International Journal of Pharmaceutical Sciences and Drug Research

Permanent URI for this collection

https://imsear.searo.who.int/handle/123456789/234707

Editor: Dr. Kalpesh Gaur

ISSN: 0975-248X

Frequency: Quarterly

Language: English

Open Access Peer-reviewed journal

Web site: https://ijpsdr.com/index.htm

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Now showing 1 - 20 of 339

FORMULATION AND EVALUATION OF NIOSOMAL GEL CONTAINING ACYCLOVIR BY USING DESIGN OF EXPERIMENTS
(MRI Publication Pvt. Ltd., 2024-08) Ramarao, N; Bindu, AVSH; Dharani, D.
The current study aims to design, optimize, and assess the niosomal gel containing acyclovir for topical application. Compatibility analysis was carried out to assess potential interactions, using techniques such as FT-IR spectroscopy and DSC thermal analysis. The niosomal suspension was created, optimized, and assessed using a 32 - factorial design. The overlay plot indicates that the F3 formulation was optimized with a 300:20 tween 80 and cholesterol ratio. The improved niosomal solution has been introduced into a gel made of carbopol and thoroughly analyzed for pH, viscosity, spreadability, and in vitro drug release characteristics. The study results demonstrated that the niosomal gel formulation exhibited a sustained release of acyclovir over a 24-hour period. The drug release data was assessed, and the findings unveiled that the medication release from the gel formulation complies with Korsmeyer peppas model. The optimized formulation's stability was demonstrated at various temperatures. The present investigation suggested that the niosome gel formulation (F3) could be a promising vesicular approach for effectively administering acyclovir via topical application.
Transgenic animals: catalysts in drug discovery
(MRI Publication Pvt. Ltd., 2024-12) Rolla, A; Kondepudi, A; Meesala, BL; Korimelli, S; Krishnan, SA; Jaha, SKK.
Transgenic technologies have fundamentally transformed scientific research by enabling precise genetic modifications with wide-ranging applications across various fields. This review examines the application of transgenic mice across various research domains, including cancer, diabetes, cardiovascular science, neurology, gastrointestinal research, and reproductive science. We explored how these models are important in enhancing the knowledge of complex biological methods, from elucidating pathways of the disease to enhancing the quality of research outcomes in these fields. Key methodologies such as CRISPR-Cas9, TALENs, knock-out, knock-in, microinjection, and embryonic stem (ES) cell transfection are highlighted, with a focus on their impact on experimental results. Additionally, the review addresses the use of various transgenic strains in drug discovery and the challenges associated with transgenic research. By integrating findings from multiple research areas, this review underscores the transformative potential of transgenic technologies and their pivotal role in driving innovation and addressing global challenges.
Investigation of Anti-inflammatory and Antioxidant Activities of Promising 1,4,5-Trisubstituted Pyrazoles Derivatives of Chalcone Ditosylates
(MRI Publication Pvt. Ltd., 2024-08) Kumar, V; Rao, CMMP; Arora, P.
Patients suffering from chronic pain and inflammatory disorders need novel COX-2 inhibitors to be developed with minimum toxicity to the kidneys, heart, and gastrointestinal tract and with excellent anti-inflammatory activity. The current study centers on an array of 1,4,5-trisubstituted pyrazoles produced via the reaction of ditosylates of chalcones with hydrochloride salt of phenylhydrazine. Chalcone was reacted with HTIB to produce a variety of derivatives of ?, ? chalcone ditosylates. Phenylhydrazine hydrochloride treatment of these chalcone ditosylates produced distinct 1,4,5-trisubstituted pyrazoles. The conversion process is mediated by 1,2-aryl migrations. IR, 1NMR, and elemental analysis were used to characterize the compounds after they had been purified by recrystallization. Using ascorbic acid as a reference, the DPPH (1,1-diphenyl-2-picrylhydrazyl) technique was used to assess the compounds' in vitro antioxidant activity. The paw edema technique caused by Carrageenan was utilized to assess the compounds' in vivo anti-inflammatory properties. The standard medication used was diclofenac sodium. A plethysmograph was used to measure the volume of the rats' paws. When compared to the standard, the compounds V5D5PH5 and V7D7PH7 showed modest antioxidant activity. When the synthetic pyrazoles were examined for their in vivo anti-inflammatory properties, substances V4D4PH4 and V7D7PH7 outperformed the reference. Here, we attempted to create new, safe, and effective drugs for the treatment of inflammatory disorders and pain by utilizing synthetic pyrazole moiety derivatives. Simple experimentation is used in the proposed study to improve pharmacological activity and yields. In the near future, chalcone ditosylate derivatives will be a powerful tool for selective modification.
Sodium-Glucose Co-Transporter-2 Inhibitors Act as AMPK Activators and Ameliorate the Depressive Symptoms Induced by Unpredictable Chronic Mild Stress in Mice
(MRI Publication Pvt. Ltd., 2024-08) Vaghela, UP; Tirgar, P; Parmar, G.
Depression is a prevalent disorder of mental health with a highly multifaceted pathogenesis thus finding an effective therapy for it remains a challenge. Depression is associated with downregulation of AMPK signaling pathways and lowers AMP/ATP and ADP/ATP ratios. Brain AMPK pathway malfunction and metabolic imbalances induce depression. The Unpredictable Chronic Mild Stress (UCMS) model was created centered on the predisposition of the stress-associated assumption of depression. SGLT2 inhibitor drugs canagliflozin and remogliflozin enhance brain AMPK signaling, reduce oxidative stress, increase neurotransmitters, and improve metabolism. SGLT2 inhibitor drugs have promising anti-depressant effects. Thus, in this investigation, we examined Sodium-glucose co-transporter-2 inhibitors to ameliorate depression symptoms in mice induced by unpredictable chronic mild stress by improving AMPK signaling. Seven groups of male mice (Swiss albino) were divided into (n=6). The disease groups received different stressors (unpredictable chronic mild stress model) for one week to produce depression, while normal control groups got 0.5% w/v Saline (orally). The standard group received Fluoxetine (10 mg/kg, orally), while the treatment groups were given canagliflozin (15 and 30 mg/kg, orally) and remogliflozin (10 and 30 mg/kg, orally). Behavioral parameters were assessed for induction of depression. Treatment with SGLT2 inhibitors showed significant (p < 0.05) antidepressant effects on behavioral, oxidative stress, neurotransmitter, brain histopathology, and gene expression evaluation of AMPK, mTOR, BNDF, and TNF-? levels. The current study found that SGLT2 inhibitor drugs have the potential to improve the AMPK signaling pathway and alleviate depression.
In vitro antioxidant potential of linolenyl alcohol isolated from Cayratia trifolia L.
(MRI Publication Pvt. Ltd., 2024-08) Meganathan, B; Panagal, M.
Cayratia trifolia, a plant rich in bioactive compounds, has been known for its diverse pharmacological properties, including antioxidant activity. In this study, we focus on linolenyl alcohol, a compound isolated from C. trifolia, and investigate its antioxidant potential through in-vitro analysis. Linolenyl alcohol was extracted from C. trifolia leaves using standard extraction techniques and characterized using spectroscopic methods. The antioxidant activity of linolenyl alcohol was evaluated using well-established antioxidant assays. The results explored the significant antioxidant activity of linolenyl alcohol, with dose-dependent scavenging of free radicals observed in all assays. Overall, our findings highlight the antioxidant potential of linolenic alcohol from C. trifolia, suggesting its utility as a natural antioxidant agent in pharmaceutical and nutraceutical applications. Further investigations are warranted to explore its therapeutic benefits and potential clinical applications.
Printing Health: Revolutionizing Pharmaceuticals through 3D Innovation
(MRI Publication Pvt. Ltd., 2024-12) Gupta, P; Bhati, K; Kajla, D; Baisoya, K; Vats, A; Sinoriya, P.
The influence of additive manufacturing has grown significantly in the last few years because of the rising awareness and need for customized pharmaceuticals, medical instruments, and equipment. With the innovation in three-dimensional printing (3D-Printing) technology providing a broad scope to explore the infinite dimensions in the pharmaceuticals field, 3D items of diverse geometries may be created. Cost-effectiveness and on-demand printing are two significant advantages of printed drugs over traditional drug production, as is the ability to create very complicated and sophisticated dose forms based on individual needs. This article discusses a few 3D printing processes useful for producing pharmaceuticals as well as how they may be applied to creating effective pharmacological and therapeutical dosage forms, demonstrating the viability of this printing technology for routine industrial production processes.The two main pharmaceutical application areas were covered in this article. First, drug delivery systems, including different medications like controlled release solid dosage form, more than one drug in the form of polypills, gastro-floating mechanism of drug, in the form of Oro dispersible drug, and printed microneedles, are the subject that has received the most research. Second, 3D-Printing contributed to the creation of pharmaceutical tools including drug-eluting devices and tools to help chemists dispense medication.
Protective action of leaves of Epipremnum aureum in gastric ulcer prevention induced by ethanol in rats
(MRI Publication Pvt. Ltd., 2024-12) Manasa, S; Cyriac, KS; Jha, DK; Raveena, SR.
The study investigated the gastroprotective effects of Epipremnum aureum leaf extracts against ethanol-induced gastric ulcers in rats. Dosages of 200 mg/kg and 400 mg/kg of the methanolic extract were administered, with omeprazole used as the positive control. The methanol extract significantly protected the gastric mucosa from ethanol-induced damage, suggesting cytoprotective potential. Ethanol exposure led to a decrease in plasma antioxidant enzyme levels and increased lipid peroxidation, indicating oxidative stress. However, rats treated with the higher extract dose (400 mg/kg) and omeprazole showed significant improvements, with increased SOD and CAT levels, reduced lipid peroxidation, and a lower ulcer index compared to the untreated ulcer group. Histopathological analysis revealed severe gastric mucosal damage in the ethanol-only group, while the high-dose extract and omeprazole groups maintained normal gastric architecture with minimal inflammation. These findings suggest that Epipremnum aureum methanolic extract exhibits potent gastroprotective effects, potentially due to its rich phytochemical profile, including flavonoids, tannins, and alkaloids, supporting its use as a natural remedy for gastric ulcers.
Anti-ulcer activity of Trianthema portulacastrum leaves in rats using an experimental ulcer model
(MRI Publication Pvt. Ltd., 2024-12) Bharti, P; Rajashekhar, U; Jha, DK.
Gastric ulcers conditions can lead to severe complications, including bleeding, perforation, and an increased risk of gastric carcinoma. Natural remedies such as Trianthema portulacastrum may help alleviate these issues by boosting antioxidant defenses and reducing inflammation. In this experiment, thirty Wistar Albino rats were assigned to different groups and observed for 16 days. The study design included several treatment approaches for gastric ulcers. The normal control (Untreated) group was received normal saline for 15 days, while the disease control group also received normal saline for the same period. The Standard Treatment group was received Omeprazole (20 mg/kg) over the 15-day duration. The first test drug group received a daily dose of 250 mg/kg of Trianthema portulacastrum extract for 15 days, while the second Test Group received 500 mg/kg of the extract for the same period. All groups, except the normal control, were administered ethanol (1 mL/200 g, p.o.) on the 16th day. Multiple variables including ulcer index, percentage inhibition of ulceration, antioxidant markers (SOD and CAT), and histopathological analysis of the stomachs of treated rats, were assessed. The methanolic extract of Trianthema portulacastrum (METP) demonstrated potential in treating ulcers. In an ethanol-induced ulcer model, the METP increased SOD and CAT levels, essential antioxidant enzymes that neutralize reactive oxygen species, indicating its capacity to alleviate oxidative stress and inflammation. Notably, the higher METP dose (500 mg/kg) significantly elevated SOD levels, approaching those observed in the normal control group. Both the standard drug Omeprazole and METP markedly reduced ulcer severity, count, and index, while also increasing the percentage of inhibition. The METP exhibited dose-dependent anti-ulcer effects, with the 500 mg/kg dose providing substantial protection against ethanol-induced ulcers. Histopathological studies further supported that Trianthema portulacastrum extracts improve mucosal integrity and reduce lesions. Overall, Trianthema portulacastrum shows promising potential for treating gastric ulcers and enhancing overall health.
Antioxidant and cytotoxic effects of Chrozophora rottleri fruit ethanol extract
(MRI Publication Pvt. Ltd., 2024-08) Nagesh, YR; Mahmood, R.
Liver cancer, particularly hepatocellular carcinoma (HCC), occurs from liver cell abnormalities, influenced by factors such viral hepatitis, obesity toxins and drugs. Non-Alcoholic Fatty Liver Disease (NAFLD) exacerbates liver disorders globally, marked by fat accumulation, whereas liver fibrosis raises cancer risk in NAFLD and Alcohol-Induced Liver Disease (ALD). Herbal medicine gains attraction for liver health, offering hepatoprotective benefits. Medicinal plant metabolites, particularly polyphenols, display antioxidative effects, possibly suppressing cancer cell development. This work focuses on evaluating the possible antioxidant and cytotoxic effects of Chrozophora rottleri fruit ethanol extract (CRFEE) using in-vitro experiments. The antioxidant capacity of CRFEE was examined by hydroxyl radical and nitric oxide scavenging experiments. CRFEE revealed considerable scavenging efficacy against both radicals, suppressing hydroxyl radicals by 48.25% with an IC50 of 35.08±1.62 ?g/ml and nitric oxide by 49.35% with an IC50 of 307.44±2.28 ?g/ml. Notably, CRFEE displayed better antioxidant efficiency compared to the standard antioxidant, butylated hydroxyl toluene (BHT), in neutralizing hydroxyl radicals. Additionally, the in-vitro cytotoxicity of Chrozophora rottleri fruit ethanol extract (CRFEE) was examined using the MTT test on HepG-2 cell line cultures. CRFEE had strong detrimental effects on HepG-2 cells, with higher dosages resulting to a major loss in cell viability. The IC50 value for CRFEE was determined 63±0.08?g/mL, suggesting its efficacy in reducing HepG-2 cell proliferation. The results demonstrate substantial antioxidant activity and cytotoxic effects against liver cancer cells (HepG-2 cell line). The bioactive chemicals contained in CRFEE show potential for future pharmaceutical applications, underscoring the relevance of natural-based research in cancer therapy and the necessity for further exploration in vivo.
Evaluation of the anti-psychotic and neuroprotective properties of Bergenia ciliata root extract in rat models
(MRI Publication Pvt. Ltd., 2024-12) Dulal, TR; Jha, DK; Sah, SK; Fathima, M.
Psychosis, a chronic mental illness, can be treated with plants and traditional herbs, which contain phytochemicals and counter oxidants to support body organs and reduce schizophrenia risk. The study aimed to evaluate the anti-psychotic potential of Bergenia ciliata by collecting, authenticating, and preparing a methanolic extract from its roots. Two experimental models were used to simulate psychotic symptoms in rats and assess the extract's influence on movement and activity patterns. The objective parameters included behavioral assessments of stereotypic and locomotor activities to quantify the effects of the extract. Biochemical analysis was conducted on brain tissue homogenates, focusing on glutathione (GSH) estimation, acetylcholinesterase (AchE) activity assay, and TNF-? measurement to evaluate inflammation levels. Histopathological analysis of the brain, particularly the frontal cortex and hippocampus, was also conducted to examine structural changes in brain tissues. Key observations: This analysis provided insights into the neuroprotective effects of the methanolic root extract on critical brain regions implicated in psychotic disorders. The results showed that the apomorphine control group had high stereotypy levels, while the apomorphine + standard drug group showed a significant reduction in stereotypy scores at 60 and 90 minutes. Both dosages of Bergenia ciliata showed significant reductions in stereotypy scores at 60 and 90 minutes, suggesting its potential in mitigating the stereotypy induced by apomorphine. The study also found significant differences in GSH, AchE, and TNF-alpha levels between the normal control (vehicle) and Apomorphine 1.5 mg/kg, the std drug (Haloperidol 1 mg/kg), and Bergenia ciliata (250 and 500 mg/kg). Recordings in an Actophotometer were taken on Days 1, 8, 15, and 23. The data revealed no significant differences between groups, except for the positive control, this exhibited a significant decrease in comparison to the healthy animals, a notable increase in locomotor activity was observed following the administration of diazepam in the B. ciliata group, particularly when contrasted with the positive control group. Additionally, B. ciliata exhibited significant effects on biochemical parameters compared to the positive control. The histology of the brain's cerebellar cortex, hippocampus, and frontal cortex under different conditions showed well-preserved layers and healthy neurons. Diazepam-treated brain showed mild neuronal degeneration with vacuolations and congested blood vessels. Oligodendrocytes and pyramidal cells were less affected, but some neuronal degeneration was evident. Both low and high doses of the test drug maintained normal cortical and hippocampal structure, with healthy neuronal architecture, oligodendrocyte presence, and adequate vascularization. The study suggests that Bergenia ciliata may be an effective anti-psychotic agent, potentially reducing inflammation and enhancing psychotropic effects.
Development, validation and greenness assessment of stability indicating RP-HPLC method for simultaneous quantification of dapagliflozin and metoprolol succinate in synthetic mixture
(MRI Publication Pvt. Ltd., 2024-12) Rathod, S; Shah, A; Patel, N.
A novel, rapid, accurate, precise and simple stability indicating RP-HPLC method has been proposed and validated for the concurrent quantitation of Dapagliflozin and Metoprolol succinate in laboratory prepared mixture. The greenness assessment of the proposed approach was accomplished utilizing GAPI and AGREE tools. The final chromatographic run was performed utilizing Methanol: 20mM Potassium Dihydrogen Phosphate: (70:30) as eluent, injected at 25°C at a rate of 1.5 mL/min. Cosmosil-MS-5 C18 column (250 mm × 4.6 mm, 5 ?m) was utilised and estimation was done using 223 nm. The APIs were exposed to stress environments (oxidation, acidic and basic hydrolysis, photolysis and thermal stimuli) and stressed samples were analysed under same chromatographic condition. Dapagliflozin and metoprolol succinate had retention times of 11.6 and 2.6 minutes, correspondingly. It was demonstrated having linearity within 10-30 µg/mL for Dapagliflozin and 50–150 µg/mL for Metoprolol succinate. The % accuracy for Dapagliflozin were in the range of 99.01 - 100.56 %, while for Metoprolol succinate it was within 99.32 - 101.41 % at three levels. The outcomes for precision study were within the limits. For Dapagliflozin, the LOD and LOQ were 0.49 µg/mL and 0.59 µg/mL correspondingly and for Metoprolol succinate, values were 1.48 µg/mL and 1.79 µg/mL correspondingly. The approach is effectively suggested for stability-indicating research as well as for routine estimation of Dapagliflozin and Metoprolol succinate in bulk and laboratory prepared mixture. Furthermore, AGREE and GAPI outcomes confirmed the developed approach’s eco–friendliness and greenness.
Quercetin Ameliorated Diabetic Stress through Upregulation of Antioxidant Enzymes and the Nrf-2/HO-1 Axis in the Spleen of Mice
(MRI Publication Pvt. Ltd., 2024-12) Sarma, S; Kashyap, A; Chakrabarti, A; Singh, SS.
Diabetes is the enduring endocrine complications increasing with tremendous challenges all over the world. Quercetin, being the predominant flavonoids has pentahydroxy polyphenolic structure that bears antioxidant activity. Our study assessed the efficacy of quercetin in mice against diabetes caused oxidative stress by modifying the radical quencher, the body’s antioxidants and their regulator-Nrf-2 and HO-1. Hyperglycemia attributes significantly (p<0.01) raised levels of lipid peroxidation, lowered levels of catalase, GSH, SOD, higher intracellular ROS generation and suppressed Nrf-2/HO-1 reactivity in studied organ (spleen). Quercetin minimizes the sugar level significantly(p<0.01) in blood, causes restoration of altered spleen and body weight, also bring down the lipid peroxide level significantly (p<0.01) and further enhanced SOD, catalase, GSH antioxidant levels. Both splenic & peritoneal macrophages revealed lower intracellular ROS generation. Quercetin uplifted the reactivity of Nrf-2 & HO-1. Study’s outcome showed that quercetin supplementation attenuated diabetes-caused oxidative stress through upregulation of antioxidant enzymes activity and Nrf-2 and its regulated gene-HO-1 in immune organ-spleen. Thus, quercetin might be fruitful in reducing the ROS-mediated damage in diabetic individuals.
Salutary effect of Commelina benghalensis (Linn.) aerial parts on streptozotocin induced diabetes linked complications in rat: Effective extract selection study
(MRI Publication Pvt. Ltd., 2024-12) Das, S; Pal, D; Singharoy, S; Lohar, P; Hazra, S; Ghosh, D.
The experiment was designed to identify the most effective extract of Commelina benghalensis aerial parts for the rectification of carbohydrate metabolic disorder, oxidative stress and hyperlipidemia in streptozotocin-induced diabetic rats, developed with a single intramuscular injection of streptozotocin (4 mg/0.1 M citrate buffer/0.1 kg body weight). Diabetic rats were treated with 0.02 g of hydro-methanol (60:40) or hydro-ethanol (60:40) or aqueous extract orally per 0.1 kg body weight in 0.5 ml distilled water for 28 days and sacrificed on 29th day. Glycemic sensors levels, carbohydrate metabolizing enzyme activities, lipid profile, oxidative stress, toxicity markers, and pancreatic histological changes were assessed using standard protocols. Treatment with mentioned extracts of Commelina benghalensis significantly (p<0.05) improved body weight, fasting blood glucose, serum insulin, lipid profile, and carbohydrate metabolic enzyme kinetics in the liver, kidney and skeletal muscle in treated groups compared to untreated diabetic control group. Additionally, treatment of said extracts of Commelina benghalensis significantly restored (p<0.05) the levels of oxidative stress sensors and pancreatic histology towards untreated control group. Among the extracts, hydro-ethanolic extract showed highest efficacy for rectifying glycemic status, lipid profile, and oxidative stress condition for developing a safe, affordable and multi-targeted anti-diabetic herbal drug.
To examine the potential effectiveness of Psidium guajava in Letrozole induced polycystic ovarian syndrome in female albino rats
(MRI Publication Pvt. Ltd., 2024-12) Shree, RR; Jha, DK.
Polycystic ovarian syndrome (PCOS) is a common endocrine disorder characterized by hormonal imbalances, metabolic disturbances, and ovarian dysfunction. This study aimed to investigate the therapeutic potential of methanol extract from Psidium guajava leaves as a natural remedy for alleviating PCOS symptoms in female albino rats. The experimental approach involved assessing critical physiological and biochemical markers both before and after treatment, including body weight, blood levels of testosterone, luteinizing hormone (LH), and follicle-stimulating hormone (FSH), ovarian weight, and the FSH/LH ratio. Anti-inflammatory effects were evaluated by measuring inflammatory markers like TNF-? and lipid-derived mediators. Furthermore, a histological analysis of ovarian tissue was performed to observe changes in follicular development and ovarian structure. The results showed that Psidium guajava treatment significantly improved hormonal profiles, reduced inflammation markers, and promoted the regeneration and maturation of ovarian follicles, counteracting hyperandrogenism and inflammation associated with PCOS. These findings suggest that Psidium guajava leaf extract could be a promising adjunct therapy for managing PCOS, supporting endocrine balance, ovarian health, and inflammation reduction. However, further studies are needed to understand the underlying mechanisms and long-term effects of this botanical treatment.
Spectroscopic Elucidation and Anticancer Potential of 7-methoxy-2-(4-methoxyphenyl)-5-O-glycosyl chromenone Isolated from Haplanthodes tentaculatus (L.) R. B. Majumdar
(MRI Publication Pvt. Ltd., 2024-12) Trivedi, PB; Badole, MR.
In this research, we report on the isolation and structural elucidation of a new flavonoid glycoside called 7-methoxy-2-(4-methoxyphenyl)-5-O-glycosyl chromenone. This flavonoid glycoside was obtained from Haplanthodes tentaculatus, a plant that is native to the Western Ghats of India. The molecule was purified via the use of chromatographic procedures, and its structure was validated by the use of spectroscopic investigations, which included HRMS, 1H NMR, 13C NMR, FTIR, and UV-Visive technologies. With the use of HRMS analysis, the chemical formula C??H??O?? was verified. The isolated molecule demonstrated anticancer activity in vitro against the MDA-MB-231 breast cancer cell line, with an IC?? value of 58.99 ± 0.495 µg/ml. This indicates that the drug is very effective in curing cancer. The natural origin of 7-methoxy-2-(4-methoxyphenyl)-5-O-glycosyl chromenone and the possibility that it has a reduced toxicity level imply that it has the potential to be a lead molecule for the creation of anticancer drugs, despite the fact that it is less effective than the conventional medicine Cisplatin. The findings of this research add to the increasing body of evidence that bioactive chemicals derived from natural sources have the potential to be used in therapeutic medicine.
The clinical efficacy of integrating dolutegravir into the conventional therapeutic regimen for HIV management
(MRI Publication Pvt. Ltd., 2024-12) Doke, N; Hajgude, S; Dhande, A; Tole, S; Gunjegaonkar, S; Joshi, A.
This study investigates the efficacy of transitioning from Tenofovir/Lamivudine/Efavirenz (TLE) to Tenofovir/ Lamivudine/ Dolutegravir (TLD) as a first-line antiretroviral therapy for the management of HIV. A retrospective analysis was conducted involving 261 individuals in whom 145 patients were initially treated with TLE in 2017 who were transitioned to TLD in 2020 and 116 patients were given TLD as first-line therapy from 2020 onwards. Clinical parameters like viral load (VL), CD4 cell count, and WHO clinical stage were evaluated at baseline to study the effectiveness of the treatment. In addition, the non- clinical variables like age, sex, weight, mode of transmission and body mass index (BMI) were analyzed. The results signified enhancements in CD4 count, viral load and weight across both groups (TLE to TLD transition and TLD initiated as first-line therapy) with a statistical significance of p < 0.001***. The median BMI for patients transitioning from TLE to TLD was 21.63 (IQR 19.62-24.37) with a p-value of 0.004**, while the median BMI for patients on TLD as a first-line therapy was 20.83 (IQR 18.95-23.87), exhibiting a p-value of 0.115ns indicating no substantial difference between both groups. The findings showed effective viral suppression, with viral loads categorized as target not detected (TND) and CD4 counts exceeding 500 cells/mm3. Overall, the integration of TLD into the ART regimen resulted in improved clinical outcomes and sustained viral suppression among the patients showing the advantage of this therapeutic transition in HIV management.
Identification of Degradation Pathway of Bilastine and Montelukast by LC/MS
(MRI Publication Pvt. Ltd., 2024-12) Markanday, D; Sharma, CK.
It is necessary for a dosage form to maintain their chemical, physical, microbiological and toxicological stability during their entire shelf life. Knowing the intrinsic stability of the chemical and the breakdown pathway of the dosage form is crucial for this reason. We have developed a straightforward analytical approach using HPLC-UV/MS for the simultaneous measurement of Bilastine and Montelukast, as well as the identification of their degradants in tablet formulation. This method is specific, linear, accurate, and robust. The narcotic compounds were broken down one by one. The Zorbax XDB C-18 column (150*4.6) mm, 5µ, with a mobile phase of Water:Acetonitrile:Formic acid (50:50:1), was used to achieve the separation. A flow rate of 1 ml/min was used with an injection volume of 20 µl. A UV-Vis Spectrophotometer was used for peak detection, while a mass spectrophotometer was employed for identification. Bilastine had a retention time of 3.22 minutes and Montelukast of 4.80 minutes. Proposed method was stability indicating, specific, linear, accurate and robust. The degradation pathway was established for Bilastine and Montelukast by studying their degradation in various stress conditions. The Bilastine was found stable in Photolytic and thermal degradation while there was degradation observed in Montelukast in all stress conditions.
Fabrication and Optimization of Glibenclamide Drug Delivery System Using Pulsatile Approach for Hyperglycemia
(MRI Publication Pvt. Ltd., 2024-12) Desai, S; Thakkar, V; Gandhi, T; Gandhi, A; Parekh, K; Joshi, A.
Diabetes mellitus is characterized by persistently high blood sugar levels, and Glibenclamide is commonly used to manage these levels. Pulsatile formulations of Glibenclamide offer controlled timed release to address early morning hyperglycemia, enhancing glucose management and reducing complications. Incorporating Aloe barbadensis miller spray-dried powder as a solid plug in the pulsatile capsule design may help control morning glucose spikes and reduce elevated triglyceride levels in diabetic patients. The present study utilized the Pulsincap® system, which incorporates ethyl cellulose (EC)--coated capsules containing optimized glibenclamide tablets and a swellable plug. Solid dispersions (SDs) were developed using Soluplus® to enhance the poor aqueous solubility of glibenclamide, with compatibility confirmed via Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). Capsules (size ‘000’), coated with 10% w/v ethyl cellulose in methanol and dibutyl phthalate solution, achieved sustained release over 12 hrs. Immediate-release (IR) tablets, formulated via wet granulation, exhibited rapid disintegration within 2 mins. Sustained-release (SR) tablets, optimized using a 3² full factorial design with varying concentrations of HPMC K4M and HPMC K100M CR, demonstrated release profiles of 16-37% at 1 hr, 33-74% at 4 hrs, and 44-100% at 8 hrs. The erodible plug, composed of HPMC K15M, guar gum, and aloe vera, provided swelling and controlled lag times ranging from 7 to 12 hrs. The pulsatile delivery system effectively enhanced glibenclamide bioavailability and modulated its release, offering potential improvements in glycemic management for diabetic patients.
Spinal Muscular Atrophy: A Systematic Review of Diagnosis, Treatment and Emerging Research
(MRI Publication Pvt. Ltd., 2024-10) Baraka, BBH; Porwal, M; Kannur, S; Pandey, A; Khan, A.
This systematic review aims at understanding the causes, consequences and therapy of spinal muscular atrophy, which is an inheritable illness which can be fatal at times. Although spinal muscular atrophy is incurable, various drugs have been developed to ameliorate the disease condition and this article aims at understanding the effect of all the available synthetic drugs on Spinal muscular atrophy (SMA). A search plan was curated using various databases like, PubMed, Google Scholar and Science Direct. Authors selected publications of Risdiplam, Onasemnogene abeparvovec and Nusinersen, and even studies comparing the drugs with one another, including studies related to drugs like hydroxyurea, phenylbutyrate and gabapentin. 40 publications were identified and finalized based on preferences. All the 3 approved drugs improved motor milestones in SMA patients as compared to natural cohort of the disease. Although Gene replacement therapy observed tremendous results, further investigations is needed to be done. Other drugs like hydroxyurea (HU), Gabapentin, Valproic acid and phenylbutyrate showed significant, little and no effect respectively. All 3 drugs showed significant outcomes and were safe and effective in the longer duration of use. Hydroxyurea and Valproic acid showed slight improvement whereas Gabapentin and Phenylbutyrate had no effect.
Citrullus lanatus (Thunb) improves an antidepressant-induced impaired fertility in depressed male mouse model
(MRI Publication Pvt. Ltd., 2024-12) Kumar, S; Tripathi, A; Singh, P.
Synthetic antidepressants are used in the treatment of mental illness, however due to their side effects people are orienting towards the herbal product as an alternative therapy. The present study therefore, explores the role of C. lanatus (CL) seed extract in evaluating the fluoxetine-induced impaired sperm functions, and fertility of the depressed mice. Adult Swiss strain male mice were separated into six group. Every group contains six animals. Group I received vehicle-treated negative control while Groups II, III, IV, V and VI administered with reserpine (RES) at dose of 0.75 mg/kgBW/day, for 14 days to induce depression, fluoxetine (FLX) at the dose of 40 mg/kgBW/day in depressed mice (positive control) for 28 days, CL seed extract (300 mg/kgBW/day) only, in normal mice, and co-administrations of FLX (40 mg/kgBW/day) with low and high doses of seed extract of CL (150 mg/kgBW/day and 300 mg/kgBW/day) respectively, in the depressed mice for the same duration. Mice of Gr. II and Gr. IV did not alter the epididymal sperm parameters and fertility. However, significant alterations were observed in such parameters in the mice of Gr. III. Partial to complete restorations were noticed in such parameters in Gr. V and VI, as compared to the positive control of Gr. III. The findings suggest that CL seed extract may emerge as a potential herbal remedy to impaired fertility which could be of therapeutic drug in future.

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