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Pharmaceutical Sciences and Drug Design

Volume 3 (2023)

Taxol (Paclitaxel): A Promising Alkaloid for Cancer Treatment
Downloads: 26
Views: 357
Written by Anna Maria Barbuti   Published on Vol 3 , 2023
Taxol, derived from the plant alkaloid paclitaxel, is a prominent anticancer agent. It acts by inhibiting microtubule formation and preventing cancer cell division. The intravenous administration of Taxol has been well established, particularly in the treatment of solid tumors. However, prolonged use of the drug often leads to reduced efficacy due to the emergence of resistance in cancer cells. Furthermore, the side effects of Taxol can vary depending on individual factors such as age, genetics,
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Protective Effects of Resveratrol and Gamma-Glutamylcysteine in Azathioprine-Induced Hepatotoxicity
Downloads: 35
Views: 164
Written by Huda Sultan Almutairi   Published on Vol 3 , 2023
The objective of this study was to evaluate the hepatoprotective effects of resveratrol (RSV) and gamma-glutamylcysteine (γ-GC) against liver damage induced by azathioprine (AZA), with potential implications for combining these compounds with immunosuppressive therapies. The study lasted for 4 weeks and included 50 male Wistar albino rats divided into five groups: a control group treated with normal saline, an AZA group given AZA at 10 mg/kg orally, an RSV group treated with both AZA and RSV (8
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Enhancing the Dissolution Rate of Dolutegravir Sodium Using Nanosuspension Technology and a 32 Factorial Design
Downloads: 45
Views: 344
Written by Bing Xie   Published on Vol 3 , 2023
Dolutegravir sodium is an effective antiretroviral medication used for the treatment of HIV. The drug is classified as BCS class II, indicating its low solubility at the typical gastric pH. The purpose of this research was to identify and optimize the key operational and formulation factors affecting the drug’s properties, using a 32-factorial design. Nanosuspensions were prepared using PVP K30, polyvinyl alcohol, polxammer 407, and polxammer 188. The study focused on polymer concentration as th
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An Overview of New Acetamide Derivatives in COX-II Inhibitors
Downloads: 35
Views: 298
Written by Karam S. Atrushi   Published on Vol 3 , 2023
Non-steroidal anti-inflammatory drugs (NSAIDs) have long been recognized as one of the most commonly used agents. However, their adverse effects on various organs are well-documented. This review focuses on the development of acetamide derivatives that retain their anti-inflammatory effects while selectively inhibiting COX-II. Several literature sources emphasize the importance of these heterocyclic compounds in the treatment of inflammatory conditions, recognizing their therapeutic value in thi
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UV-Spectrophotometric Method Development and Validation for Quantifying Dapagliflozin in Bulk and Pharmaceutical Formulations
Downloads: 88
Views: 606
Written by Saipranavi Vadla   Published on Vol 3 , 2023
This research focused on establishing a new and highly sensitive UV-spectrophotometric approach for quantifying dapagliflozin in tablet dosage form while ensuring comprehensive validation of analytical parameters following ICH guidelines. The maximum absorbance (λmax) of dapagliflozin was identified at 220 nm using a UV-Vis spectrophotometer equipped with a 1 cm quartz cell. A stock solution of 1000 μg/ml was prepared using a solvent system consisting of methanol and water in a ratio of 15:85, a
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UV-Spectrophotometric Analysis of Diazepam Using Calibration Curve and Reference Standard Methods
Downloads: 48
Views: 444
Written by Dobrina Tsvetkova   Published on Vol 3 , 2023
This study aimed to evaluate the method of the calibration curve (MCC) and the external reference standard method (MRS) to assess the accuracy and precision to validate the UV-spectrophotometric technique for quantifying diazepam at λmax = 328 nm in 95% ethanol. Selectivity was confirmed by the absence of absorbance at λmax = 328 nm in the UV spectrum of the blank solution, whereas this wavelength was distinctly observed for diazepam. The experimental data were analyzed using linear regression,
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Composition and Potential Applications of Biologically Active Complexes from Natural Raw Materials
Downloads: 32
Views: 246
Written by Poznyakovsky Valeriy Mikhailovich   Published on Vol 3 , 2023
This research explores a novel approach to enhance the absorption of biologically active compounds with poor bioavailability by combining partially soluble arabinogalactan polysaccharides with chitosan-based polysaccharides. The study focuses on a bioactive polymer matrix composed of chitosan succinate, succinic anhydride, and arabinogalactan with covalently unbound dihydroquercetin, with respective weight proportions of 3.0-5.0, 2.0-4.0, 15.0-20.0, and 3.0-5.0. These elements act as specialized
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Limited Predictive Performance of Existing Amisulpride PopPK Models: External Validation and Proposal of Model-Based Remedial Regimens for Non-Adherence
Downloads: 20
Views: 69
Written by Thabo Nkosi   Published on Vol 3 , 2023
This work sought to assess how well previously published population pharmacokinetic (PopPK) models of amisulpride perform in individuals with schizophrenia using an independent dataset, and to design dosing adjustments suitable for patients who miss or delay their amisulpride doses. A comprehensive literature search of PubMed, Embase, and Web of Science was used to collect PopPK models for comparison. A total of 390 serum samples from 361 hospitalized Chinese adults diagnosed with schizophrenia
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Xiaoyao Sanjie Decoction Suppresses Triple-Negative Breast Cancer through Quercetin-Mediated Inhibition of EZH2/AKT1: Insights from Network Pharmacology and In Vivo Validation
Downloads: 30
Views: 64
Written by Julian Gray   Published on Vol 3 , 2023
Triple-negative breast cancer (TNBC) is an aggressive subtype of breast cancer with high mortality, representing a serious challenge to women’s health worldwide. Xiaoyao Sanjie Decoction (XYSJD) has shown promising anti-TNBC effects, yet the molecular mechanisms behind its therapeutic activity remain largely unexplored. This study aimed to investigate the efficacy of XYSJD and its active compound quercetin in TNBC and to elucidate the underlying mechanisms of action. The chemical composition of
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Repositioning Nitrofurantoin for Breast Cancer Treatment Using Cubosome-Based Delivery Systems
Downloads: 32
Views: 66
Written by Emma Wright   Published on Vol 3 , 2023
Nitrofurantoin (NITRO), a well-established antibiotic for urinary tract infections, is activated by nitroreductases, a mechanism that has prompted its investigation for repurposing in breast cancer treatment, as these cancers express the nitroreductase gene.NITRO-loaded cubosomes were prepared via hot homogenization following a 2³ full factorial design. Variables examined included the drug-to-oil phase ratio (1:10 and 2:10), oil-to-aqueous phase ratio (1:10 and 1:5), and Glyceryl mono-oleate (GM
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Systems-Based Metabolomics and Network Pharmacology Reveal MAOA-Dependent Anti-Ferroptotic Mechanisms of Curcumin in Acute Kidney Injury
Downloads: 29
Views: 92
Written by Katerina Dimitrova   Published on Vol 3 , 2023
Acute kidney injury (AKI) remains a major global health concern due to its considerable morbidity and mortality. Increasing evidence points to ferroptosis as a dominant pathological process in AKI, and suppression of monoamine oxidase A (MAOA) as well as 5-hydroxytryptamine signaling has been linked to protection against this form of cell death. Curcumin (Cur), the principal polyphenolic constituent of Curcuma longa, has shown renal protective activity in AKI models, yet the molecular basis thro
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Population Pharmacokinetics of Sirolimus in Adult Liver Transplant Recipients: Hematocrit-Guided Dosing Recommendations from a Large Cohort
Downloads: 26
Views: 98
Written by Elena Russo   Published on Vol 3 , 2023
Sirolimus is widely prescribed as an immunosuppressive agent following solid organ transplantation. Its therapeutic index is narrow and exposure is highly inconsistent across individuals, highlighting the need to clarify the contributors to this variability and create patient-specific dosing strategies. This work sought to conduct a population pharmacokinetic (PK) evaluation of sirolimus in adult recipients of liver transplants and to formulate dosage recommendations tailored to patient-level ch
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Neonatal Umbilical Artery pH Following Position-Specific Metaraminol Infusion During Elective Caesarean Delivery: A Randomised Noninferiority Trial
Downloads: 20
Views: 95
Written by Luka Petrov   Published on Vol 3 , 2023
The standard 15° left tilt during cesarean delivery has long been recommended, but its actual clinical benefit has been questioned in recent studies. We investigated whether starting metaraminol at a higher dose in the supine position could maintain neonatal umbilical arterial pH as effectively as the conventional left tilt approach. A total of 124 healthy women scheduled for elective cesarean delivery were randomly assigned to either a supine position (n = 62) or 15° left tilt (n = 62) followin
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Ciprofol Mitigates Myocardial Ischemia/Reperfusion Injury by Suppressing Ferroptosis via HIF-1α Upregulation
Downloads: 27
Views: 80
Written by Evelyn Mitchell   Published on Vol 3 , 2023
Ciprofol, a recently developed intravenous anesthetic, is increasingly utilized in anesthesia and sedation. While prior research has shown its potential to alleviate cerebral ischemia/reperfusion (I/R) injury by reducing oxidative stress and inflammation, its cardioprotective effects and underlying mechanisms remain unexplored. This study investigated whether ciprofol mitigates myocardial I/R injury by modulating ferroptosis. Myocardial I/R injury was induced in mice by 30 minutes of ischemia fo
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Mechanistic Insights into Radix Paeoniae Rubra and Radix Angelicae Sinensis Granules for Diabetes-Induced Erectile Dysfunction Using Network Pharmacology and In Vivo Studies
Downloads: 25
Views: 88
Written by Charlotte Reed   Published on Vol 3 , 2023
Diabetes mellitus-induced erectile dysfunction (DMED) remains a challenging condition without effective targeted therapies. This study aimed to explore the potential mechanisms and molecular targets of Radix Paeoniae Rubra and Radix Angelicae Sinensis Granules (RAG) in DMED using a combination of network pharmacology and experimental validation. Active compounds of RAG and their predicted targets were retrieved from the Traditional Chinese Medicine Systems Pharmacology Database (TCMSP). DMED-rel
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Population Pharmacokinetic Analysis of Factors Influencing Vancomycin Trough Levels in Non-Critical Care Patients in Saudi Arabia
Downloads: 25
Views: 105
Written by Matej Novak   Published on Vol 3 , 2023
Vancomycin is a primary therapy for methicillin-resistant Staphylococcus aureus infections, but its pharmacokinetics show considerable variability, particularly among older adults. Data on factors affecting vancomycin pharmacokinetics in Saudi adult patients are scarce. This study aimed to develop a population pharmacokinetic (Pop-PK) model for vancomycin in medical ward patients and to identify patient-specific factors influencing trough concentrations.We conducted a retrospective multicenter s
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Prolonged Corneal Analgesia Without Impairing Wound Healing Using a Novel Quaternary Ammonium N-Propylamiodarone Bromide
Downloads: 29
Views: 67
Written by Isabella Rivera   Published on Vol 3 , 2023
Pain originating from corneal epithelial damage is a prevalent and distressing symptom caused by factors such as mechanical trauma, chemical exposure, ulceration, UV irradiation, or infection. Despite its frequency, effective and long-lasting treatments remain limited. This study evaluated a newly synthesized quaternary ammonium compound, N-propylamiodarone bromide (NPA), for its ability to provide prolonged corneal analgesia via selective entry through transient receptor potential vanilloid 1 (
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A Binary Nanoparticle Drug-Delivery System for Leukemia Therapy: Daunorubicin- and Luteolin-Coloaded Nanoparticles Decorated with Aptamer and Transferrin
Downloads: 24
Views: 64
Written by Noah Hughes   Published on Vol 3 , 2023
This study focused on developing a dual-targeted nanodrug-delivery system functionalized with aptamers (APs) and transferrin (Tf) and co-loaded with daunorubicin (Drn) and luteolin (Lut) for leukemia therapy.AP- and Tf-containing oligonucleotide ligands were individually synthesized. Nanoparticles loaded with Drn and decorated with APs (AP-Drn NPs) and Lut-loaded Tf-functionalized NPs (Tf-Lut NPs) were prepared via self-assembly. These were then combined to form a dual-ligand, dual-drug nanodrug
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Role of OmpH in Cec4-Mediated Reduction of Acinetobacter baumannii Biofilm
Downloads: 26
Views: 105
Written by Ricardo Pinto   Published on Vol 3 , 2023
The rise of carbapenem-resistant Acinetobacter baumannii (CRAB) presents significant challenges in clinical management and has been identified by the World Health Organization as a priority pathogen requiring new antibiotic strategies. In our previous study, the novel antimicrobial peptide Cec4 demonstrated notable efficacy in reducing clinical CRAB biofilms, yet its underlying mechanism remains unclear. To assess the therapeutic potential of Cec4, it is essential to investigate how it disrupts
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A Network-Based Pharmacologic Analysis Combined With Experimental Confirmation Was Used to Unravel How Compound Huangbai Liquid Exerts Its Therapeutic Actions against Acne
Downloads: 26
Views: 62
Written by Samantha King   Published on Vol 3 , 2023
Acne is a common dermatological condition in which inflammation plays a central role. Compound Huangbai Liquid (CHL), a well-known traditional Chinese medicine (TCM) formulation, has demonstrated notable clinical benefits for acne, yet its mechanistic basis has not been comprehensively clarified using an integrated network pharmacology strategy.We identified the bioactive constituents of CHL and their putative molecular targets using the BATMAN-TCM platform. Acne-associated genes were collected
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Impact of Low-Dose Esketamine Pretreatment on Etomidate-Induced Myoclonus: A Randomized Controlled Trial
Downloads: 24
Views: 73
Written by Laura Schmidt   Published on Vol 3 , 2023
Etomidate is known to trigger myoclonus during the induction of general anesthesia. This study aimed to evaluate whether pretreatment with a low dose of esketamine could reduce the occurrence of etomidate-induced myoclonus.One hundred adult patients scheduled for elective surgeries under general anesthesia were randomly assigned to two groups: the esketamine group (Group E) and the control group (Group C). Group E received 0.15 mg/kg of esketamine, while Group C received an equal volume of norma
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