Journal of Applied Pharmaceutical Research (JOAPR)
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The potential effect of peel extracts of banana varieties: an in-vitro assessment
Get PDFBackground: Assamese cuisine is known for its use of kolakhar, a traditional ingredient; Rhizome, the skin and stem of bananas, can be used to make it. An ash filter from a banana tree is used to produce antacids. The word: kol” or “kola” is a local term for banana. In Assam, India, kolakhar is a common food additive and traditional ingredient. Method: Water is filtered through banana tree ashes to create this. The banana peel is burned after it has been dried. The ash is subsequently blended with water and left overnight. The mixture is filtered through a fine cloth once the ash has settled to the bottom of the container by the following morning. Several studies were carried out by evaluating the preparation of peel extract, Physicochemical parameters, antioxidant activity, etc. followed by some analytical methods to find the biologically active components, potential uses, and additional benefits of banana peels beyond what they currently serve as waste products. Finally, an antimicrobial study was performed by using the disc diffusion method. In this study, 4 different types of banana species investigated sought to determine the antioxidant capacity, antimicrobial activity, FT-IR, and UV to determine which one is better. Result: The physicochemical parameters, analytical technique, and assay provide an overview of the chemical characteristics, phytoconstituents, and food safety of kolakhar, which contribute to its unique properties in both traditional medicine and culinary applications. Conclusion: In conclusion, depending on the banana type used, banana peel extracts exhibit considerable promise as organic antioxidants and antibacterial agents. Therefore, considering all parameters, we obtained various potential effects from this study. The results are discussed with a graphical representation of the banana peel extract
Pharmacophore insights and molecular docking of ciprofloxacin analogues against 2XE1: strategies for reduced antibiotic resistance
Get PDFBackground: Antibiotic resistance is a silent pandemic disease that is growing and causing a global threat. Existing antibiotics are less effective against infectious diseases, so we must discover more potent and effective drugs. The latest report from the World Health Organization (WHO) underscores the global nature of the situation, revealing that high levels of antibiotic resistance in bacteria worldwide lead to life-threatening bloodstream infections and resistance to treatment. Methods: This study focuses on the Molecular Docking and Pharmacophore Modeling of Ciprofloxacin and its analogs to explore ligand-protein interactions and identify potent drugs against AMR. Twenty ciprofloxacin analogs, designed using ChemDraw Pro12.0, were docked with the 2XE1 protein. Molecular docking assessed the binding affinity, with Arguslab 4.0 scoring the lowest docking scores to indicate strong interactions and biological activity. Pharmacophore modeling identified essential molecular features like HBA, HBD, and AI for optimal biological activity. Results: The computational screening identified several compounds with improved binding properties, showing greater affinity towards ALA129, TYR149, and PHE88 amino acids, essential for biological activity. Conclusion: The study identifies the best analog of ciprofloxacin, which can effectively combat antibiotic resistance. Compound 13 showed promising docking scores and relevant pharmacophoric features, outperforming the parent ciprofloxacin in binding affinity, suggesting it could be a potent drug candidate against AMR
Analyzing the mechanisms involved in the antidiabetic activity of some native plants
Get PDFBackground: Research on diabetes treatment is advancing yearly, and it is estimated that 643 million adults worldwide will have diabetes by 2030. This is a comprehensive review of antidiabetic mechanisms in medicinal plants, aims to identify natural antidiabetic plants and provide details on their mechanisms of action, and rigorous testing techniques. Methodology: Information was gathered from offline and online sources to identify indigenous medicinal plants that lower blood glucose. Different databases were searched for ethnopharmacological literature using the following keywords: medicinal plants, diabetes, and India. Other sections about clinical trials, toxicological evaluations of certain plants, and preclinical trials have since been added. These sections were retrieved from Scopus using pertinent keywords. In this study, 117 species of medicinal plants from 55 families that are used to treat diabetes mellitus were listed. Conclusion: The variety of plants discussed in this review clearly demonstrated the importance of herbal plants in the treatment of diabetes. Result of the study shows Fabaceae, Rutaceae, and Combretaceae were the most prevalent plant families and species having antidiabetic properties among these plants. It also gives researchers information that they may use to develop future plans, like finding plants that may be effective in preventing diabetes and isolating bioactive molecules to help manage the disease. More research is necessary to completely comprehend these newly identified anti-diabetic drugs at the molecular, therapeutic, and physiological levels, nevertheless, in order to treat and manage diabetes mellitus globall
A pharmacognostic, phytochemical, and antioxidant potential of Oxalis triangularis
Get PDFBackground: To evaluate Oxalis triangularis with pharmacognostical parameters (macroscopy, microscopy & physico-chemical analysis), phytochemical analysis, and to investigate the in-vitro antioxidant capacity of different extracts obtained. Methods: Using specific standard protocols, the following tests were performed: loss on drying, extractive value, ash value, t.s. & powder microscopy, fluorescence analysis, and phytochemical screening. The Folin-Ciocalteu technique was adopted to ascertain the amount of phenolic compounds. In-vitro antioxidant activity was evaluated using 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) & 2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging assays. Results: The extractive values varied between solvents, ranging from 1.28% (ethyl acetate) to 18.8% (water), while the ash values were 16.25% (total), 2.9% (acid insoluble), and 10.625% (water-soluble). Numerous vascular systems, lignified trichomes, and calcium oxalate crystals were visible under a microscope. Saponins, steroids, flavonoids, phenols, anthocyanins, and alkaloids were detected by phytochemical screening; glycosides were not detected. At 200 µg/ml, the phenolic concentration of the ethanolic extract was the highest, at 1151.7 ± 59.22 µg/ml. The ethanolic extract exhibited greater DPPH (IC50 = 2.403 µg/ml) and ABTS (IC50 = 22.94 µg/ml) radical scavenging activity in comparison to the aqueous extract, i.e., (DPPH, IC50= 76.67 µg/ml & ABTS, IC50= 43.52 µg/ml). In contrast, both extracts showed notable antioxidant activity. Conclusion: A comprehensive examination of Oxalis triangularis revealed a rich reservoir of bioactive chemicals, such as phenols, which make the plant rich in antioxidant properties. This may serve as a foundation for the discovery of novel medicines
Insights of nose to brain delivery in treating Parkinson’s disease: A systematic review
Get PDFBackground: In Parkinson's disease (PD), a complicated neurodegenerative ailment, neurons in the substantia nigra that produce dopamine are lost, resulting in an insufficiency of the neurotransmitter that is essential for the regulation of voluntary and smooth muscular movements. This review focuses on the obstacle triggering the effectiveness of traditional PD treatments, which is the blood-brain barrier (BBB), which prevents some therapeutic medicines from reaching the brain. It encompasses the potential strategy of nose-to-brain administration by innovative approaches, including nanoparticles, liposomes, dendrimers, and cell-based carriers, directly delivering the drugs from nose to brain. Methods: The methodology involved examining the characteristics, advantages, applications, and challenges of various nanoparticles like SLNs, Nanoliposomes, Quantum dots, dendrimers, etc., through meticulous analysis of articles including from PubMed (5), ScienceDirect (5), Bentham Science (4) and Scopus databases (5). Conclusion: The review concludes by emphasizing the potential applications of nanoparticles in circumventing the problems encountered with traditional methods of drug administration in treating PD. This detailed study brings to light the applications and the challenges that need to be faced in utilizing nanoparticles for nose-to-brain delivery. Attention is directed towards the enlightenment of advanced carriers that target specific brain regions via the olfactory and trigeminal routes. The drug directly reaches the brain, bypassing BBB
Exploring the neuroprotective role of probiotics in the therapeutic interventions of cognitive decline
Get PDFBackground: Cognitive decline is developing as a critical alarm in public health concerns initiated by neuroinflammation, an indispensable contributing factor in neurodegenerative diseases. Probiotics and postbiotics have evolved as key therapeutic factors in treating neuroinflammation by modulating neuroinflammatory pathways and therapeutically controlling cognitive decline by its influence on the gut-brain axis. Methodology: This comprehensive review integrates the current status of the insight into the molecular mechanisms of probiotics that promote cognitive health. The review explains their synergistic effects on gut microbiota and their influence on neuroinflammation, mitochondrial function, neurotransmitter levels, and insulin sensitivity. It also explores preclinical and clinical studies involving the neuroprotective benefits of specific probiotic strains. Results: Probiotics are reported to alter gut microbiota by supporting neuroinflammation, thus enhancing cognitive function. The key findings were their role in reducing plaque formation and controlling tau protein hyperphosphorylation, thus improving mitochondrial efficiency. Recent research reveals that strains such as Lactobacillus and Bifidobacterium have proven efficacy in reducing tau phosphorylation and amyloid β pathology in animal models. In addition, probiotics improve insulin sensitivity and neurotransmitter levels, leading to improved cognitive outcomes. Discussion: The microbiota-gut-brain axis is essential in studying the neuroprotective role of probiotics. Probiotics have been reported for their ability to reduce neuroinflammatory markers, leading to improved neurogenesis in the brain's hippocampus. Thus transforming these research findings to clinical therapies requires further research to support and to overcome the limitations and exploring the complete mechanism involved.
Conclusion: Probiotics thus being explored to develop as new therapeutic interventions in cognitive decline, with substantial preclinical evidence supporting their benefits. Still persistent research is essential to transform these findings in clinical trials in the development of probiotic-based therapies for cognitive health
Antidiabetic effects of Semecarpus anacardium leaf extracts in streptozotocin-induced diabetes in rats
Get PDFBackground: A class of metabolic diseases known as diabetes mellitus is typified by persistently high blood sugar levels brought on by malfunctions in the production or function of insulin. Conventional treatments frequently have drawbacks and side effects, prompting interest in alternative treatments such as herbal remedies. Semecarpus anacardium, known for its medicinal properties, was investigated for its antidiabetic potential. Methods: Semecarpus anacardium leaves were collected, authenticated, and extracted using various solvents. The ethanol extract was subjected to preliminary phytochemical screening, HPLC-DAD analysis, and tested for antidiabetic activity in streptozotocin-induced diabetic rats. Biochemical parameters, histopathological studies, and lipid profiles were analyzed over a 20-day period. Results: The ethanol extract exhibited the highest yield (13.53% w/w) and contained significant amounts of bioactive compounds, including flavonoids and alkaloids. In diabetic rats, the ethanol extract at 200 mg/kg significantly reduced blood glucose levels from 333.35 ± 5.2 mg/dL to 121.68 ± 7.56 mg/dL. Highly significant results were obtained in lipid profiles, with total cholesterol reducing from 176.82 ± 1.07 mg/dL to 103.69 ± 2.85 mg/dL and triglycerides from 188 ± 5.73 mg/dL to 97.17 ± 8.41 mg/dL. Histopathological analysis showed partial restoration of pancreatic islets and reduced fibrosis, indicating the protective effects of the extract. Conclusion: The ethanol extract of Semecarpus anacardium leaves demonstrates significant antidiabetic and lipid-lowering effects in streptozotocin-induced diabetic rats. These findings support the potential of this plant as a natural therapeutic agent for diabetes management, warranting further research for clinical application
In vitro evaluation of Punica granatum fruit peel extract for its potential anti-diabetic effects
Get PDFBackground: With growing awareness of pomegranate's health benefits, pomegranate products have been consumed more frequently in recent years, and pomegranate peel has emerged as one of the most prevalent wastes in the food industry. Pomegranate Peel concentrate is an indigenous substance with strong antioxidant and antidiabetic actions as a result of its tannins as well as polyphenols content. Methods: In the present study, pomegranate skin extract, both liquid and alcohol-based, was evaluated for polyphenolic and flavonoid content. Alcoholic fruit peel extract was also assessed for 1,4-α-D-glucan glucanohydrolase and α-D-glucoside glucohydrolase enzyme activity. Results: According to findings, pomegranate peel extract showed significant antioxidant content. Phytochemical analysis of ethanol-derived extract of pomegranate peel found a noteworthy amount of ellagitannins and flavonoids such as Punicalin, Punicalgin, Punicic acid, Catechin, Quercetin, Rutin, and Kaempferol. In contrast, punicalgin, ellagic acid, and gallic acid are responsible for antidiabetic activity. The LC-MS characterization of peel extract of pomegranate showed 10 bioactive compounds. The IC50 value for 80% alcoholic extract of pomegranate peel was found to be 5.86 mg/ml of α- amylase and 6.58 mg/ml of α-glucosidase. Conclusion: It was found that the inhibition of 1,4-α-D-glucan glucanohydrolase and α-D-glucoside glucohydrolase enzymes could be an effective mechanism by which it can give anti-diabetic effects
Design and development of thermosensitive rectal in situ gel from Luffa acutangula fruits for the treatment of ulcerative colitis
Get PDFBackground: Luffa acutangula has good anti-inflammatory and antioxidant activity. Ulcerative colitis has inflamed intestinal mucosal lining with frequent diarrhoea, mucosal, and bloody stools. The rectal administration provides high bioavailability, rapid absorption, and instant therapeutic effect. Conventional rectal formulations may be painful, while insertion and discomfort may also be experienced from the rectum leakage. Methodology: Luffa acutangula fruit extract was used for the preparation a novel rectal mucoadhesive in situ-gel by using thermosensitive polymers such as Poloxamer 407, Poloxamer 188. HPMC K4M and carbopol 940 are two mucoadhesive polymers that are used to boost the mucoadhesive force and gel strength. The response surface method design was used to optimize the formulation. The formulated in situ gel batches were analysed by gelation temperature, gel strength, gelling ability, gelling time, viscosity and in vitro drug release and mucoadhesive strength. Results and Discussion: The concentration of poloxamer 407 (15%) and poloxamer 188 (3%) was optimized by design expert. The optimized formulation F10 showed 36.35±0.890 gelation temperature and 94.66±0.57 % cumulative drug release. Drug release kinetics follows Higuchi release model and according to Korsemeyer Peppa's model value of n= 1.1114 indicates supercase -II transport. Gelation temperature of mucoadhesive in situ gel (F10HP2) was found in the range 36.45±0.102°C with 91.37±0.84 % cumulative drug release. Mucoadhesive in situ gel was tested in rat model of ulcerative colitis for 7 days. Conclusion: Preclinical study of optimized formulation shows that Luffa acutangula fruit extract can stop or prevent further progression of acetic acid induced ulcerative colitis in rat model
Rivaroxaban solid dispersions for dissolution enhancement and formulation of mouth disintegrating tablets
Get PDFBackground: Work is carried out to improve rivaroxaban's dissolution rate (DR) and develop mouth-disintegrating tablets for rapid onset of action. Objectives: The work objective was to improve the dissolution rate of rivaroxaban using PEG 6000 by preparing its solid dispersions (SDs) further to prepare mouth-disintegrating tablets (MDTs). Methods: Methods like physical mixing, melting, and solvent evaporation were used to prepare SDs at 1:0.5, 1:1, and 1:1.5 w/w ratios of rivaroxaban with PEG 6000 were prepared. Differential scanning calorimetry (DSC) and Infrared spectroscopy (IR) were used to characterize the SDs. The selected solid dispersion at an appropriate drug: carrier ratio was used to develop MDTs by direct compression, using super disintegrants. Results: The SDs show improved solubility and rate of dissolution. SDs developed using a melting or solvent evaporation technique showed a more than two-fold increase in dissolution rate. In the dissolution study, after 60 min, the pure drug dissolved 45 %, while the prepared SDs showed almost more than 90 % within the same period. No significant drug carrier interaction was observed in the IR and DSC studies. However, minor shifts in peak values were observed for the characterization of functional groups in the drug structure. Conclusions: Formulation of solid dispersions of the drug with PEG 6000 is a successful approach for the dissolution rate improvement of rivaroxaban. This work for dissolution rate improvement of rivaroxaban using PEG 6000 showed significant improvement in dissolution rate at a 1:1 w/w ratio prepared by solvent evaporation method, which was further selected for mouth disintegrating tablet formulation