https://myresearchjournals.com/index.php/IJPSDR/issue/feed International Journal of Pharmaceutical Sciences and Drug Research 2022-06-07T09:00:25+02:00 Bavita Gaur [email protected] Open Journal Systems <p><strong>International Journal of Pharmaceutical Sciences and Drug Research (IJPSDR)&nbsp;</strong>is a bimonthly, international published online Journal devoted to Pharmaceutical and allied Sciences. IJPSDR is included in&nbsp;<a href="https://ugccare.unipune.ac.in/Apps1/User/User/ViewDetails?JournalId=101002202&amp;flag=Search"><strong>UGC-CARE List of Journals</strong></a>, published by University Grant Commission (UGC) India, for the purpose of Career Advancement Scheme (CAS) and Direct Recruitment of Teachers and other academic staff as required under the UGC.&nbsp;</p> <p>IJPSDR publishes innovative research papers, reviews, mini-reviews, short communications and notes either experimental or theoretical in the following area:</p> <div> <div> <ul> <li class="show">Pharmaceutical Technology</li> <li class="show">Pharmaceutics</li> <li class="show">Biopharmaceutics</li> <li class="show">Pharmacokinetics</li> <li class="show">Pharmaceutical/Medicinal Chemistry</li> <li class="show">Computational Chemistry</li> <li class="show">Molecular Drug Design</li> <li class="show">Pharmacognosy</li> <li class="show">Phytochemistry</li> <li class="show">Pharmacology</li> <li class="show">Pharmaceutical Analysis</li> <li class="show">Pharmacy Practice</li> <li class="show">Clinical and Hospital Pharmacy</li> <li class="show">Cell Biology</li> <li class="show">Genomics and Proteomics</li> <li class="show">Pharmacogenomics</li> <li class="show">Bioinformatics</li> <li class="show">Biotechnology</li> </ul> </div> </div> <p>All manuscripts are subject to rapid peer review. Those of high quality (not previously published and not under consideration for publication in another journal) will be published without delay.</p> https://myresearchjournals.com/index.php/IJPSDR/article/view/9501 Visible Light Promoted Catalyst Free, the Sustainable Synthesis of Dihydropyrano [2,3-C] Pyrazoles and Docking Studies with COVID-19 Mpro 2022-06-07T09:00:25+02:00 Shafiullah [email protected] Mohd Rehan [email protected] A highly efficient, simple, cost-effective, and environmentally benign method has been described for the synthesis of dihydropyrano[2,3-c]pyrazoles via one-pot, three-component condensation of 3-methyl-1- phenyl-2-pyrazoline-5-one, malononitrile, substituted aromatic aldehydes under visible light irradiation in catalyst-free condition at room temperature. This methodology's main advantage is good to excellent yield, simple work-up procedure, mild and clean reaction conditions, no chromatographic separation, and catalyst-free condition. All synthesized compounds are screened in silico with 6LU7, which is a COVID-19 Mpro. These computational studies were performed on AutoDock Vina, BIOVIA Discovery Studio 2017 R2, Auto Dock Tools-1.5.6 software. From screening results, we found that compound 4i and nitro group compounds 4d, 4e, 4f are showing a strong correlation at the active center of 6LU7. So, it is predicted that these compounds may be useful for COVID-19 patients. 2020-01-30T00:00:00+01:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9502 Effect of Vitex trifolia on Alloxan induced Diabetic Rat 2022-05-31T17:28:39+02:00 Neelakanth M Jeedi [email protected] Harsha M Naikwad [email protected] The leaves of plant Vitex trifolia by tradition used to treat of diabetes and correlated complications. Plants V. trifolia and Vitex negundo belongs to the Verbenaceae family, have some similar phytoconstituents. Leaf extract of Vitex negundo proven for its anti-diabetic property. Diterpenoids present in fruits of V. trifolia, they have anti-diabetic property. Vitexilactone a phytoconstituents in V. trifolia has insulin sensitizing property. The present study aimed to investigate in vivo anti-diabetic activity of aqueous leaf extract of V. trifolia in alloxanized diabetic albino wistar rats. Diabetes induced in rats by injecting alloxan hydrate at dose 150 mg/kg body weight. Diabetic rats were treated with 100 and 200 mg/kg of aqueous extract of V. trifolia for 21 days. Anti-diabetic activity of extract assessed by measuring blood glucose by Trinder's method, insulin by enzyme-linked immunosorbent assay, lipid profile by colorimetric methods, total proteins by Biuret method and calcium measured by using ligand Arsenazo III in an aqueous alkaline medium. Aqueous extract of V. trifolia did not show significant changes of blood sugar level in normal rats. But extract significantly reduces blood sugar, total serum cholesterol, triglycerides levels but increases insulin, HDL-cholesterol, total proteins, and calcium in diabetic rats. Aqueous extract of V. trifolia showed significant anti-diabetic activity in alloxan-induced diabetic rats. 2020-01-30T00:00:00+01:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9503 Statistical Optimization of Miconazole Nitrate Microemulgel by using 23 Full Factorial Design 2022-05-31T17:28:39+02:00 Rajesh Desai [email protected] Jayesh Dhalani [email protected] Suresh Koradia [email protected] Pankaj Nariya [email protected] Miconazole nitrate is a broad-spectrum antifungal agent, poorly water-soluble drug, and is used to treat superficial fungal infections. Microemulgel could increase drug deposition over to the skin. Therefore, the aim of this study was to prepare 2% miconazole nitrate transparent micro emulgel that contains 99% w/w liquid. Preliminary screening of oils and polymers was carried out. Oil phase of the microemulgel selected based on maximum solubility of miconazole nitrate in oil. A 23 full factorial design was used to check the effect of cinnamon oil (X1), HPMC K4M (X2) and tween 20 (X3) on viscosity (Y1) and % of cumulative drug release at 6 hours (Y2). Multiple linear regression analysis, ANOVA and graphical representation of the influence factor by 3D response surface plots were performed using Design Expert 7.1.5. A checkpoint batch was prepared to validate the evolved model. Optimized batch F5 was found to be stable and it showed globule size 26 ± 3 µm. In Ex-vivo drug permeation study batch, F5 was shown 87.05 ± 2.42% drug released after 6 hours and drug deposition on the upper layer of skin was found 52.5%. Accelerated stability study showed no significant change in the micro emulgel parameters within three months, and similarity factor f2 was 91.05 ± 1.67 %. Therefore, 2% miconazole nitrate micro emulgel was providing an effective treatment against topical infections. 2020-03-03T00:00:00+01:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9504 Optimization of Repaglinide Osmotic Drug Delivery System Using Two Different Techniques 2022-05-31T17:28:40+02:00 Roshan Salfi [email protected] Fatima Shireen [email protected] Makula Ajitha [email protected] The current study aimed to formulate an elementary osmotic pump (EOP) and push-pull osmotic pump (PPOP) based drug delivery system for controlled release of an anti-diabetic agent, repaglinide is expected to provide sustained release. EOP and PPOP method prepared repaglinide tablets by wet granulation technique. EOP designed 15 formulations F1-F15 and 14 formulations were done by PPOP method. All the formulations were evaluated for various physicochemical parameters and in-vitro dissolution studies. The release data was fitted into mathematical kinetic modeling studies to check the release mechanism. Further, the optimized formulations from both methods were characterized by FTIR and stability studies. EOP and PPOP methods successfully prepared repaglinide osmotic tablets. All the formulations exhibitedb satisfactory results for all evaluated parameters. The highest drug release was exhibited from F15 prepared by EOP method with 99.76% and FF14 with 15% coating prepared by PPOP method with drug release of 99.73%. Based on the in vitro dissolution profile, formulation F15 and FF14 exhibited zero-order with Korsmeyer-Peppas kinetics with Fickian diffusion-controlled release mechanism with high drug release in 24 hours and hence were selected as optimized formulations. The drug-excipient compatibility study by FTIR indicated no significant interactions between drugs and excipients. The formulations were stable after 3 months of accelerated stability studies. EOP and PPOP were designed to effectively administrate repaglinide drugs for a prolonged period of time. 2020-03-11T00:00:00+01:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9505 Comparative Phyto-Remedial Effect of Zingiber officinale and Cuminum cyminum on Hepatocytes of Alloxan Induced Diabetic Mus musculus 2022-05-31T17:28:40+02:00 Arun K Singh [email protected], [email protected] Roushan Kumari [email protected], [email protected] Sudhanshu K Bharti [email protected], [email protected] Diabetes mellitus is a metabolic disorder that causes chronic hyperglycemia. Diabetes and its crippling complications are a significant cause of morbidity and mortality. This study evaluates the comparative antihyperglycemic and hepatoprotective effects of alcoholic extracts of rhizome of Zinger officinale plant and seed extract of Cuminum cyminum plant on alloxan-induced diabetic mice. Mice were divided into four groups (one normal control, one diabetic control and two diabetic groups treated with the two extracts). Mice were induced diabetes by intraperitoneal administration of alloxan. Normal control and diabetic control mice received normal saline water during the treatment period while diabetic mice were administrated with ethanolic extracts of ginger rhizome @100mg/kg/BW and cumin seeds extract @80mg/kg/BW for 16 weeks. At the end of the experiment, animals were sacrificed, and biochemical as well as histopathological examinations were carried out. Hyperglycaemia with increased SGPT and bilirubin have been observed in diabetic mice. However, normoglycemic conditions along with restored liver marker enzymes have been observed in diabetic rats treated with extracts. Histopathological examination showed that alloxan administration causes damage to hepatic cells. Conversely, in ginger and cumin-treated diabetic groups, a significant improvement in the architecture of hepatic cells has been observed, which showed the ability of the extracts to repair the damaged tissue. Thus, this study safely submitted that ginger and cumin significantly reduce the blood glucose level, with ginger having greater potential as a hepatoprotective agent than cumin. 2020-03-29T00:00:00+01:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9506 Assessment of Hepatoprotective Activity of Hyptis capitata Jacq. Against Oxidative Stress Induced by H2O2 2022-05-31T17:28:40+02:00 V Sumitha [email protected] I Mini [email protected] Laija S Nair [email protected] Medicinal plants occupy a key position in maintaining the health of the human population. Hyptis capitataJacq. is an exotic ethnomedicinal plant of Lamiaceae possessing immense potential. The present study was carried out to assess the in vitro hepatoprotective activity of methanolic leaf extract of H. capitata against H2O2 induced oxidative stress in HepG2 cell lines. Total antioxidant capacity and Superoxide radical scavenging activity of the extract were also performed. The extract displayed considerable free radical scavenging activity (P IS LESS THAN 0.01). MTT assay was used to assess the in vitro hepatoprotective activity in HepG2 cell lines. The extract displayed concentration-dependent cell viability with maximum protection (63.97 ± 1.23%) in H2O2 induced HepG2 cell lines at 100 μgml-1. H. capitata is a promising herb with significant antioxidant and hepatoprotective potential. 2020-03-28T00:00:00+01:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9507 Research Article Total Phenolic, Flavonoid Content, and Antioxidant Activity of Justicia tranquebariensis LF and Cycas Beddomei Dyer. Leaves 2022-05-31T17:28:40+02:00 Veluru Hari [email protected] Dhamotharan Jothieswari [email protected] Kalluru Sesha Maheswaramma [email protected] Polyphenolics such as tannins and flavonoids are proved as powerful antioxidants to resolve cellular stress, sustain homeostasis in the body and prevent stress-associated disorders. Plant-based medicine gained importance due to its safety margin and multiple benefits. Regular intake of antioxidants is an alternative to avoid serious illness. The current investigation is aimed to measure the phenolic, flavonoid content, the antioxidant activity of Justicia tranquebariensis L.f. and Cycas beddomei leaves. The selected plants are used by tribes and traditional medicine to cure various diseases. Total phenolic content was estimated using the Folin–Ciocalteu colorimetric method, taking gallic acid as standard. At the same time, total flavonoid content was determined by aluminum chloride colorimetric assay using Rutin as standard.The absorbance was measured at 760 nm and 510 nm, respectively. Antioxidant activity was measured by two In vitro methods (DPPH and NO free radical scavenging assay) using standard protocols, where Ascorbic acid served as a reference standard. Results disclosed that the total phenolic content for the methanolic extracts of C. beddomei (36.14 ± 1.72) and J. tranquebariensis (28.57 ± 0.91) was found to be higher than petroleum ether extracts. Similarly, C. beddomei (28.13 ± 2.48) is richer in flavonoids than Jtranquebariensis (20.32 ± 1.24). In DPPH assay, methanolic extract C. beddomei (78.21%) is more effective to inhibit the free radicals than J. tranquebariensis (73.05%) with IC50 values 41.55µg/ml AND 59.52 µg/ml respectively at higher doses that are comparable to standard ascorbic acid (84.34%, IC50 =63.27 µg/ml). Similarly, in NO free radical scavenging assay, methanolic extract of C. beddomei (72.54%) stood best among all to scavenge the free radicals with IC50 values 50.06 µg/ml, whereas ascorbic acid is found to inhibit 83.26% with IC50 values 39.75µg/ml. The presence of various secondary metabolites such as alkaloids, carbohydrates, phenols, steroids, terpenoids, glycosides, saponins, especially tannins and flavonoids, either alone or in combination, may be responsible for the observed scavenging property. The quantity of the phenolic compounds and flavonoids can be directly correlated to the exhibited activity. 2020-03-29T00:00:00+01:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9508 Enantioselective RP-UFLC Method for the Simultaneous Estimation of Sitagliptin (STG) Enantiomers (R and S) in the Racemic Mixture and their Pharmacokinetic Assessment in Male Wistar Rats 2022-05-31T17:28:40+02:00 Ciddi Veeresham [email protected] Chinta Srinivas [email protected] Husna Kanwal Qureshi [email protected] Panga Shyam [email protected] The present work aims to develop and validate a simple, rapid, and reproducible reverse phase ultra-fast liquid chromatography method with a UV detector (RP-UFLC-UV) was developed for the separation and determination of sitagliptin (STG) enantiomers (S-(STG) and R-(STG)) simultaneously. Baseline separation was achieved on Lux cellulose-1 column, (cellulose tri-(3,5-dimethyl phenyl carbamate (Chiralcel OD-RH, 250 mm × 4.6 mm, 5 µm) column and mobile phase consisted of 20mM borate buffer solution (pH = 9±0.05) and ACN in the ratio of (60:40, v/v) at a flow rate of 0.8 mL/min was used. Detection of peaks was monitored at 262 nm. For analyzing the STG enantiomers in the rat serum and pure API, a method was developed using the chiral RP-UFLC-UV method was validated. The single oral dose of 2.5 mg/kg of STG racemate was administered to a group of 6 healthy rats for a comparative pharmacokinetic study of both the enantiomers. The linear range of the calibration curve for each enantiomer was 0.5–64 µg/mL. The precision of this method at concentrations between 0.5–48 µg/mL was within 8.65% and the % recovery (accuracy) of both sitagliptin (STG) enantiomers (S-(STG) and R-(STG) were 98.47–101.02% and 98.93- 100.52%. The precision at LLOQ (0.5 µg/mL) was between 8.65%-7.09%, which was poor than that at QC levels, and the average extraction recovery was higher than 85% for both sitagliptin (SGT) enantiomers at QC levels, and its pharmacokinetics of enantiomers was found to be stereoselective. 2020-03-30T00:00:00+02:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9509 Quantitative and Qualitative Assessment of Marketed Nutraceuticals for Active Ingredients and Heavy Metals for Safety and Efficacy 2022-05-31T17:28:40+02:00 Anju Dhiman [email protected]; [email protected] Rohit Bansal [email protected]; [email protected] The global nutraceutical market is expanding fast, and people nowadays are inclined towards nutraceutical supplements for daily micronutrient needs and health benefits in some disease conditions. Hence, ensuring the safe and effective use of these supplements is the need of the hour. The current study is aimed at determining the accuracy and regulatory compliance of marketed nutraceutical formulations by quantifying the active nutraceutical ingredients and heavy metal content in these formulations using advanced analytical techniques. Total 12 marketed formulations were selected and analyzed in NABL (National Accreditation Board for Testing and Calibration Laboratories) accredited laboratory using High-performance liquid chromatography (HPLC) and inductively coupled plasma-mass-spectrometry (ICP-MS). The quantified values were compared with label-stated values and recommended values as per FSSAI. The quantified values in two lycopene samples varied significantly (-16 and +16%) from the label stated content and were found non-compliant with the regulatory recommendations. The measured intake values of calcium and vitamin D varied from 24 to 204% from the recommended daily allowances established by FSSAI. The quantified daily intake values varied from 4.2 to 58 mg and from 4 to 21.5 mg for lycopene and lutein, respectively. Heavy metal content determination resulted in two samples deviating from the tolerance limits of heavy metals for lead and arsenic. The mean values for lead and arsenic were found to be 2.482 ± 6.921 and 0.311 ± 0.655 ppm, respectively. The present study results provided vital information on the composition of marketed nutraceutical formulations. The regulatory agencies require stringent monitoring practices to ensure compliance with the existing regulatory guidelines to provide the consumer safe and effective nutraceutical products. 2020-03-30T00:00:00+02:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9510 Evaluation of Healing Effect of Stromal Vascular Fraction and Platelet Rich Plasma Application on Ulcerative Ear Wound in Diabetic Rabbit 2022-05-31T17:28:41+02:00 Vijay Sharma [email protected] Anuka Sharma [email protected] Parag R Ghorpade [email protected] Manohar Nandanwar [email protected] Atul Kansagara [email protected] Sandeep Tripathi [email protected] A debilitating complication of diabetes mellitus is diabetic ulcers, which leads to increased overall morbidity in patients. The high growth factor content in Platelet Rich Plasma (PRP) makes it a widely used intervention for the treatment of diabetic foot ulcers. The topical application of Stromal Vascular Fraction (SVF) could possibly enhance wound healing. This study aims at evaluating the efficacy of combining SVF and PRP on wound healing in diabetic rabbit model. Diabetes was induced in New Zealand white rabbits by intravenous injection of 125 mg/Kg Alloxan. After two weeks of alloxan, three 6 mm diameter, full thickness excision wounds were made, on inner side of the right ear pinna. The animals after induction were allocated into 4 groups with [8 Diabetic (treated with SVF+PRP), 4 Diabetic (treated with 10% Povidone Iodine (PI)), 1 non-diabetic (treated with SVF+PRP), 1 non diabetic (treated with 10% PI)]. The effect of combined therapy was evaluated by assessing wound margin closure rate, histo-pathological evaluation, and inflammatory cell infiltration, epithelization of ulcerative region, neo-vascularization, and fibrosis. We observed that the rate of wound closure is enhanced in wounds treated with SVF+PRP as compared to the PI solution. Wound closure and healthy healing were demonstrated by histo-pathological analysis. The analysis clearly indicates that the healing process of PI treated animals is slower than that of SVF + PRP treated animals. In conclusion, based on wound healing assessment and histo-pathological examination, the diabetic rabbits treated with SVF + PRP exhibited early development of granulation tissue and early signs of wound closure as compared to diabetic animals with normal PI dressing 2020-03-30T00:00:00+02:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9511 Design, Synthesis and Molecular Docking Study of N-Heterocyclic Chalcone Derivatives as an Anti-cancer Agents 2022-05-31T17:28:41+02:00 Bharti Fegade [email protected] Shailaja Jadhav [email protected] The Claisen-Schmidt condensation of 4-(aryl)-aminobenzaldehyde and 2-hydroxyacetophenone resulted in a new series of heterocyclic chalcone (4a-4g) derivatives. Nucleophilic aromatic substitution (SNAr) of 4-fluorobenzaldehyde with heterocycle amines by ultrasonication in the presence of a base and polar aprotic solvent yielde 4-(aryl)-aminobenzaldehydes. Spectral investigations were used to establish the structures of synthesized compounds. The in vitro anti-cancer activity of the synthesized derivative was evaluated against MCF-7 (breast cancer) cells by SRB assay. Compounds 4c, 4b, and 4c have a high affinity for the ER receptor binding site, whereas compounds 4c and 4g have a moderate affinity for the VEGER-2 receptor. The GI50 value of 4c ((E)-1-(2-hydroxyphenyl)-3-(4-(4-methylpiperazin-1-yl)-phenyl) prop-2-en-1-one) was 44.6 uM, while the GI50 value of all other derivatives was greater than 80 uM. These findings lay the groundwork for additional research into the combination's potential uses in cancer therapy. 2020-03-30T00:00:00+02:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9512 A Validated LC-MS/MS Method for Pharmacokinetic Study of Edoxaban in Healthy Rabbits 2022-05-31T17:28:41+02:00 D Atul Vasanth [email protected] B Rajkamal [email protected] A liquid chromatography-tandem mass spectrophotometric (LC–MS/MS) method was developed to quantify Edoxaban in rabbit plasma employing liquid liquid extraction with ethyl acetate. Developed method was validated for specificity, precision, accuracy, recovery, and stability characteristics. Chromatographic separation was achieved on Chromolith C18column (100 mm x 4.6 mm x 5 µm) with 70:30 ratio of methanol and 0.1% formic acid as an isocratic mobile phase with a flow rate of 0.80 mL/min. The developed LC-MS method was applied to assess pharmacokinetics parameters of edoxaban in healthy rabbits. Six Male albino rabbits weighing 2.0-2.5 Kg were randomly selected for the pharmacokinetic study. Blood samples (1-mL) were withdrawn from the marginal ear vein from 0 to 24 hours after administration (1.2 mg/kg). Plasma was separated by centrifugation and the plasma concentrations of edoxaban at various times were determined by LC-MS/MS. Pharmacokinetic parameters was calculated. Edoxaban showed Tmax of 2.0 and mean Cmax, AUC0®t andAUC0®a for Test formulation is 213.83 ± 10.46, 945.13 ± 24.32 and 986.135 ± 19.31, respectively. A highly specific, rugged, and rapid method with sufficiently low LLOQ was developed to analyze routine samples of single dose or multiple-dose pharmacokinetics with any marketing formulation of edoxaban. 2020-03-30T00:00:00+02:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9513 Investigations on Flavonoid-rich Extracts of Martynia annua Linn. and Tephrosia purpurea Linn. for Anti-inflammatory and Antihemorrhoidal Effects in Rats 2022-05-31T17:28:41+02:00 Mohan L Kori [email protected] Rakesh Singh [email protected] The present study is aimed to study the anti-inflammatory and anti-hemorrhoidal effect of Martynia annua and Tephrosia purpurea extracts in rats. Aerial parts of Tephrosia purpurea and leaves of Martynia annua were selected for extraction with petroleum ether and ethanol. Flavonoid-rich extracts were tested for anti-inflammatory and anti-hemorrhoidal activities (200 and 300 mg/kg bwt.). The anti-inflammatory effect was investigated on Carrageenan and histamine-induced paw edema models by measuring percent inhibition of paw edema at different time intervals. The anti-hemorrhoidal activity was studied by using croton oil-induced hemorrhoid on rats. Effect was assessed by measuring pro-inflammatory mediators in blood, Severity score and Recto Anal Co-efficient and antioxidants level in rectoanal tissues of rats. Results of the study indicate that flavonoid-rich extract of Tephrosia purpurea and Martynia annua significantly inhibited edema in a dose-dependent manner with the treatment of 200 and 300 mg/kg b.wt p.o. in both methods. Both extracts are significantly able to restore pro-inflammatory mediators (TNF-α, IL-6 and PGE2) near normal level. Both, flavonoid-rich extracts treated group also maintained Severity score and rectoanal coefficient (0.268 ± 0.08 and 0.405 ± 0.11) near to the normal control group of animals. MDA level was found statistically significant (p is less than 0.001) decreased after five days of treatment. The tissue antioxidant level is very close to the normal level after treatment with both flavonoid-rich extracts. The present study concluded that the anti-inflammatory and anti-hemorrhoidal effect of flavonoid-rich extracts of Martynia annua and Tephrosia purpurea could be due to the presence of major flavonoid components, namely quercetin and luteolin in both plants. 2020-03-30T00:00:00+02:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9514 Design and Evaluation of Gastro-retentive Drug Delivery System for Glimepiride using Design of Experiment 2022-05-31T17:28:41+02:00 Anil K Sharma [email protected] Aseem Kumar [email protected] Rohit Dutt [email protected] Glimepiride, oral sulfonyl urea, BCS class-II drug is used to treat diabetes (type-II). Due to its low solubility, it is an ideal candidate for solubility enhancement, leading to better bioavailability and subsequent dose. In the present study, the solid dispersion technique was used to improve the solubility using solvent evaporation method. The solid dispersions were prepared using affnisol 912 as a solubility enhancer. The prepared solid dispersions were evaluated for solubility in 0.1N HCl pH 1.2 and phosphate buffer pH 7.8 medium. The solubility of glimepiride in optimized solid dispersion (SD1) formulation was 682.44 µg/mL compared to 6.88 µg/mL for pure drug in pH 7.8 medium. The solid dispersion (SD1) was further formulated into the tablets. The gastro-retentive and mucoadhesive properties were contributed to the tablets by HPMC K4M and Carbopol 940, respectively. Factorial design (Central composite design) was used to optimize the gastro-retentive tablets. The tablet formulations showed good mucoadhesive properties and drug release up to 12 hours in pH 1.2 with 0.5% SLS medium. The optimized formulation (F2) showed cumulative drug release up to 97.20 ± 0.99% in 12 hours. The drug release kinetics also showed that the drug is release by dissolution and diffusion from the drug matrix. The gastro-retention studies in rabbits also showed the tablets remain within the GIT up to 12 hours as confirmed by x-ray images. 2020-03-30T00:00:00+02:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9515 Quality by Design Enabled Development and Optimization of the Nanoparticulate System of Cabazitaxel 2022-05-31T17:28:41+02:00 Mahesh Paithankar [email protected] Mangesh Bhalekar [email protected] Cabazitaxel (CTX), a novel taxane derivative, has proven effective in many solid tumors. It is also approved in many countries for multiple uses in solid tumors. The current marketed formulation lacks the tumortargeting ability, and its uneven distribution in the body causes toxicity to normal tissues. Further, it is a surfactant (polysorbate 80) based micellar formulation composed of ethanol as a co-solvent to improve the solubility of CTX, which causes severe and life-threatening side effects. Hence, to avoid the problem associated with this conventional CTX formulation, the nanoparticulate drug delivery system of CTX was developed by employing the Quality by Design (QbD) approach. The CTX nanoparticulate system was developed by employing a bottom-up followed by a top-down approach. The size reduction was obtained by High-Pressure Homogenizer (HPH). The formulation optimization was done using QbD approach. Design of experiments (DoE) was used to understand the effect of various formulation and process variables on a dependent variable like particle size distribution. The stabilizer concentration, concentration of solubilizer, HPH pressure, and passes were selected as independent factors while particle size distribution was selected as a dependent factor for evaluation. The nanoparticulate system was developed using PEG-400 as solubilizing agents, while Soya Phosphatidylcholine (SPC) was used as a surface stabilizer. Response surface plots revealed a decrease in particle size with increasing concentration of SPC and PEG 400. Similarly, a decrease in particle size with increased HPH passes and pressure was found. The optimum concentrations of SPC and PEG 400 were found to be 20% and 2.5%, respectively. 20 KPSI pressure and 5 HPH passes were derived as optimized processing parameters from DoE. The optimized formulation had a size of 43.5 nm, with PDI is less than 0.4. Due to its narrow particle size distribution, the formulation did not show any increase in particle size or aggregation up to 24 hours. The present research confirms the feasibility of developing the nanoparticulate system of CTX using the bottom-up followed by the top-down technique. The formulation was systematically optimized using QbD approach. The optimum concentration of PEG 400 as solubilizer and concentration of SPC as stabilizer was obtained from DoE, yielding optimum particle size and stability 2020-03-30T00:00:00+02:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9516 Potency of Phytocompounds as Hydroxychavicol and Plumbagin in Combination to Fight Against Leukemia via Activation of MAPKMediated Apoptotic Pathway: An In vitro Approach 2022-05-31T17:28:41+02:00 Snehasikta Swarnakar [email protected]; [email protected] Anirban Manna [email protected]; [email protected] Tapasi Roy [email protected]; [email protected] Tanusree Das [email protected]; [email protected] Santu Bandyopadhyay [email protected]; [email protected] Plants provide natural molecules as an effective agent for phytomedicine. Anticancer properties of natural products are well described. Several studies on hydroxychavicol (HCH), and plumbagin (PLB), which are found in Piper betle leaf and Plumbago sp. respectively, are evidenced as anti-carcinogenic effect on chronic myeloid leukemic (CML) cells through increased reactive oxygen species (ROS). An attempt was taken to determine the efficacy of a new combination of HCH and PLB on CML cells (K562) and the mechanism of apoptosis thereon. 3-{4,5-Dimethylthiazol-2-yl}-2,5-diphenyltetrazolium bromide (MTT) assay was performed to determine the dose for individual and combination treatments of HCH and PLB against leukemic cells, (K562). Apoptotic activity was assessed through flow cytometric analysis with annexin V-FITC/propidium iodide staining. Immunoblots were also performed on cell extracts before and after the treatments. Levels of ROS and nitric oxide (NO) in K562 cells were measured by DCF-DA and DAF-FM staining, respectively. In addition, P38 and JNK siRNA transfection were performed to assess the roles of mitogen-activated protein kinase (MAPK) pathways on apoptosis. Combination treatments of HCH (16 µM) and PLB (0.5 µM) showed synergistic effects on reducing viability and increased cellular apoptosis of K562 cells. Combined treatments showed elevated reactive oxygen species (ROS) and NO levels than individual treatments of HCH and PLB. Moreover, decreasing the ROS generations by antioxidants/ catalase reversed cell deaths and increased viability. Immunoblotting of MAPK pathways components showed reduction of pERK levels, while upregulation pJNK and pP38 levels upon HCH+PLB treatments. Furthermore, silencing of JNK and/or P38 rescued the K562 cells from deaths. The present study indicates combination treatments of HCH and PLB act as a better therapeutic against CML by promoting MAPK-mediated apoptosis via increased oxidative and nitrosative stress. This in vitro approach is the first report describing the mechanism of action of HCH/PLB to fight against Leukemia via interaction with phosphorylated P38. 2020-03-30T00:00:00+02:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9517 Ameliorative Role of Mixed Hydro-methanolic (60:40) Extract of Andrographis paniculata on Chromium (VI)-induced Immunomodulation in Male Albino Rats 2022-05-31T17:28:42+02:00 Sankar K Dey [email protected] Durgapada Dolai [email protected] The immune system controls the body’s homeostatic state and helps to defend against infections. Activation and expansion of many biomolecules are crucial for the homeostatic state. Chromium, a common heavy metal found in nature, is an active in its hexavalent state. The abundant use of chromium in paints, steel plants, intoxicated the workers and modulates their body homeostasis. In this article, we were intended to evaluate the role of Andrographis paniculata Nees extract on restoration of the body homeostatic state in terms of immune system. For the present investigation, a group of male albino rats (80–100 g) were induced by intraperitonial injection of vehicle (0.9% NaCl), Potassium dichromate (K2Cr2O7) (0.8 mg / 100 g body weight / day), K2Cr2O7 plus mixed hydro-methanol solvent extract in the ratio of 60:40 at a dose of 500 mg/kg body weight daily at an interval of six hours after injection of K2Cr2O7 for a period of 28 days. We found that Cr (VI) induces a hyper response of pro-inflammatory cytokines followed by apoptosis in liver and lung tissue. Excess production of reactive oxygen species (ROS) is controlling the whole phenomena. The A. paniculata Nees extract successively inhibit the ROS generation, as a result a significant quenching of pro-inflammatory cytokine production was noted. A. paniculata Nees extract prompted decrease amount of ROS and its associated inflammation provoke the cell survival and helps to maintain a homeostatic state of the body 2020-03-30T00:00:00+02:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9518 Case Report Study of an Integrated Treatment Approach in Critical Case of COVID-19 Patient 2022-05-31T17:28:42+02:00 Atul Desai [email protected] Kavita Desai [email protected] Hemshree Desai [email protected] Rutvij Desai [email protected] Chirag Desai [email protected] The world has seen various variants of coronavirus and attempting all the feasible options to combat this pandemic situation. By far, vaccination is the most remarkable approach in controlling the Pandemic. India is fighting against the delta variant of the second wave COVID-19. Meanwhile, World Health Organization has already warned about the initial stages of the third wave in all countries. Therefore, on considering the variants of coronavirus, no standard option of care is available to date. In this article, we present a case study on the clinical outcome of the integrated treatment approach in COVID-19 patients suffering from critical conditions. The patient with a history of coronavirus was advised of strict home quarantine and standard treatment of care for 14 days. She was brought to the COVID-19 healthcare center in an unconscious state by her family. On examination, she had a 79% oxygen saturation, heart rate 88 beats/minute and her laboratory findings: CRP 37.3(mg/dL), ESR 84(mm/hour), D-dimer 793(ng/mL), and RBS 158 mg/d. After receiving consent from her family members, we initiated the integrated treatment approach. It includes T-AYU-HM Premium 600mg, is a herbo-mineral formulation, and Acupen 600 mg thrice a day with modern medicines. By adhering to the treatment, she recovered completely within a one-month duration. Her HRCT report showed a significant reduction in lung involvement with ill-defined low-density ground-glass opacities and atelectatic bands in both lungs. The patient's vitals and laboratory parameters presented striking improvement. This case study provides information about the effect of the integrated treatment approach in critical COVID-19 cases. 2020-03-30T00:00:00+02:00 ##submission.copyrightStatement## https://myresearchjournals.com/index.php/IJPSDR/article/view/9519 Influence of Particle Size and Particle Deposition of Inhaled Medication in Lung Disease: A Comrehensive Review 2022-05-31T17:28:42+02:00 Kiran R Dudhat [email protected], [email protected] Harsha V Patel [email protected], [email protected] Drug particles less than 5 µm have the greatest probability of deposition in the lung, whereas those less than 2 µm tend to be concentrated in the alveoli. A large proportion of particles within the 2-5 μm range are present in the dose released from the inhaled drug, providing a relatively even distribution across the lungs. The efficient need for inhaled therapy highly depends on the essence of the method of drug delivery and the patient's ability to correctly use the system. A large range of inhaler products, each with positive and negative aspects, are on the market. It facilitates the administration of a lower dose; there is a quicker onset of action and less severe side effects. The deposition of the inhaled drug in the lung is dependent on particle size, inhalation technique and the type of inhaler device. Importance of particle size distribution and Particle aerodynamic diameter, Influence of environmental humidity on particle size Particle deposition in the airways, Methods to identify drug deposition in lungs, Physiological factors which affect the therapeutic efficacy of pulmonary delivery drugs. The nano and micro size particles is a mainstay of treatment for a variety of pulmonary diseases because they provide a platform to deliver drugs directly reliably and inexpensively to the disease site, thus allowing for a minimum amount of drug to be used and minimize side effects. 2020-03-30T00:00:00+02:00 ##submission.copyrightStatement##