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Articles 91 - 120 of 1052
Full-Text Articles in Pharmacy and Pharmaceutical Sciences
Hexasodium Fytate (Snf472 Or Csl525) Inhibits Ectopic Calcification In Various Pseudoxanthoma Elasticum And Calcinosis Cutis Animal Models, Miguel Ferrer, Maria Pérez-Ferrer, Marc Blasco, Ida Jacobs, Qiaoli Li, Olivier Vanakker, Lisa Dangreau, Andrea López, Gianluca Malagraba, Firas Bassissi, Joan Perelló, Carolina Salcedo
Hexasodium Fytate (Snf472 Or Csl525) Inhibits Ectopic Calcification In Various Pseudoxanthoma Elasticum And Calcinosis Cutis Animal Models, Miguel Ferrer, Maria Pérez-Ferrer, Marc Blasco, Ida Jacobs, Qiaoli Li, Olivier Vanakker, Lisa Dangreau, Andrea López, Gianluca Malagraba, Firas Bassissi, Joan Perelló, Carolina Salcedo
Department of Biochemistry and Molecular Biology Faculty Papers
Background/Objectives: Ectopic calcification is a pathological condition characterized by the mineralization of soft tissues due to the deposition of calcium phosphate crystals. Hexasodium fytate (CSL525, previously known as SNF472) is a crystallization inhibitor being developed for the treatment of ectopic calcification-related disorders. Our aim was to investigate CSL525 for the treatment of soft-tissue calcification disorders in animal models of pseudoxanthoma elasticum and calcinosis cutis. Methods: In a first study, abcc6-/- zebrafish larvae were exposed to 1 mM CSL525 for 7 days or kept under the same conditions without CSL525, and spinal mineralization was quantified. In a second study, abcc6 …
Preparation And Evaluation Of Mesoporous Celecoxib For Improved Antiarthritic Activity In Rodents, Reena I. Fernandaes, Sayani Bhattacharyya
Preparation And Evaluation Of Mesoporous Celecoxib For Improved Antiarthritic Activity In Rodents, Reena I. Fernandaes, Sayani Bhattacharyya
The Thai Journal of Pharmaceutical Sciences
Background: Celecoxib, a model anti-inflammatory drug, used in the management of arthritis exhibits limited oral bioavailability and slow onset of action due to its poor solubility. Objective: The present study explores a mesoporous drug delivery of celecoxib to investigate the efficacy of its antiarthritic activity in animal models, and develops a low-oral dose therapy. Materials and Methods: The solvent evaporation method was employed for the preparation of mesoporous delivery of celecoxib, using Syloid®, and Neusilin®, at a molar ratio of silica/ drug 1:2.5. The formulations were characterized for drug loading, in vitro drug release, and material …
Enhancing Topical Drug Delivery Of Apremilast Through Niosomal Gel Formulation: Ex Vivo Skin Permeation And In Vivo Evaluation For Psoriasis, Megha Shyam Matlapudi, Anka Rao Areti, Yukti Jaiswal, Veeresh Bantal, Raghavender Medishetti
Enhancing Topical Drug Delivery Of Apremilast Through Niosomal Gel Formulation: Ex Vivo Skin Permeation And In Vivo Evaluation For Psoriasis, Megha Shyam Matlapudi, Anka Rao Areti, Yukti Jaiswal, Veeresh Bantal, Raghavender Medishetti
The Thai Journal of Pharmaceutical Sciences
Background: Psoriasis is a dynamic and chronic disease characterized by inflammatory changes and an increased rate of keratinocyte proliferation leading to the formation of erythematous scleroderma plaques with a silvery sheen. The existing therapies come with shortcomings in terms of effectiveness and leave behind a trail of side effects. Hence, there is a need of alternative therapeutic measures. Objectives: This study aimed to assess the therapeutic potential of Apremilast Niosomal Gel (APR Nio Gel) in treating psoriasis, comparing its effectiveness with conventional gel (APR Gel) and oral suspension (APR Oral) formulations. Materials and Methods: Apremilast niosomes were prepared by thin …
The Design, Construction, And Testing Of Mrna Vaccine Against Equine Herpes Virus, Bhawana Devkota
The Design, Construction, And Testing Of Mrna Vaccine Against Equine Herpes Virus, Bhawana Devkota
LSU Master's Theses
Equine Herpesvirus-1 (EHV 1) is a worldwide significant pathogen that causes respiratory illness, abortion, and neurological disorders in equine. Current vaccines, including live attenuated, inactivated, and subunit platforms, do not prevent viral latency, mucosal shedding, or cross-strain immunity, requiring alternative approaches. To address these gaps, this project explores the design, synthesis, and in vitro testing of an mRNA vaccine targeting immunogenic EHV 1 glycoprotein (gB, gC, gD, gG, and gM). Epitopes were computationally predicted using the Immune Epitope Database (IEDB), codon-optimized for Bos taurus, and cloned into pUCIDT vectors using SP6/T7 promoters. In vitro transcription (IVT) used nucleotide modifications …
Takotsubo Cardiomyopathy: A Case Of The Broken Heart, Lilian Huynh, Kaylee Putney
Takotsubo Cardiomyopathy: A Case Of The Broken Heart, Lilian Huynh, Kaylee Putney
Annual Research Symposium
Takotsubo cardiomyopathy (TC), or "broken heart syndrome," is a rare cardiac condition causing temporary left ventricular dysfunction due to severe stress. Though the exact cause is unclear, it mimics myocardial infarction and can lead to cardiogenic shock. Current treatment lacks specific guidelines and relies on heart failure protocols. We report a case of a patient with TC-induced cardiogenic shock, likely triggered by emotional stress. She required vasopressors, a percutaneous intervention, an Impella device, and guideline-directed medication therapies. This case underscores the significance of establishing guideline optimizations for managing TC and cardiogenic shock.
In-Silico Modeling And Characterization Of Kcc2 Protein Interaction With A Small Molecule Direct Agonist Identifies Potential Binding Sites For Modulating Behaviors Associated With Substances Of Abuse, William Hai Dang Ho, Alfred Amendolara, Kenyon Mitchell, Jaden Miner, Ruth Northcott, Braxton Bingham, Andrew J. Payne
In-Silico Modeling And Characterization Of Kcc2 Protein Interaction With A Small Molecule Direct Agonist Identifies Potential Binding Sites For Modulating Behaviors Associated With Substances Of Abuse, William Hai Dang Ho, Alfred Amendolara, Kenyon Mitchell, Jaden Miner, Ruth Northcott, Braxton Bingham, Andrew J. Payne
Annual Research Symposium
Purpose
KCC2 is a potassium-chloride cotransporter that plays a critical role in neuronal function by regulating GABAergic signaling via chloride gradients. Maintaining this concentration gradient is crucial for balancing excitation and inhibition in the brain. While KCC2 dysregulation has been implicated in epilepsy and seizures, recent studies suggest that KCC2 inhibition results in phenotypes mirroring those seen in chronic opioid dependence. As such, increasing evidence support KCC2 being a potential therapeutic target for modulating behaviors associated with substances of abuse. Currently, only a few direct small molecule agonists against KCC2 have been reported, and no definitive active site on the …
Centella Asiatica: Recent Cosmeceutical Uses For Treatment Of Skin Diseases, Iman I. Soliman, Nouran Medhat, Huda Saleh, Mai El Halawany
Centella Asiatica: Recent Cosmeceutical Uses For Treatment Of Skin Diseases, Iman I. Soliman, Nouran Medhat, Huda Saleh, Mai El Halawany
Bulletin of Faculty of Pharmacy Cairo University
Centella asiatica is one of the well-known herbal species used in traditional medicine across Asia such as India, Indonesia, and China. It had been used as a medicinal plant for hundreds of years. Besides its general pharmacological activities such as neuroprotection, anti-cancer and anti-diabetes. It demonstrated effective dermatological actions as being a potent anti-inflammatory, antioxidant, healing and moisturizing properties. The major constituents responsible for these effects were triterpenoids. Triterpenoids included asciaticoside which was reported to induce collagen synthesis. Madecassoside was known for its wound healing properties. It was well known for its efficiency in improving the treatment of hypertrophic wounds. …
Orchestrating Cytosolic Access: The Partnership Of Cationic Lytic Peptide L17e And Potassium Channel Kca3.1, Keykavous Parang
Orchestrating Cytosolic Access: The Partnership Of Cationic Lytic Peptide L17e And Potassium Channel Kca3.1, Keykavous Parang
Pharmacy Faculty Articles and Research
In this issue of Molecular Therapy, the study by Kuriyama et al.1 represents an advance in the field of intracellular delivery systems by elucidating a novel mechanism for cytosolic delivery mediated by a cationic amphiphilic lytic peptide L17E (IWLTALKFLGKHAAKHEAKQQLSKL-amide). The investigators demonstrate that the peptide achieves cytosolic delivery primarily through transient plasma membrane disruption, bypassing some of the endocytic pathways, and highlight the pivotal role of the calcium-activated potassium channel KCa3.1, encoded by the gene KCNN4, in facilitating this process. These findings offer a deeper understanding of peptide-mediated delivery using a potassium channel and raise intriguing questions about …
Mergers And Acquisitions (M&As) In Pharmaceutical Markets: Associations With Market Concentration, Prices, Drug Quantity Sold, And Shortages, J. Daniel Mcgeeney M.S., Aylin Sertkaya Ph.D., Leah Ross M.A., Fred Ledley M.D., Cody Hyman Ph.D.
Mergers And Acquisitions (M&As) In Pharmaceutical Markets: Associations With Market Concentration, Prices, Drug Quantity Sold, And Shortages, J. Daniel Mcgeeney M.S., Aylin Sertkaya Ph.D., Leah Ross M.A., Fred Ledley M.D., Cody Hyman Ph.D.
CISI Publication
In recent decades, the pharmaceutical industry has become increasingly concentrated in the United States, in part due to mergers and acquisitions (M&As) between drug manufacturers. This consolidation from M&As has been cited as a key factor affecting drug prices and drug shortages (U.S. Federal Trade Commission, 2022). In this study, we assessed trends in pharmaceutical M&As during 2010–2023 and evaluated the characteristics of drugs and companies involved in those M&As. We considered the effects of M&As on market concentration, drug prices, drug quantity sold, and drug shortages. We also considered how these associations vary by drug characteristics, including brand drugs …
Evaluation Of Disulfiram And Derivatives As Antimicrobial Adjuvants, Surya Bhaskar Karuturi
Evaluation Of Disulfiram And Derivatives As Antimicrobial Adjuvants, Surya Bhaskar Karuturi
Theses, Dissertations and Capstones
Disulfiram (Antabuse) is an oral drug used for the treatment of alcohol dependence. Previous studies showed that disulfiram has antibiotic activity on multidrug-resistant bacteria. Here disulfiram was further evaluated for its ability to increase the potency of existing antimicrobials against the bacteria and yeast by acting as a drug adjuvant. Microbial cultures were treated with antibiotic or antifungal drugs in combination with disulfiram and its derivatives to determine whether potency is increased. The structure activity relationship (SAR) of disulfiram analogs was assessed against a triazole resistant Aspergillus panel. It showed that the shorter chained analogs of disulfiram are more potent …
Scaffolds With Spatiotemporally Controlled Growth Factor Delivery And Cyclodextrin-Enabled Antagonism Of Growth Factor Receptor Sequestration Promote Cutaneous Wound Healing, Jelena Marjanovic, Veronica Jurczuk, Lilian Valadares Tose, Yarixa Cintron Diaz, Francisco Fernandez Lima, Beatriz Abdo Abujamra, Sara Danker, Sinan Jabori, Devinder Singh, Jamie L. Burgess, Joshua Tam, Mohamadmahdi Samandari, Rivka C. Stone, Stephen C. Davis, Robert S. Kirsner, Marjana Tomic-Canic, Fotis M. Andreopoulos, Ivan Jozic
Scaffolds With Spatiotemporally Controlled Growth Factor Delivery And Cyclodextrin-Enabled Antagonism Of Growth Factor Receptor Sequestration Promote Cutaneous Wound Healing, Jelena Marjanovic, Veronica Jurczuk, Lilian Valadares Tose, Yarixa Cintron Diaz, Francisco Fernandez Lima, Beatriz Abdo Abujamra, Sara Danker, Sinan Jabori, Devinder Singh, Jamie L. Burgess, Joshua Tam, Mohamadmahdi Samandari, Rivka C. Stone, Stephen C. Davis, Robert S. Kirsner, Marjana Tomic-Canic, Fotis M. Andreopoulos, Ivan Jozic
Mechanical & Aerospace Engineering Faculty Publications
Chronic wounds present a major burden to patients, health care professionals, and health care systems worldwide, yet treatment options remain limited and often ineffective. Although initially promising, growth factor-based therapies displayed limited and underwhelming effectiveness largely due to poor bioavailabilbioity and impaired receptor function within the chronic wound microenvironment. Here we demonstrate that chronic wounds exhibit elevated cholesterol synthesis, which disrupts growth factor signaling by sequestering receptors within lipid rafts. To address this, we developed a novel therapy combining growth factors with cyclodextrin in an ECM-mimetic scaffold, enabling localized cholesterol modulation and improved receptor accessibility. We demonstrate that this approach …
Gramseq-Dta: A Grammar-Based Drug-Target Affinity Prediction Approach Fusing Gene Expression Information, Kasul Debnath, Pratip Rana, Preetam Ghosh
Gramseq-Dta: A Grammar-Based Drug-Target Affinity Prediction Approach Fusing Gene Expression Information, Kasul Debnath, Pratip Rana, Preetam Ghosh
Computer Science Faculty Publications
Drug–target affinity (DTA) prediction is a critical aspect of drug discovery. The meaningful representation of drugs and targets is crucial for accurate prediction. Using 1D string-based representations for drugs and targets is a common approach that has demonstrated good results in drug–target affinity prediction. However, these approach lacks information on the relative position of the atoms and bonds. To address this limitation, graph-based representations have been used to some extent. However, solely considering the structural aspect of drugs and targets may be insufficient for accurate DTA prediction. Integrating the functional aspect of these drugs at the genetic level can enhance …
Magnetic And Ph-Sensitive Dual Actuation Of Biohybrid Microswimmer Of Targeted Drug Release Suitable For Cancer Cell Microenvironment, Richa Chaturvedi, Yumin Kang, Yunji Eom, Sri Ramulu Torati, Cheolgi Kim
Magnetic And Ph-Sensitive Dual Actuation Of Biohybrid Microswimmer Of Targeted Drug Release Suitable For Cancer Cell Microenvironment, Richa Chaturvedi, Yumin Kang, Yunji Eom, Sri Ramulu Torati, Cheolgi Kim
Center for Bioelectronics Publications
The chemotherapeutic agents most frequently used in cancer treatment often have limited effectiveness because of their low specificity for tumors and poor therapeutic performance. In addition to the aforementioned therapeutic challenges the drug delivery carriers conjugated with the drug encounter early detection and elimination from the immune system before arriving at the affected area continues to be a significant research focus among researchers. To address this prevalent issue, an effective approach has been developed that leverages the physiological differences between normal and tumor tissue to enhance the efficacy of anticancer drugs. This drug delivery system is designed based on pH-sensitive …
The Future Of Ai Regulation In Drug Development: A Comparative Analysis, Gabriela Lenarczyk, Timo Minssen, Nicholson Price, Arti Rai
The Future Of Ai Regulation In Drug Development: A Comparative Analysis, Gabriela Lenarczyk, Timo Minssen, Nicholson Price, Arti Rai
Faculty Scholarship
As artificial intelligence (AI) transforms drug development, regulatory frameworks are evolving to oversee its implementation, particularly at the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA). This paper makes three contributions to understanding emerging regulatory approaches. First, we offer a comparative analysis of how these agencies have responded to AI-driven advances, incorporating new US executive orders and the European Union (EU)’s AI Act. Second, we propose a novel analytical framework to understand regulatory divergence: the FDA’s flexible, dialog-driven model contrasts with the EMA’s structured, risk-tiered approach, reflecting broader institutional and political-economic differences. While the former encourages …
Rwanda's Natural Remedies: A Fresh Look At The Fight Against Malaria, Leandre Nsabimana Ndisanze
Rwanda's Natural Remedies: A Fresh Look At The Fight Against Malaria, Leandre Nsabimana Ndisanze
Pomona Senior Theses
Malaria remains one of the most devastating parasitic diseases globally, disproportionately affecting sub-Saharan Africa, where Rwanda continues to face high transmission rates and rising resistance to conventional interventions. Despite decades of control efforts, the emergence of drug-resistant Plasmodium falciparum and insecticide-resistant Anopheles mosquitoes threatens to reverse recent gains. This research responds to the urgent need for sustainable and culturally relevant alternatives by exploring the therapeutic potential of Rwandan traditional medicinal plants. These indigenous remedies, long used by local healers, offer an underexplored reservoir of bioactive compounds that may provide the basis for novel antimalarial drugs.
The central hypothesis of this …
Folic Acid-Decorated Lipidic Nanocapsules Co-Loaded With Atorvastatin And Curcumin To Enhance Glioma Targeting In Mice, Mahitab Bayoumi, John Youshia, Osama Abdelkawy, Sara Abdelgaber, Mona Arafa, Maha Nasr, Omaima Sammour
Folic Acid-Decorated Lipidic Nanocapsules Co-Loaded With Atorvastatin And Curcumin To Enhance Glioma Targeting In Mice, Mahitab Bayoumi, John Youshia, Osama Abdelkawy, Sara Abdelgaber, Mona Arafa, Maha Nasr, Omaima Sammour
Pharmacy
Background: Glioma remains an intractable and highly aggressive brain tumor, mainly due to the daunting obstacle presented by the blood-brain barrier (BBB). To overcome this challenge and enhance therapeutic efficacy, a dual-drug delivery system was engineered. This system co-encapsulated curcumin, a nutraceutical with multitargeted anticancer potential, with atorvastatin calcium, a repurposed anticancer agent, within lipidic nanocapsules (LNCs). Methods: LNCs were prepared via the phase inversion temperature method and optimized using a Box–Behnken design. The optimized LNCs were subsequently functionalized with folic acid (FA) to enable active targeting. FA-LNCs were characterized using, XPS, TEM, in vitro release, and MTT cytotoxicity …
Targeting Bone In Cancer Therapy: Advances And Challenges Of Bisphosphonate-Based Drug Delivery Systems, Fariba Ganji, Mohammadmahdi Eshaghi, Hossein Shaki, Lobat Tayebi
Targeting Bone In Cancer Therapy: Advances And Challenges Of Bisphosphonate-Based Drug Delivery Systems, Fariba Ganji, Mohammadmahdi Eshaghi, Hossein Shaki, Lobat Tayebi
Electrical & Computer Engineering Faculty Publications
Background and Purpose: Bisphosphonates (BPs) are well-known for their strong affinity toward bone mineral matrices and are widely used to inhibit excessive osteoclast activity associated with various bone disorders. Beyond their clinical use, their unique bone-targeting capability has positioned them as promising ligands for drug delivery systems aimed at treating bone-related cancers. Approach: The review analyses published studies on BP-functionalized drug delivery systems, including direct drug conjugates, calcium-based nanomaterials, carbon-based nanostructures, and self-assembling systems such as micelles and liposomes. In vitro assays (e.g. hydroxyapatite binding, cell viability) and in vivo biodistribution studies are discussed to evaluate targeting efficiency and …
Novel Micro-And Nanoformulations Of Paclitaxel For Targeting Metastatic Breast, Non-Small Cell Lung, And Pancreatic Cancers, Lobat Tayebi, Mehran Alavi
Novel Micro-And Nanoformulations Of Paclitaxel For Targeting Metastatic Breast, Non-Small Cell Lung, And Pancreatic Cancers, Lobat Tayebi, Mehran Alavi
Electrical & Computer Engineering Faculty Publications
Nonlinear pharmacokinetics resulting from high lipophilic and low oral bioavailability, and hypersensitivity reactions and hyperlipidemia caused by formulation by Cremophor EL have limited clinical effectiveness of paclitaxel (Taxol). In this way, there is the critical necessity of innovative drug delivery systems (DDSs) to mitigate severe side effects and overcome clinical limitations of paclitaxel. In recent years, various micro- and nanoformulations, specifically polymeric nanoparticles (NPs) and lipid NPs, have been presented and approved by the Food and Drug Administration (FDA). In addition, other nanoformulations, such as polymeric nanoparticles (NPs), micelles, liposomes, and mesoporous silica nanoparticles, have shown promising results in vitro …
Protein Marker-Dependent Drug Discovery Targeting Breast Cancer Stem Cells, Ashley V. Huang, Yali Kong, Kan Wang, Milton L. Brown, David Mu
Protein Marker-Dependent Drug Discovery Targeting Breast Cancer Stem Cells, Ashley V. Huang, Yali Kong, Kan Wang, Milton L. Brown, David Mu
Department of Biomedical and Translational Sciences Faculty Publications
Breast cancer is one of the most common cancers globally. Unfortunately, many patients with breast cancer develop resistance to chemotherapy and tumor recurrence, which is primarily driven by breast cancer stem cells (BCSCs). BCSCs behave like stem cells and can self-renew and differentiate into mature tumor cells, enabling the cancer to regrow and metastasize. Key markers like CD44 and aldehyde dehydrogenase-1 (ALDH1), along with pathways like Wingless-related integration site (Wnt), Notch, and Hedgehog, are critical to regulating this stem-like behavior of BCSCs and, thus, are being investigated as targets for various new therapies. This review summarizes marker-dependent strategies for targeting …
High-Throughput Drug Screening For Disease-Modifying Arthritis Therapy, Janapriya Vijayakumar
High-Throughput Drug Screening For Disease-Modifying Arthritis Therapy, Janapriya Vijayakumar
Honors Undergraduate Theses
Current therapy for arthritis predominantly focuses on the symptoms rather than the underlying causes of disease progression. Thus, it is necessary to identify novel drugs which target the underlying molecular basis of such diseases. Using high-throughput cell-based drug screening, we screened 458 different compounds, narrowed down from 811 starting compounds from the NIH Mechanistic Set. We selected drugs from the Mechanistic Set following Lipinski's Rule of 5 to ensure optimal pharmacokinetic properties. The study used modified primary human chondrocytes (IIAM-PRG4Luc), which secrete a lubricin promoter-driven luciferase reporter. We use this luciferase expression as a proxy to measure lubricin, a compound …
Investigation Of Lubricin-Stimulating Fda-Approved Compounds For A Disease-Modifying Osteoarthritic Drug, Swathi S. Menon
Investigation Of Lubricin-Stimulating Fda-Approved Compounds For A Disease-Modifying Osteoarthritic Drug, Swathi S. Menon
Honors Undergraduate Theses
Osteoarthritis (OA) is a degenerative disease that affects many people worldwide. Current methods of treatment are palliative, and no treatment exists to fully reverse or cure OA once it begins to progress. The discovery of a disease-modifying osteoarthritic drug (DMOAD) would increase the quality of life for millions and reduce the need for invasive procedures. Screening FDA-approved drugs ensures more promise due to their known safety profile and potential for faster translation to the clinic. The goal of this project was to conduct dose-response assays with FDA-approved drugs that have been shown to stimulate lubricin production in cells that mimic …
The Short And Sweet On Sodium-Glucose Cotransporter Inhibitors And Glucagon-Like Peptide-1 Receptor Agonists In Heart Failure, Jose L. Batista, Tracy Makuvire, Jonathan D. Davis, Salvatore Carbone
The Short And Sweet On Sodium-Glucose Cotransporter Inhibitors And Glucagon-Like Peptide-1 Receptor Agonists In Heart Failure, Jose L. Batista, Tracy Makuvire, Jonathan D. Davis, Salvatore Carbone
EVMS School of Health Professions Faculty Publications
Heart failure (HF) affects 6 million people in the US, and type 2 diabetes (T2D) is a significant risk factor for HF. Since 2008, regulatory agencies have required cardiovascular safety trials for new T2D therapies, and these have consistently demonstrated the cardiovascular benefits of glucose-lowering drugs. Sodium-glucose cotransporter inhibitors (SGLTi) and glucagon-like peptide-1 (GLP-1) receptor agonists (RAs)/glucose-dependent insulinotropic polypeptide (GIP) reduce major adverse cardiovascular events and deaths, regardless of diabetes status, and improve cardiorespiratory fitness. SGLTis, such as dapagliflozin and empagliflozin, benefit patients with reduced and preserved ejection fraction, significantly reducing HF hospitalizations and cardiovascular deaths. The DAPA-HF and EMPEROR-Reduced …
Synthesis And Evaluation Of Anti-Hiv Activity Of Fatty Acyl Conjugates Of Tenofovir Alefanamide, Muhammad Sajid, Naglaa Salem El-Sayed, Louise A. Ouattara, Amita Verma, Gustavo F. Doncel, Keykavous Parang, M. Iqbal Choudhary, Hina Siddiqui
Synthesis And Evaluation Of Anti-Hiv Activity Of Fatty Acyl Conjugates Of Tenofovir Alefanamide, Muhammad Sajid, Naglaa Salem El-Sayed, Louise A. Ouattara, Amita Verma, Gustavo F. Doncel, Keykavous Parang, M. Iqbal Choudhary, Hina Siddiqui
CONRAD Publications
The activity of nucleoside and nucleotide analogs as antiviral agents requires phosphorylation by intracellular enzymes. Phosphate-substituted analogs have low bioavailability due to the presence of ionizable negatively-charged groups. To circumvent this limitation, several prodrug approaches have been proposed and developed. Herein, we hypothesized that the conjugation of anti-HIV fatty acids with the nucleotide tenofovir alafenamide (TAF) (1) could improve the anti-HIV activity of the nucleotide. Several fatty acyl amide conjugates of TAF were synthesized and evaluated in comparative studies with TAF. The synthesized compounds were evaluated as racemic mixtures for anti-HIV activity in vitro in a single-round HIV-1 infection assay …
Rational Design Of Small Molecules Targeting Mitochondrial Redox Proteins, Matheus Barbosa Belchior
Rational Design Of Small Molecules Targeting Mitochondrial Redox Proteins, Matheus Barbosa Belchior
Graduate Theses, Dissertations, and Problem Reports (ETD)
Reactive oxygen species play a crucial role in many cellular processes. Despite being a natural byproduct of cellular metabolism, overexpression of these species causes damage to the cell, leading to cell dysfunction. Central to the regulation of these highly reactive molecule is the mitochondria. Impairment in its function has been associated with oxidative stress within the cell. Herein, a ligand-based and structure-based approach to design new small molecules to inhibit mitochondrial redox proteins associated with oxidative stress and reactive oxygen species. In the first project two molecules were synthesized and characterized as potential monoamine oxidase B inhibitors. Results showed two …
Development Of Novel Carbohydrate-Based Nanoparticles For Precision Drug Delivery, Krystal Ann Hughes
Development Of Novel Carbohydrate-Based Nanoparticles For Precision Drug Delivery, Krystal Ann Hughes
Graduate Theses, Dissertations, and Problem Reports (ETD)
Nanoparticle-based drug delivery has made tremendous advancements in the last decade. However, several critical factors, including precision drug delivery at the site of interest, long-term storage stability, and controlling release profiles of drugs in the systemic circulation, need to be addressed for successful clinical translation of nanomedicine. This dissertation presents novel carbohydrate-based nanoparticles that achieve precise intracellular delivery and therapeutic release at the disease site. We present the formulation and optimization of polymeric and polymer-lipid hybrid nanoparticles that enable precision intracellular delivery and passive accumulation of therapeutics in the bone marrow. Intracellular delivery is highly impactful and sought after. One …
Association Of Prenatal Exposure To Phthalates And Phenols With Adverse Pregnancy Outcomes, Misa Hayasaka, Diana Aboukhater, George Saade, Tetsuya Kawakita
Association Of Prenatal Exposure To Phthalates And Phenols With Adverse Pregnancy Outcomes, Misa Hayasaka, Diana Aboukhater, George Saade, Tetsuya Kawakita
Department of Obstetrics & Gynecology Faculty Publications
OBJECTIVE:
To evaluate the association between prenatal exposures to phthalates and phenols and adverse pregnancy outcomes, including preterm birth (PTB), small-for-gestational-age (SGA) birth weight, and gestational diabetes mellitus (GDM).
METHODS:
This study analyzed data from the Environmental Influences on Child Health Outcomes consortium, which harmonized longitudinal data on more than 30,000 pregnancies and 57,000 children from 69 cohorts across the United States and Puerto Rico. Pregnancy outcomes included PTB, SGA, and GDM, identified from medical records or self-reports. Generalized estimating equations models with Poisson distribution and robust variance were used to estimate relative risks (RRs) and 95% CIs per interquartile …
Changes In Cardiovascular Risk Factors And Health Care Expenditures Among Patients Prescribed Semaglutide, Yuan Lu, Yuntian Lu, Tedi Totojani, Chungsoo Kim, Rohan Khera, Hua Xu, John E. Brush Jr., Harlan M. Krumholtz, Jason Abaluck
Changes In Cardiovascular Risk Factors And Health Care Expenditures Among Patients Prescribed Semaglutide, Yuan Lu, Yuntian Lu, Tedi Totojani, Chungsoo Kim, Rohan Khera, Hua Xu, John E. Brush Jr., Harlan M. Krumholtz, Jason Abaluck
Department of Medicine Faculty Publications
Importance Semaglutide, a glucagon-like peptide-1 receptor agonist, has demonstrated substantial weight reduction and cardiovascular benefits in clinical trials. However, its association with clinical outcomes and health care expenditures remains underexplored.
Objective To evaluate changes in cardiovascular risk factors and health care expenditures among patients prescribed semaglutide across multicenter cohorts.
Design, Setting, and Participants This retrospective cohort study included 23 522 adults (≥18 years) who received an initial semaglutide prescription between January 1, 2018, and January 1, 2025, at Sentara Healthcare and between January 1, 2018, and May 1, 2025, at Yale New Haven Health System.
Exposure The first prescription of …
Investigating The Bioactivity Potential And Standardization Of Two Stingless Bee Propolis From East Kalimantan, Paula Mariana Kustiawan, Muhammad Ali Syahbana, Rika Pratika, Muhammad Nor Ichsan, Ika Ayu Mentari, Indah Hairunnisa, Irfan Muris Setiawan, Putri Hawa Syaifie, Donny Ramadhan, Chanpen Chanchao
Investigating The Bioactivity Potential And Standardization Of Two Stingless Bee Propolis From East Kalimantan, Paula Mariana Kustiawan, Muhammad Ali Syahbana, Rika Pratika, Muhammad Nor Ichsan, Ika Ayu Mentari, Indah Hairunnisa, Irfan Muris Setiawan, Putri Hawa Syaifie, Donny Ramadhan, Chanpen Chanchao
Pharmaceutical Sciences and Research
The standardization of raw materials from nature is essential before they are made into products. Until now, there is still limited information regarding the standardization of propolis from stingless bees. This research aims to determine the bioactivity with standardized specific and non-specific parameters of ethanol extracts from Homotrigona apicalis and Homotrigona fimbriata propolis. The methods include organoleptic tests, tests for water-soluble and ethanol-soluble compound content, drying shrinkage tests, specific gravity tests, water content tests, metal contamination tests, phytochemical screening, and determining total phenolic and flavonoid content. The free radical scavenging capacity was measured using the DPPH (1,1-diphenyl-2-picrylhydrazyl) method, and antimicrobial …
Utilizing Water Hyacinth (Eichhornia Crassipes) From Srandakan Bantul, Indonesia For ‘Bright Fever Patch’ As An Alternative Children’S Fever Therapy, Anggita Kamalia Niswara, Nabillah Ainun Kusrinanti, Rizqi Amalia Firdaus, Azis Ikhsanudin
Utilizing Water Hyacinth (Eichhornia Crassipes) From Srandakan Bantul, Indonesia For ‘Bright Fever Patch’ As An Alternative Children’S Fever Therapy, Anggita Kamalia Niswara, Nabillah Ainun Kusrinanti, Rizqi Amalia Firdaus, Azis Ikhsanudin
Pharmaceutical Sciences and Research
In 2022, Indonesia experienced a public health crisis involving acute kidney failure in children, traced to paracetamol syrup contaminated with ethylene glycol and diethylene glycol. This underscores the urgent need for safer antipyretic alternatives. This study investigates the antipyretic potential of transdermal patches formulated with ethanol extract of water hyacinth (Eichhornia crassipes) leaves sourced from Srandakan, Bantul, Yogyakarta. Extract concentrations of 0.8%, 1.0%, and 1.2% were tested, alongside a negative control (no extract) and a positive control (paracetamol). The patches underwent evaluations for organoleptic properties, weight uniformity (0.41±0.02 to 0.52±0.02 g), thickness (0.36±0.03 to 0.41±0.03 mm), water absorption …
Optimization Of External Disintegrating Materials In Wet Granulation Formulation Of Ondansetron Tablets, Yandi Permana, Syahrul Tuba, Taufik Riyadi, Sugindro Sugindro
Optimization Of External Disintegrating Materials In Wet Granulation Formulation Of Ondansetron Tablets, Yandi Permana, Syahrul Tuba, Taufik Riyadi, Sugindro Sugindro
Pharmaceutical Sciences and Research
Inadequate management of chemotherapy-induced side effects, including nausea and vomiting, can impact the healing response of cancer patients. Ondansetron, a preferred medication for the treatment, is classified as a biopharmaceutic classification system (BCS) class II drug, which limits its bioavailability. To enhance its solubility, sodium starch glycolate (SSG) and pregelatinized starch (PG) are used as super disintegrants. This study investigates the impact of these super disintegrants on ondansetron dissolution and identifies the optimal formulation. Ondansetron tablets were prepared using the wet granulation method, with nine formulations varying in SSG and PG concentrations (0%, 1%, 3%, 5%, and 7%). The tablets …