Innovare Academic Sciences: E-Journals
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AMELIORATIVE EFFECTS OF SELECTIVE PDE-10 INHIBITORS AGAINST KETAMINE-MEDIATED SCHIZOPHRENIC OUTCOMES IN MICE
No full textObjectives: Schizophrenia (SCZ) is characterized by significant impairments in perception and cognitive flexibility. Making accurate plans for therapy demands a deeper comprehension of the brain mechanisms behind these disorders. The purpose of our investigation is to analyze the protective effects of papaverine, a phosphodiesterase-10 inhibitor, on ketamine-induced SCZ -like behavioral and biochemical alterations in mice.
Methods: For 10 consecutive days, mice were exposed to ketamine (30 mg/kg; i.p.) to develop a SCZ-like phenotype. Various behavioral tests, including social interactions, catalepsy, cognitive impairment (Morris water maze), locomotor and anxiety (open field test), and immobility duration (forced swim test), were assessed. Biochemicals (acetylcholinesterase [AChE] activity, glutathione, and lipid peroxides), and histopathological alterations were also investigated. In this study, papaverine (30 mg/kg; i.p.) and clozapine (7.5 mg/kg p.o.) served as test and standard, respectively. Results were statistically analyzed and “one-way ANOVA” was performed, and Tukey’s multiple comparison test was subsequently applied.”
Results: After 28 days of ketamine therapy, significant (p≤0.05) behavioral alterations have been noted, including increased immobility duration, altered locomotor and anxiety-like behaviors, social interactions, cognitive impairment, and catalepsy. Significant alterations in histopathology, AChE activity, and oxidative stress (increased lipid peroxides and lower glutathione) were also observed in mice treated with ketamine. Treatment with clozapine and papaverine considerably (p≤0.05) improved the biochemical changes, behavioral problems, and histological changes.
Conclusion: We may conclude that papaverine may have neurodefensive effects against ketamine-induced SCZ in mice based on behavioral, histological, and biochemical observations
PHYTO-PHARMACOLOGICAL EVALUATIONS OF NELUMBO NUCIFERA (GAERTN) IN CYCLOPHOSPHAMIDE-INDUCED NEPHROTOXITY IN RATS
No full textObjectives: Nelumbo nucifera (Gaertn) (Sacred Lotus) is a medicinally important plant conventionally used for the treatment of inflammatory and oxidative stress-related disorders. The present study aimed to evaluate the phytochemical profile, antioxidant potential, and protective effects of methanolic and aqueous extracts of N. nucifera against cyclophosphamide (CP)-induced toxicity.
Methods: Extractive values of methanolic and aqueous extracts were determined, followed by preliminary phytochemical screening and quantification of total phenolic and flavonoid contents. Antioxidant activity was evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay. Cytotoxicity and growth curve studies were performed using wild-type and Δtrx2 yeast strains to assess biocompatibility and stress response. In vivo nephroprotective effect was evaluated in CP-induced nephrotoxicity models by measuring serum creatinine, urea, uric acid, protein, globulin, alanine aminotransferase, aspartate aminotransferase, glutathione, catalase, and malondialdehyde levels, along with pro-inflammatory cytokines tumor necrosis factor-alpha and interleukin-1 beta.
Results: The aqueous extract yielded higher extractive value (13.0% w/w), whereas the methanolic extract exhibited higher phenolic (1.50 mg/100 mg) and flavonoid (2.33 mg/100 mg) content. DPPH assay revealed potent free-radical scavenging activity for methanolic extract (IC50=42.32 μg/mL), closer to ascorbic acid. Yeast cytotoxicity studies confirmed the safety of the extracts and demonstrated their membrane-protective effects. In vivo studies showed that both extracts significantly (p<0.05–p<0.001) attenuated CP-induced alterations in renal and oxidative stress biomarkers, with methanolic extract (200 mg/kg) showing maximal protective effects.
Conclusion: N. nucifera extracts, particularly the methanolic fraction, possess strong antioxidant, nephroprotective, hepatoprotective, and anti-inflammatory activities. These findings support its potential therapeutic application in managing CP-induced nephrotoxity and oxidative stress-related disorders
TERATOGENICITY STUDY OF OLEANOLIC ACID (PENTACYCLIC TRITERPENOID) EXTRACTED FROM ROOT OF LANTANA CAMARA IN WISTAR RATS
No full textObjectives: The aim of the present study was to observe any teratological effects in the fetus parameters anogenital distance (AGD), crown to rump length (CRL), body weight, visceral as well as skeletal structure and dams fertility parameters due to repeated dose administration of oleanolic acid extracted from root of Lantana camara atthe different dose level of 250, 500 and 1000 mg/kg body weight in pregnant dams from implantation day to day before parturition. Furthermore, the aim of this study was to determine the no-observed-adverse-effect level (NOAEL)/lowest-observed-adverse-effect level (LOAEL).
Methods: Oleanolic acid was extracted from the roots of L. Camara by the extraction and isolation process. Three treatment groups at the dose level of 250, 500 and 1000 mg prepared in 0.1% between 80 and 0.5% CMC in milli Q water. Doses were administered once daily to pregnant rats from gestation day 5 to GD 19, and on GD 20, rats were terminally sacrificed. Biochemistry, hematology, body weight, feed intake, dam, and fetus parameters were observed.
Results: No test item-related significant changes observed in the evaluation of body weight, food, necropsy findings, organ weight, hematology, and biochemistry dam and fetus parameters (AGD, body weight, CRL, visceral and skeletal examination) at the maximum dose level of 1000 mg/kg bwt.
Conclusion: There were significant differences observed in the biochemical parameters, such as albumin, alkaline phosphatase, total bilirubin, total cholesterol, serum glutamic oxaloacetic transaminase, serum glutamic pyruvic transaminase, total protein, and hematology parameters such as hemoglobin, hematocrit, and mean corpuscular volume. These changes are not uniform, dose-dependent, minimal in magnitude, and not correlated with the histopathological findings of the respective organs. On theobservation of results of clinical signs, clinical pathology, histopathological findings, dams and fetus parameters, it may be concluded that NOAEL/LOAEL of test item oleanolic acid extracted from L. camara roots at the highest dose level of 1000 mg/kg body weight when administered orally once daily from gestation day 5 to gestation day 19
COMPREHENSIVE PHYTOCHEMICAL PROFILING AND PHARMACOLOGICAL SCREENING OF ETHNOMEDICINAL PLANT EXTRACTS TO INVESTIGATE THEIR ANTI-INFLAMMATORY, ANTIOXIDANT POTENTIAL AND ANTIULCER EFFICACY
No full textObjectives: The objective of the study was to evaluate the phytochemical composition and antioxidant, anti-inflammatory, and anti-ulcer activities of selected ethnomedicinal plant stem bark extracts.
Methods: Stem bark extracts were prepared using standard solvent extraction methods and subjected to phytochemical screening and chromatographic profiling. Antioxidant activity was assessed by superoxide radical scavenging and reducing power assays. Anti-inflammatory effects were evaluated using the carrageenan-induced paw edema model, while anti-ulcer activity was determined using the pylorus ligation–induced gastric ulcer model. Gastric secretion parameters and histopathological analysis were performed to confirm gastroprotection.
Results: The extracts exhibited a high content of phenolics and flavonoids, correlating with strong, dose-dependent antioxidant activity. Significant reductions in ulcer index, gastric volume, and total acidity were observed, with effects comparable to standard drugs. Anti-inflammatory studies showed marked inhibition of paw edema. Histopathological findings confirmed preservation of gastric mucosal integrity and reduced lesion severity in treated groups.
Conclusion: The results validate the traditional use of the investigated ethnomedicinal plants and demonstrate that acetone and ethanol extracts possess potent antioxidant, anti-inflammatory, and anti-ulcer activities, supporting their potential development as natural gastroprotective agents
PREPARATION AND OPTIMIZATION OF ONCE DAILY QUETIPINE FUMARATE SUSTAIN RELEASE TABLETS
No full textObjective: Quetiapine fumarate (QF) belongs to the atypical antipsychotic class. The elimination half-life of QF is 6 h necessitates the development of sustain release (SR) formulation. In the current research, two polymers, HPMC K100M and Polyox WSR N80, were used in combination as per the central composite design (CCD) with an objective of sustained drug release for 24 h with low initial burst release.
Methods: The SR matrix tablets of QF were prepared by wet granulation method. Fourier transform infrared and differential scanning calorimetry study for the physical mixture of QF with HPMC K100M and Polyox WSR N80 in 1:1 ratio demonstrated compatibility between the drug and polymers. The selection of the optimum formulation highlights the precision of CCD in optimizing the formulation parameters to achieve the desired release profile.
Results: The integration of two polymers, HPMC K100M (58.2 mg/tablet) and Polyox WSR N80 (44.8 mg/tablet), proved effective in modulating the drug release dynamics. Specifically, the polymers synergistically contributed in attaining the desired responses vis-à-vis Q1 9.73%, t50 10.45 h, and Q18 82.46%, thereby ensuring minimized initial burst release and sustained release of QF over 24 h.
Conclusion: The development of a once-daily formulation aligns with modern patient-centric approaches in pharmaceutical design, catering to convenience and improving quality of life for patients requiring long-term therapy
EVALUATION OF GASTROPROTECTIVE PROPERTIES OF COMBRETUM MOOREANUM LEAF
No full textObjective: This study aimed to evaluate the antiulcer activity of the leaves of C. mooreanum.
Methods: Methanol-dichloromethane extract of C. mooreanum (MDECM) was prepared and used for the study. The antiulcer activity of the leaf extract was evaluated in vivo using ethanol-, acidified ethanol-, aspirin-, and indomethacin-induced ulcers in rats. The MDECM was also subjected to phytochemical analysis.
Results: The MDECM showed a significant reduction in ulcer index in the four models. Compared to the other treatment doses, the 200 mg/kg demonstrated the highest inhibition in acidified ethanol-and aspirin-induced models, and was only marginally more effective than 400 mg/kg in the indomethacin-induced gastric lesion models. The MDECM (400 mg/kg) elicited a higher reduction of ulcer index compared to the standard drug, omeprazole, in the ethanol-induced ulcer model (p < 0.05). Also, the highest inhibition of gastric ulcer elicited by MDECM in the other three models were comparable to that of the standard drug. Phytochemical analysis showed the presence of alkaloids, flavonoids, tannins, phenolics, saponins, terpenoids, anthocyanins, and glycosides in MDECM.
Conclusion: C. mooreanum effectively protected the gastric mucosa against ulcer, supporting its traditional use in the treatment of gastric ulcers. Further studies are ongoing to isolate and characterize the active molecule(s)
Perception of the Social Governance of School Establishments and Teacher Engagement in Mutualist Activities: Case of Teachers Members of the Central Mutual Society for Teachers of Zoukoougbeu, Côte d\u27Ivoire
No full textThis study aims to determine the relationship between perceptions of school social governance and teachers’ motivation at work in the preschool and primary education district of Zoukougbeu. The theoretical anchoring of this study comprises the theories of the logic of collective action by Mancur Olson (1965), participatory governance by William Ninacs (2008), and the strengthening of Burrhus Frederic Skinner (1953). A quantitative sample of 100 primary school teachers, drawn from the reasoned choice sampling, in particular the screened sorting, and a qualitative sample of thirty (30) volunteers, including eight (8) former managers, were interviewed. In accordance with the study’s mixed-methods design, observation techniques, semi-structured interviews, and questionnaires were used. The quantitative data were statistically processed using SPHINX software version 4.5. The qualitative data were analyzed qualitatively. The main results reveal that teachers’ low engagement in Central Mutual of Teachers of Zoukougbeu (MUCIZ) activities stems from their negative perceptions of the social governance of schools in the preschool and primary education inspection of Zoukougbeu
DESIGN OF EXPERT-BASED ECO-FRIENDLY RP-HPLC ANALYTICAL METHOD FOR THE ESTIMATION OF LUMEFANTRINE FROM THE CARBON DOTS
No full textObjective: The most common and lethal malaria-causing species in humans, Plasmodium falciparum and Plasmodium vivax, are caused by protozoan parasites belonging to the genus Plasmodium. Due to the substantial therapeutic obstacles posed by these parasites, novel therapy strategies are being investigated. By improving the solubility and cellular absorption of antimalarial drugs, including lumefantrine (LUM), carbon dots (CDs), a new nanomaterial, hold promise for the management of malaria. In order to evaluate the stability, drug release profile, and percentage entrapment efficiency (%EE) of LUM-loaded CDs and support their potential for the treatment of malaria, this study set out to design and validate an analytical approach based on HPLC.
Methods: A Design of Experiments (DoE) strategy was employed to optimize the HPLC process, systematically altering the injection volume, flow rate, buffer ratio, and buffer pH to improve performance. The following responses were tracked: theoretical plates (Tp), tailing factor (Tf), drug peak area, and retention time (RT). Following the requirements of ICH Q2(R2), linearity was established for LUM throughout a range of 0.5 to 20 µg/ml.
Results: The result was a linear regression equation with an R2>0.999, demonstrating strong linearity. For both intra-day and inter-day studies, the method\u27s precision with a %CV<2% and accuracy between 98 and 102% ensured repeatability when used for evaluating LUM stability, %EE, and drug release in CDs. The technique exhibited sensitivity for low concentrations and selectivity, separating LUM from excipients and degradation products. Its eco-friendliness was confirmed with an AGREE score of 0.7, indicating less waste and solvent consumption.
Conclusion: The quantification of LUM in CDs, formulation parameter optimization, and the development of sustainable malaria treatment techniques are all made possible by this verified HPLC approach
ESTIMATION OF TRACE LEVEL OF N-NITROSO FLUOXETINE IMPURITY IN FLUOXETINE CAPSULES BY LC-MS/MS
No full textObjective: Nitrosamine impurities, particularly nitrosamine drug substance-related impurities (NDSRIs), have gained focus in recent past due to their carcinogenic potential. Due to the low sensitivity of conventional techniques like high-performance liquid chromatography (HPLC) and gas chromatography (GC), the exact levels of these impurities could not be determined. This study aims to develop and validate a sensitive liquid chromatography hyphenated with mass spectrometry (LC-MS/MS) method to estimate the trace levels of N-Nitroso fluoxetine (a fluoxetine-related NDSRI) in fluoxetine capsules (60 mg).
Methods: We developed a sensitive and selective LC-MS/MS method for the quantification of trace levels of N-Nitroso fluoxetine in fluoxetine capsules (60 mg) using the AB Sciex 5500+quadrupole ion trap (QTRAP) LC-MS/MS system. To achieve the maximum response at quantitation level for N-Nitroso fluoxetine impurity, chromatographic conditions optimized by selecting a specific combination of column, mobile phase, and diluent. Mobile Phase A and B consisted of 10 mmol ammonium acetate buffer and methanol, respectively. Waters X-Bridge C18 column (250 × 4.6 mm, 3.5 μm, Part No. 186003943) at temperature 40 °C and mobile phase flow rate to 0.5 ml/min has yielded consistent results by employing an optimized gradient elution program (Tmin/%B): 0/75, 2/75, 16/95, 28/98, 28.1/75, and 35/75 for the analysis. To further maximize the response of the N-Nitroso fluoxetine impurity, the multiple ion reaction monitoring (MRM) mass spectrometry method in positive electron spray ionization (ESI) mode is preferred over single ion monitoring (SIM) method.
Results: The newly developed method is validated by performing parameters such as specificity, method precision, intermediate precision, detection limit, quantitation limit, linearity, and accuracy in accordance with the international conference on harmonization (ICH Q2 (R1)) Guidelines. Limit of detection (LOD) and limit of quantitation (LOQ) are established as 0.06 ppm and 0.11 ppm, respectively. The method is found capable to demonstrate accuracy, precision, and linearity across the range of 0.11 to 1.68 ppm (10% to 150% of the specification), where linearity study shows the correlation coefficient (r²) greater than 0.99 for linearity plot between concentration and area. Recovery data at 10%, 50%, 100%, and 150% of the specification levels indicates that the recovered impurity content observed between 80% and 120%. Based on these results, we have successfully established the method for batch analysis of fluoxetine capsules (60 mg).
Conclusion: A new rapid and sensitive reverse-phase ultra-high-performance liquid chromatographic (UHPLC) method coupled with a mass spectrometry detector has been developed and validated for the estimation of N-Nitroso fluoxetine impurity in fluoxetine capsules. Method validation is accomplished according to the ICH Q2 (R1) guidelines, assessing parameters such as limit of detection, limit of quantitation, accuracy, precision, and linearity. We found the method suitable for its intended use and successfully applied it to test batches of the fluoxetine capsules drug product
PROFILING AND GROUPING OF FLAVONOID COUMPOUND USING LCMS FROM A COMBINATION OF WHITE TURMERIC EXTRACT AND HONEY AND ITS BIOACTIVITY TEST IN OBESE RATS
No full textObjective: The aim of this study was to identify and classify flavonoid compounds from a combination of white turmeric (Curcuma zedoaria) extract and honey, which have the potential as anti-obesity and anti-diabetic type 2 agents in obese Wistar rats.
Methods: This study used 25 rats divided into 5 groups, namely the normal, the obese, the obese group plus 100 mg/kg bw white turmeric extract, the obese group plus 100 mg/kg bw honey, and the obese group plus the combination of white turmeric and honey. The treatment was carried out for 4 w and the parameters measured were body weight, free fatty acid, glucose, and serum triglycerides levels of rats. Identification of flavonoid compounds using Liquid Chromatography-Mass Spectrometry (LC-MS).
Results: The results showed that the combination of white turmeric extract and honey was able to reduce the weight of rats (Lee\u27s obesity index), free fatty acid (FFA), glucose and triglycerides (TG) levels with significant differences (p<0.05) from the obese rats. The average decrease in glucose, triglyceride, free fatty acid, and Lee\u27s obesity index levels was 66.12%, 74.31%, 42.57%, and 20.59%, respectively. The results of LC-MS analysis identified 33 flavonoid compounds from white turmeric and 15 flavonoids from honey, which are thought to play an active role in reducing weight, free fatty acids, glucose and triglycerides.
Conclusion: The results of this study stated that there were 48 flavonoid compounds identified from the combination of white turmeric extract (Curcuma zedoaria) and honey which have the potential as anti-obesity and anti-diabetic type 2 in obese wistar rats