®. The nanomedicines of cabazitaxel have the potential to overcome the constraints of drug use and overcome taxane resistance. This review reports on the recent cabazitaxel-based drug delivery systems, explains the obstacles encountered in creating cabazitaxel nanoformulations and provides solutions to address these challenges.
Study on trace element and phytochemical profiling of Alpinia galanga rhizome and Clerodendrum colebrookianum leaves extracts and their in-vitro bioactivity
Authors: Imchen Putusenla , Zhimomi Betokali K , Phucho Tovishe
Published: July 2024

Alpinia galanga and Clerodendrum colebrookianum belonging to the Zingiberaceae and Verbenaceae family, respectively is known to have many physiological properties like anti-bacterial, anti-oxidant, anti-tumor, etc. Both the plant samples possess many admirable curative properties as traditional medicine for the treatment of various diseases and disorders. The aim of this work is to identify the phytochemical and elemental components of both plant extracts which will support the therapeutic and traditional use of both plant samples. The presence or absence of micro- and macro-elements in the extracts was determined using atomic absorption spectrometry (AAS). Phytochemical analysis of the acetone and ethanol extract of both the plant samples also showed the presence of some necessary phytochemicals. Two in-vitro techniques (2,2-diphenylpicrylhydrazyl (DPPH) and ferric reducing antioxidant capacity (FRAP) assay where the absorbance was measured at 517 and 700 nm, respectively) were used to assess antioxidant activity, and ascorbic acid and trolox were used as the reference standard. For the DPPH assay, the highest activity (IC50 = 54.82 μg/mL) was shown by the acetone extract of C. colebrookianum, and the lowest (IC50 = 67.41 μg/mL) was shown by the acetone extract of A. galanga. The anti-microbial studies also revealed that the best activity was shown by the acetone extract of C. colebrookianum leaves against Escherichia coli i.e., 12 mm with minimal inhibitory concentration (MIC) value of 0.117 mg/mL.
Exploration of the Distinctive Flower Diversity and their Therapeutic Efficacy from Surajpur District of Chhattisgarh, India
Authors: Rahangdale Tulsi Ram , Pandey Dhananjay , Ram Bharosh , Singh Surajbhan
Published: July 2024

The present research spots light on diversity and therapeutic potentiality of flowers collected from Surajpur district of Chhattisgarh, India. Recently, the traditional knowledge of flowers as therapeutics is gaining increased attention across the globe. The curative potentiality of flowers based on the traditional knowledge of local healers and village dwellers of Surajpur unturned the enigma of enormous efficacy of flowers against several alarming diseases. The different colours of same flower collected from six adjoining tehsils of Surajpur district also divulge that the flower possesses diverse colour and morphology in different areas which is an indicator of rich floral diversity of this region. Despite of immense flora, the region is relatively untouched with special reference to flower diversity and its ethno-medicinal studies. Keeping the above facts into consideration, an attempt was made to focus on the floral diversity and therapeutic efficacy of 68 flowers which covers twenty nine families to cure seventy eight dreadful diseases. The above documentation accord a clear insight on the vast biological and pharmacological potentiality of all the flowers under investigation. Although, the present work is an initial step towards the documentation of local potential flowers having tremendous healing ability with natural, cost effective and without any side effects. However, in time ahead vigorous efforts will be envisaged to extract the active compound from the flowers and to elucidate the complete structure of bioactives using spectral analysis. The above study will lay the strong foundation of floriculture and will definitely pave the path for natural floral medicine as curatives in years ahead.
FORMULATION AND IN VITRO EVALUATION OF FEXOFENADINE FLOATING TABLETS USING NATURAL AND SYNTHETIC POLYMERS
Authors: A Seetha Devi , Sankula Kameswara Rao
Published: July 2024

The extent of therapeutic advantages led to the development of controlled drug delivery systems, which could be taken once a day. The prime objective of these dosage forms would be single dose, which releases the active ingredient over an extended period. Secondly, it should release the active entity directly to the site of action, thus, minimizing or eliminating side effects. In the present manuscript, fexofenadine was selected as drug of choice to design effervescent gastric floating matrix tablets (EGFMT) using natural polymers as well as synthetic polymers as matrix-forming agents. Natural polymers comprise bhara gum, grewia gum and mucuna gum, whereas synthetic polymers consist of hydroxypropyl methylcellulose (HPMC) K4M, K15M, and K100M. These were compared; it was found that low concentrations of natural gum were enough to produce prolonged release. Hence out of three natural gums that were available, bhara gum had given promising results. Therefore bhara gum was selected for further studies.
Zinc Acetate as a Catalyst: Improved Method of Protection of Amino Group in Synthesis of Nucleobase Derivatives and its Biological Applications
Authors: Chaurasia Himani , Sharma Ashwani , Mishra Kuldeep , Pandey Archana
Published: July 2024

2-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-1H-benzoisoquinoline-1,3(2H)-dione was synthesized by reacting 5-amino uracil with 1,8-naphthalic anhydride in the presence of zinc acetate as a catalyst and screened for the in-silico/in-vitro antimicrobial activities. All the analyzed physicochemical descriptors (viz. drug-likeness, bioactivity score, and absorption, distribution, metabolism, excretion, and toxicity (ADMET)) of the compound provide an impetus to the docking results obtained by simulating against the catalytic site of Escherichia coli peptide deformylase enzyme (PDF, PDB ID: 1G2A) and allosteric site of human immunodeficiency viruses (HIV) reverse transcriptase enzyme (PDB ID: 3MEC). Docking results revealed that the compound has interacted well with the amino acid residues Lys103, Lys101, and Pro 236 of non-invasive blood pressure (NIBP) of human immunodeficiency viruses (HIV) reverse transcriptase (RT) and Ile44, Gly89, Leu91, and Glu133 of peptide deformylase (PDF). The predicted free binding energy ΔG (-6.83 kcal/mol) showed that the compound formed a stable complex with PDF protein receptor, thus, can behave as a probable drug regimen in antibiotics. Whereas, the calculated total binding energy (-38.87 kcal/mol) alluded to the anti-HIV property of the compound as probable nucleoside reverse transcriptase inhibitor (NNRTI). In-vitro antibacterial screening, results exhibited promising inhibitory activity against Pseudomonas aeruginosa and E. coli (MIC value, 12.5 and 25 μg/mL, respectively).
PROTECTIVE EFFECT OF NQO-1 MODULATOR QUERCETIN IN HYPERTENSIVE RATS
Authors: Kanzaria Sainika , Shah Hital , Patel Anjali , Gandhi Tejal
Published: July 2024

Despite abundant anti-hypertensive therapies, there always remains an opportunity (perhaps need) to identify novel targets. One such emerging target is NAD(P)H:quinone oxidoreductase 1 (NQO-1), which acts downstream in Nrf2 cascade. This study was planned to investigate the effect of Nrf2 activator quercetin on NQO-1 modulation in hypertensive wistar albino rats. The hypertension was induced by DOCA (25 mg/kg s.c. twice weekly) and 1% NaCl in drinking water. The animals were randomized into six groups receiving either vehicle (control), DOCA- 1% NaCl salt (model) or treatments (Telmisartan (10 mg/kg) and quercetin (10, 25, 50 mg/kg) for 5 weeks. Various haemodynamic parameters, left ventricular functions, biological markers, lipid and protein peroxidative marker, antioxidant enzymes activity as well as histology (heart and kidney) were carried out. The expression of mRNA of NQO-1 gene in heart homogenate was estimated. Treatment with quercetin significantly prevented the rise in blood pressure, organ weight, improved left ventricular function, cardiac markers profile, kidney markers, restored antioxidant enzymes along with decrease in lipid and protein peroxidation. The normal architecture of heart and kidney were preserved in histopathological analysis by quercetin treatment. The upregulation of NQO-1 gene in heart by quercetin resulted in normal blood pressure. Altogether, quercetin prevented hypertension, improved cardiac function by augmenting the innate cell defense system in DOCA-salt rats. Such promising effects are attributed to novel cellular level target, NQO-1, which have multiple effects like regularisation of oxidative stress, eNOS activation and inhibition of ACE shedding.
Apoptotic potential of bioactive fraction isolated from Aliidiomarina taiwanensis KU31894 against skin (A375) cancer cell lines
Authors: Unnikrishnan Nithin T. , Raghavan Keerthi Thalakattil
Published: July 2024

In the present study, the marine bacteria Aliidiomarina taiwanensis KU31894 was used. The bioactive secondary metabolites extracted from marine bacteria A. taiwanensis KU31894 were found to exhibit anticancer activity. The cell-free supernatant of the bacterial culture was extracted with ethyl acetate and showed effective cytotoxicity against skin cancer (A375) cell line, with IC50 concentration of 83.01 ± 1.6 μg/mL by MTT assay. Bioassay-guided fractionation of the ethyl acetate was done by silica gel column chromatography using gradients of the solvent system (chloroform: methanol). Fraction 7 exhibited cytotoxicity, with an IC50 concentration of 59.13 ± 2.53 μg/mL. The bioactive fraction treated cancer cell lines showed morphological changes such as cell shrinkage, rupture of the nuclear membrane, and chromatin condensation was visualized by AO/EB staining. Flow cytometric analysis of treated cancer cells showed a decreased concentration of DNA in the S phase and results in G0/G1 phase arrest. Apoptotic-related gene expression studies of treated cells illustrated the increased expression of pro-apoptotic gene Bax and tumor suppressor gene p53 and decreased expression of anti-apoptotic genes (Bcl-2 and Bcl-xL). These are the primary molecular mechanism following the implementation of apoptosis. The results concluded that A. taiwanensis KU31894 exhibit significant anticancer activity against skin cancer (A375) cells.
Synthesis, Preliminary Anticonvulsant (Electro-Shock) and Acute Oral Toxicity Screening of Substituted-3-Acetyl-2-(substitutedphenyl)-4-methylbenzo[b][1,4]thiazepin-5(2H)-yl)-1-(substitutedphenyl)propan-1-one
Authors: CHAUDHRI VIKASH KUMAR , Pathak Devender , Hussain Zeashan
Published: July 2024

The current research aimed to synthesize a novel series of 5-substituted mannich bases using the substitution at 5th position at which the hydrogen atom was replaced by two different substituents, p-nitroacetophenone and p-chloroacetophenone having significant anticonvulsant activity. A novel series of substituted-3-acetyl-2-(substitutedphenyl)-4-methylbenzo[b][1,4]thiazepin-5(2H)-yl)-1-(substitutedphenyl)propan-1-one (6a-6t) were synthesized and evaluated for pharmacological activity. A total of 20 compounds, were synthesized by conventional methods and the purity of synthesized compounds were confirmed by melting point and thin layer chromatography (TLC) analysis. Fourier transform infrared (FTIR), proton nuclear magnetic resonance (1H-NMR), mass and elemental analysis characterized the structures of lead compounds. All the novel synthesized compounds (6a-6t) were preliminarily screened by anticonvulsant activity by maximum electroshock induced seizure against phenytoin as a standard drug at a 30 mg/kg dose. In the results of the spectral study, all the compounds showed characteristic peaks in FTIR and 1H-NMR spectroscopy. Compounds containing chlorine moiety show [M+2]+ peak in mass spectrum. In this study all the novel synthesized compounds showed significant anticonvulsant activity. The most significant synthesized compound 3-acetyl-2-(3-chlorophenyl)-4-methylbenzo[b][1,4]thiazepin-5(2H)-yl)-1-(4-chlorophenyl)propan-1-one (6e) found as a primary class of anticonvulsants that have shown practically identical anticonvulsant action with uniquely lower neurotoxicity. Further, the preliminary safety profile of the most potent significant compound (6e) was screened for 'acute oral toxicity' as per organisation for economic co-operation and development (OECD) guidelines, in total fourteen days of observation the normal behavior of animals suggest that compound (6e) was safe and non-toxic in nature. This study suggested further modification and improvement in the field of anticonvulsants drug development.
Validation of Reverse Phase High-performance Liquid Chromatography Analytical Method for Osimertinib Mesylate and its Degradation Products for Osimertinib Mesylate Tablets
Authors: Bhutnar Arun D. , Sapale Seema R. , Vaidya Vikas V. , Desai Anita
Published: July 2024

The purpose of this study is to develop an accurate, simple, and fast reverse-phase high-performance liquid chromatographic (RP-HPLC) method and validate for analyzing organic impurities in osimertinib mesylate (OSM) tablets. The developed method separates and validated for chloro impurity, hydroxy impurity, methoxy impurity, des-acrylic acid impurity, N-oxide, OSM dimer and OSM. The separation of all these impurities were achieved on inert sustain C18 (4.6×250) mm, 3 μ column, The mobile phase consists of 0.1% formic acid with pH to 6.50 adjusted with ammonium hydroxide and acetonitrile delivered in gradient elution mode. The analytes were monitored at 268 nm. Stress studies were performed to evaluate the capability of stability-indicating of this method. The OSM was observed to be stable under thermal, photolytic and neutral conditions. However, it is labile under acidic, basic and oxidative conditions. All the degradants are well resolved form the principle peak OSM. All the major degradation products were isolated and characterized through UHPLC-IMS-Q-TOF-MS. The method was validated as per International Conference on Harmonization (ICH) guidelines, and the validation included specificity, limit of detection (LoD), limit of quantification (LoQ), linearity, accuracy, precision, robustness, and solution stability for isolated impurities and OSM. The method was developed for this drug product with the purpose of properly defining the quality specification of the drug product or drug substance. This method can be incorporated in the monographs of USP, EP/BP, IP etc.
Preliminary Investigation of Mimosa pudica Linn seeds extracts for antiulcer potential on experimental albino rats
Authors: SINGH PUNIT , KORI MOHAL LAL
Published: July 2024

Ulcer is a common disorder in oral mucosa and gastrointestinal. Number of synthetic drugs are available to treat ulcers but these drugs have undesirable side effects. The present study aimed to investigate Preliminary screening of Mimosa pudica Linn seeds for oral and stomach ulcers. Plant material of both plants were extracted with different organic solvents and yield was calculated. Preliminary phytochemical tests were applied for the detection of presence of different chemical constituents in petroleum ether, chloroform, ethyl acetate, ethanol and aqueous extracts. All these extracts were also screened for anti-ulcer effect on ethanol induced stomach ulcer and glacial acetic acid oral ulcer. The effect was observed by the measurement of ulcer index, percentage inhibition, pH Total acidity, and gastric volume. Biochemical assessment of antioxidant substances and pro-inflammatory mediators (TNF-α, IL-6 and PGE-2) were done in the mucosal tissues. Phytochemical screening revealed the presence of steroids, terpenoids, and fatty acid in petroleum ether and alkaloids, tannins and phenolic compounds in chloroform extract of M. pudica Linn seeds the ethyl acetate and ethanol extract contain flavonoids, tannins and phenolic compounds, glycosides. Results of Preliminary pharmacological screening was showed that ethanolic extract of M. pudica Linn seeds with 200 and 400 mg/kg b.w. dose have significant anti-ulcer potential and is comparable to the standard (Omeprazole and ORASORE Gel). The significant restoration of antioxidant substance and inflammatory mediators indicated supporting mechanism of ulcer healing of ethanolic extract. In conclusion, the anti-ulcer effects were showed in dose-dependent manner. The potential anti-ulcer effect may be due to presence of flavonoid components i.e., quercetin, luteolin, etc. in the ethanolic extract of M. pudica Linn seeds.
The heavy metal analysis of three Tinospora species frequently used in traditional medicine preparation sampled from different environmentally diverse locations
Authors: Janardhanan Hareendran Nair , Sasidharan Shan
Published: July 2024

Herbal drugs have been used as remedies for the treatment of a large number of human ailments since ancient times as part of the traditional medicine system. Significant groups of the indigenous systems of medicine are based on herbal drugs. Of these herbal drugs, Tinospora cordifolia plays a vital role in treating various diseases and disorders. But nowadays, these plants are heavily contaminated with heavy metals. Heavy metal contamination in herbal medicines is a global threat to humans, especially at levels above known threshold concentrations. This investigation aimed to evaluate the concentrations of four heavy metals: cadmium (Cd), lead (Pb), arsenic (As) and mercury (Hg) in three Tinospora species: T. cordifolia, T. crispa and T. malabarica using inductively coupled plasma - optical emission spectrometry (ICP-OES). Samples were collected from environmentally diverse locations. Our investigation made it clear that T. crispa had the highest quantity of heavy metals, followed by T. malabarica and T. cordifolia. In most samples, mercury and arsenic were above the detection limit recommended by WHO. Warty tubercle samples of T. species had significantly higher amounts of heavy metal when compared to the rest of the parts tested. In addition to this, the samples collected from industry/urban areas recorded a considerable amount of heavy metals. These results suggest that T. cordifolia for formulation should be properly collected from wild/rural areas in order to avoid the accumulation of harmful heavy metals. Furthermore, it was suggested that the cultivation of medicinal plants should be curtailed near environmentally polluted areas, especially industrial areas, to avoid health hazards. Usually, T. malabarica and T. crispa will substitute or adulterate for T. cordifolia. So, identifying T. cordifolia is very important before going for ayurvedic formulations. The present study’s findings also highlight the need for relentless monitoring of heavy metal residues to ensure the quality and safety of finished herbal products.
In-vitro Anti-oxidant Activity and Gas Chromatography–Mass Spectrometry Analysis of Methanolic Extracts of Saussurea lappa Clarke and Premna mucronata Roxb
Authors: Sadia Humera , Sumalatha Govindu
Published: July 2024

The main aim of the present investigation is identification of bioactive compounds from methanolic extraction of Saussurea lappa clarke and Premna mucronata, by GC–MS analysis and also evaluated the phytochemical screening. Methanolic extraction of S. lappa clarke and P. mucronata revealed the presence of flavonoids, phenolic compounds, triterpenoids, tannins, saponins, amino acids, proteins, steroids, gums and carbohydrates. Gas chromatography-mass spectrometry (GC-MS) analysis of the methanol extracts of S. lappa clarke and P. mucronata was performed on a GC-MS equipment. In-vitro antioxidant activity (hydroxyl radaical scavenging activity, determination of reducing power, metal chelating activity, carbon tetrachloride (ccl4) induced lipid peroxidation, inhibitory test on protein oxidative modification, lipid peroxidation assay, catalase assay and reduced glutathione assay) was evaluated by adopting different methods. The GC-MS analysis has shown the presence of different bio active compounds in the methanolic extract of S. lappa clarke A total of 10 compounds were identified in that the main active compounds are 2-nonynoic acid, lupeol and dodecanal and P. mucronata GC-MS analysis showed the presence 15 bio active compounds in that the main compounds are L-cysteine, undecanoic acid, tetradecanoic acid, gamma.-sitosterol, vitamin E acetate and fucosterol. From the results, it is evident that S. lappa clarke and P. mucronata contains various phytocomponents and is recommended as a plant of phytopharmaceutical importance. Methanolic extraction of S. lappa clarke and P. mucronata possesses antioxidant activity.