Open Access. Powered by Scholars. Published by Universities.®
Pharmaceutics and Drug Design Commons™
Open Access. Powered by Scholars. Published by Universities.®
- Discipline
-
- Other Pharmacy and Pharmaceutical Sciences (22)
- Diseases (17)
- Life Sciences (17)
- Chemicals and Drugs (16)
- Medical Specialties (16)
-
- Medicinal and Pharmaceutical Chemistry (14)
- Nanotechnology (13)
- Medical Sciences (11)
- Amino Acids, Peptides, and Proteins (10)
- Nanomedicine (10)
- Oncology (7)
- Medical Pharmacology (6)
- Natural Products Chemistry and Pharmacognosy (6)
- Nervous System Diseases (6)
- Pharmacology, Toxicology and Environmental Health (6)
- Analytical, Diagnostic and Therapeutic Techniques and Equipment (5)
- Biochemistry, Biophysics, and Structural Biology (5)
- Physical Sciences and Mathematics (5)
- Cell and Developmental Biology (4)
- Therapeutics (4)
- Anatomy (3)
- Biochemistry (3)
- Cell Biology (3)
- Chemistry (3)
- Engineering (3)
- Genetics and Genomics (3)
- Immunology and Infectious Disease (3)
- Institution
-
- Chapman University (10)
- Old Dominion University (10)
- Universitas Indonesia (6)
- Chulalongkorn University (3)
- The British University in Egypt (3)
-
- University of Louisville (3)
- JSS Academy of Higher Education and Research (2)
- Marshall University (2)
- Roseman University of Health Sciences (2)
- University of Central Florida (2)
- University of Nebraska Medical Center (2)
- West Virginia University (2)
- Advocate Health - Midwest (1)
- Baptist Health South Florida (1)
- Bentley University (1)
- Binghamton University (1)
- Bulletin of the Faculty of Pharmacy Cairo University (1)
- Claremont Colleges (1)
- Duke Law (1)
- Duquesne University (1)
- LSU Health New Orleans (1)
- Louisiana State University (1)
- Medical University of South Carolina (1)
- Ohio Northern University (1)
- Pepperdine University (1)
- The University of Southern Mississippi (1)
- Thomas Jefferson University (1)
- University of Connecticut (1)
- University of Lynchburg (1)
- University of Mississippi (1)
- Keyword
-
- Drug delivery (4)
- Drug development (3)
- Humans (3)
- Nanotechnology (3)
- Wound healing (3)
-
- Bioavailability (2)
- Cancer (2)
- Cartilage (2)
- Drug discovery/methods (2)
- Female (2)
- Growth factors (2)
- Heart failure (2)
- Lubricin (2)
- Molecular dynamics (2)
- Osteoarthritis (2)
- Selenium nanoparticles (2)
- Targeted drug delivery (2)
- 28-day toxicology study (1)
- 5-Fluorouracil (5-FU) (1)
- 8-steps (1)
- <p>Drugs -- Research.</p> <p>Disulfiram.</p> <p>Antibiotics.</p> <p>Drug resistance in microorganisms.</p> <p>Anti-infective agents.</p> <p>Aspergillus.</p> <p>Pharmacology.</p> (1)
- <p>Pharmaceutical chemistry.</p> <p>Chitosan.</p> <p>Wound healing.</p> <p>Aleppo oak.</p> <p>Fluorouracil.</p> <p>Emulsions.</p> <p>Nanoscience.</p> (1)
- ADC (1)
- ADKAR (1)
- AMPs (1)
- Acarbose (1)
- Acquired resistance (1)
- Adjuvant (1)
- Adult (1)
- Adverse effects (1)
- Publication
-
- Pharmacy Faculty Articles and Research (10)
- Pharmaceutical Sciences and Research (6)
- Electronic Theses and Dissertations (4)
- The Thai Journal of Pharmaceutical Sciences (3)
- Annual Research Symposium (2)
-
- Electrical & Computer Engineering Faculty Publications (2)
- Graduate Theses, Dissertations, and Problem Reports (ETD) (2)
- Honors Undergraduate Theses (2)
- International Journal of Health and Allied Sciences (2)
- Pharmacy (2)
- Theses & Dissertations (2)
- Theses, Dissertations and Capstones (2)
- Bulletin of Faculty of Pharmacy Cairo University (1)
- CISI Publication (1)
- CONRAD Publications (1)
- Center for Bioelectronics Publications (1)
- Computer Science Faculty Publications (1)
- Department of Biochemistry and Molecular Biology Faculty Papers (1)
- Department of Biomedical and Translational Sciences Faculty Publications (1)
- Department of Medicine Faculty Publications (1)
- Department of Obstetrics & Gynecology Faculty Publications (1)
- Doctoral Projects (1)
- EVMS School of Health Professions Faculty Publications (1)
- Faculty Scholarship (1)
- Honors Scholar Theses (1)
- Honors Theses (1)
- Honors Thesis (1)
- Journal of Patient-Centered Research and Reviews (1)
- LSU Master's Theses (1)
- Lynchburg Journal of Medical Science (1)
- Publication Type
Articles 31 - 60 of 66
Full-Text Articles in Pharmaceutics and Drug Design
Investigating The Cytotoxic Effects Of Amino Acid-Based Ionic Liquids And Peg-Pla Nanoparticles On Mcf10a Human Breast Epithelial Cells For Drug Delivery Applications, Ella C. Mertins
Honors Theses
This study investigates the cytotoxic effects of polyethylene glycol-polylactic acid (PEG-PLA) nanoparticles (NPs) both bare and coated with choline-based ionic liquids (ILs) on MCF10A human breast epithelial cells. The goal was to evaluate how IL-modified NPs influence cell viability at varying concentrations and to assess their potential as drug delivery systems. Three choline-based ILs, Choline-L-Asparagine 1:1, Choline-DL-Isoleucinate 1:1, and Choline-L-Leucinate 1:1, were used as surface coatings for PEG-PLA NPs. Additionally, the ILs were tested independently to establish a baseline for their cytotoxicity. Using a luminescent ATP-based viability assay following the treatment of MCF10A cells, the ILs were found to be …
The Endocannabinoid System's Influence And Modulation Of Nociception, Doreen M. Flannery
The Endocannabinoid System's Influence And Modulation Of Nociception, Doreen M. Flannery
Honors Thesis
The anatomy and physiology of pain is a well-defined pathway where noxious stimuli is processed by different systems in the brain. The central research question of this review is how can we better understand the neurobiological effects pain has, and assess if there is therapeutic potential in using endocannabinoids to modulate these effects. Endocannabinoids are signaling molecules that play a key role at both the cellular and molecular level in modulating both acute and chronic pain by influencing different processes within each level that affect how the body responds to both internal and external stimuli. The endocannabinoid system is a …
Application Of Bioactive Materials Primary Cilia As A Novel Delivery Vehicle, Ayan K. Barui, Farideh Amirrad, Vansh Goel, Sharareh Ohadi, Rajasekharreddy Pala, Ashraf M. Mohieldin, Andromeda M. Nauli, Surya M. Nauli
Application Of Bioactive Materials Primary Cilia As A Novel Delivery Vehicle, Ayan K. Barui, Farideh Amirrad, Vansh Goel, Sharareh Ohadi, Rajasekharreddy Pala, Ashraf M. Mohieldin, Andromeda M. Nauli, Surya M. Nauli
Pharmacy Faculty Articles and Research
Primary cilia are hair-like structured cell organelles functioning as cellular antennae with chemosensory and mechanosensory roles. Dysfunction of cilia results in ciliopathies, including renovascular diseases (polycystic kidneys, hypertension, aneurysm), mental impedances (Alzheimer's disease, Parkinson's disease, dementia), metabolic diseases (obesity, developmental skeleton defects), blindness, and so on. With a diameter of 150 nm, cilia can be cleaved, released and circulated in the body as injury biomarkers. We here assessed the potential use of isolated cilia as a novel delivery vehicle. Cilia were isolated from renal epithelial cells, and a specific-targeting chemotherapeutic was designed on the cilia. The data show a remarkable …
Valproic Acid Loaded Niosomal In Situ Gel: A Novel Approach For Epilepsy Treatment, Rutuja Bastapure, Akshay Gawali, Gopal Lohiya, Kranti Satpute, Mahesh Birajdar, Sameep Sonvane
Valproic Acid Loaded Niosomal In Situ Gel: A Novel Approach For Epilepsy Treatment, Rutuja Bastapure, Akshay Gawali, Gopal Lohiya, Kranti Satpute, Mahesh Birajdar, Sameep Sonvane
International Journal of Health and Allied Sciences
Valproic acid is an antiepileptic medication that is primarily used to treat epilepsy and bipolar disorder. This investigation was designed with three objectives in mind. First, improve the solubility and bioavailability of the BCS class II medicine valproic acid; second, make it easy to give the drug to an epileptic patient during an episode; and third, lower the dosage for long-term treatment. Niosomal formulations were optimized using various Tween and Span range ratios. The formulations were made using the ether injection method. The formulation's morphological characterization, entrapment efficiency, viscosity, and particle size were evaluated. Valproic acid niosomes prepared with Tween …
Development And Assessment Of Liposomal Nasal Spray For The Treatment Epilepsy, Sayali Dongare, Sushmaji Sontakke, Gopal Lohiya, Shoeb Syed, Rohit Sarda
Development And Assessment Of Liposomal Nasal Spray For The Treatment Epilepsy, Sayali Dongare, Sushmaji Sontakke, Gopal Lohiya, Shoeb Syed, Rohit Sarda
International Journal of Health and Allied Sciences
Abstract:
Background: Levetiracetam is a pyrrolidine class antiepileptic drug mainly used to treat epilepsy and seizures.
Objective: The purpose of this research was to synthesize a liposomal nasal spray incorporating levetiracetam for nose to brain delivery in epilepsy.
Materials and methods: The preparation method employed thin film hydration to prepare liposomes loaded with levetiracetam with lecithin and tween 80 at different concentrations. The liposome formed were characterized in terms of particle size and entrapment efficiency. Finally, the prepared liposomes were converted into nasal spray and characterized for drug content, pH, viscosity, in vitro release profile, clarity, Ex-vivo permeation study. …
Fluorescent Labeling And Size-Dependent Uptake Of Mesoporous Silica Nanoparticles In Ovarian Cancer Tumor Spheroids, Kimberly R. Berardis
Fluorescent Labeling And Size-Dependent Uptake Of Mesoporous Silica Nanoparticles In Ovarian Cancer Tumor Spheroids, Kimberly R. Berardis
Honors Scholar Theses
Ovarian cancer is the most lethal gynecologic malignancy, with most patients presenting at an advanced stage. While surgical debulking improves survival, nonresectable tumors (<1 cm) contribute significantly to morbidity and remain difficult to treat. Nanocarrier-based drug delivery systems offer an innovative approach to targeted therapy and palliation. In vivo models have demonstrated that intraperitoneally delivered mesoporous silica nanoparticles (MSNs) preferentially accumulate in tumors with low systemic exposure, enabling targeted chemo- and radiotherapy.
MSNs are particularly suited for radiotherapeutic delivery, as their strong interactions with tumor extracellular matrices drive selective uptake. Additionally, they exhibit excellent stability under neutron flux, allowing for loading with stable isotopes and irradiation immediately prior to administration. High radionuclide retention after dilution further minimizes systemic exposure and toxicity.
A key …
Studies To Understand The Stability And Liabilities Of Legumain-Cleavable Antibody-Drug Conjugates, Michele Yi
Studies To Understand The Stability And Liabilities Of Legumain-Cleavable Antibody-Drug Conjugates, Michele Yi
Undergraduate Honors Theses
Antibody-drug conjugates (ADCs) offer targeted drug delivery of potent cytotoxic payloads, minimizing systemic toxicity. However, the stability of the linker is integral to ensure that there is minimal off-target payload release and little systemic toxicity. This study analyzes the physical and biological stability of our new legumain-cleavable vs traditional cathepsin-cleavable antibody-drug conjugates (ADCs), with a focus on hydrophobicity, thermal stability, aggregation, and biological payload release. Our findings indicate that decreased hydrophobicity of the legumain-cleavable ADCs compared to cathepsin-cleavable ADCs is correlated with decreased aggregation (predicting lower uptake by liver macrophages and therefore slower clearance and less systemic toxicity) and lower …
Advancing A Patient- And Carer-Centered Approach For The Clinical Development Of New Therapeutics For Aneurysmal Subarachnoid Hemorrhage: Insights From A Qualitative Study, Sonya Abraham, Silvia Amaro, Ellyn Getz, Sylvia Herget, Gregory J. Kato
Advancing A Patient- And Carer-Centered Approach For The Clinical Development Of New Therapeutics For Aneurysmal Subarachnoid Hemorrhage: Insights From A Qualitative Study, Sonya Abraham, Silvia Amaro, Ellyn Getz, Sylvia Herget, Gregory J. Kato
Journal of Patient-Centered Research and Reviews
Aneurysmal subarachnoid hemorrhage (aSAH) is characterized by a high rate of fatality and high risk of secondary brain injury. More treatment options are needed to improve outcomes. There are very few reports in the medical literature involving patient experience of aSAH, which is known for its unexpected onset and profound medical impact. Improved understanding of this patient experience would help make future clinical research more patient centered. To this end, we convened an advisory board consisting of aSAH patients and care partners in the United States. Participants emphasized the critical role that care partners play during hospitalization and in accessing …
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 …
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 …
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 …
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 …
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 …
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 …
Optimization Of Chitosan Nanoemulsion And Its Application In Delivering 5-Fluorouracil And Quercus Infectoria For Wound Healing, Kalkedan Ameha
Optimization Of Chitosan Nanoemulsion And Its Application In Delivering 5-Fluorouracil And Quercus Infectoria For Wound Healing, Kalkedan Ameha
Theses, Dissertations and Capstones
BACKGROUND: Chitosan-based nanoemulsions are increasingly recognized for their potential in enhancing drug delivery for wound healing applications. The integration of Quercus infectoria (Qi) extract, known for its antibacterial and anti-inflammatory effects, with 5- fluorouracil (5-FU), a chemotherapeutic agent that regulates abnormal cell proliferation, presents a synergistic approach for treating chronic and non-healing wounds. Ensuring long-term physicochemical stability of these nanoemulsions is critical for their therapeutic viability.
OBJECTIVE: To optimize and characterize a chitosan-based nanoemulsion for the codelivery of 5-FU and Quercus infectoria extract, with emphasis on physicochemical properties including particle size, polydispersity index (PDI), and zeta potential. The …
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 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 …
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 …