Pharmaceutics and Drug Design Commons^™

Avaren-Fc's Effects On Lymphoma Cells., Jacob Hahn

Electronic Theses and Dissertations

This thesis investigates the therapeutic potential of Avaren-Fc (AvFc), a novel lectin fusion protein that integrates the Fc region of human IgG1 with the engineered lectin Avaren, specifically targeting lymphoma. The study delineates the in vitro binding capabilities of Avaren-Fc with a human B-cell lymphoma cell line, a canine B-cell lymphoma cell line, healthy canine peripheral blood mononuclear cells (PBMCs), and healthy human PBMCs. AvFc was shown to exhibit significant binding to human lymphoma cells. Furthermore, the direct cytotoxicity of Avaren-Fc against canine lymphoma cells, canine lymphoma cells and healthy canine PBMCs was assessed. It was found that there is …

Safety Evaluation Of Epicertin, An Oral Biotherapeutic Candidate For Treating Ulcerative Colitis: A 28-Day Repeated Dose Toxicity Study., Jimmy Fernando Cifuentes Jimenez

Electronic Theses and Dissertations

Ulcerative colitis (UC) is an inflammatory bowel disease characterized by chronic, relapsing inflammation of the colon and rectum with limited treatment options. Among them, immunosuppressive agents have a high rate of adverse side effects and do not cure the disease. EPICERTIN (EPT), a recombinant variant of the cholera toxin B subunit (CTB) with a C-terminal hexapeptide extension consisting of a KDEL endoplasmic reticulum (ER) retention motif, is a promising oral biotherapeutic candidate for the treatment of UC. EPT has demonstrated mucosal healing activity in mouse models of colitis and human colonic explants. EPT's mechanism of action involves binding to GM1 …

Breastfeeding Safety Following Maternal Anesthesia: A Guideline Development, Megan Honea, Mary Johnson

Doctoral Projects

Recommendations regarding breastfeeding following maternal anesthesia are inconsistent and often not up to date with current best practice guidelines. Previous recommendations have led to mothers unnecessarily “pumping and dumping” breast milk has benefits for both mother and baby. These benefits include (a) increasing the infant’s access to colostrum, (b) encouraging mother-baby bonding, (c) improving the mother’s breastfeeding experience, (d) and providing significant health benefits to the infant. The purpose of this scholarly project was to develop a set of evidence-based recommendations that focus on mothers who desire to breastfeed following general anesthesia. These recommendations will highlight maternal- fetal transfer of …

Development And Optimization Of Moxifloxacin Solid Lipid Nanoparticles Via Double Emulsion Organic Solvent Free Technique Applying Box–Behnken Experimental Design, Esraa M. Elshazly, Mona G. Arafa, Samia A. Nour

Pharmacy

The current research proposes the preparation of Moxifloxacin-loaded solid lipid nanoparticles through a solvent-free double emulsion technique, to overcome chronic wound healing limitation. The independent variables: stearic acid, Span 80, and Tween 80 were optimized via Box–Behnken design, based on entrapment efficiency (EE%), zeta potential (ZP), and particle size (PS). To statistically optimize the formulation variables, a three-factor, three-level (3³) design involving 15 runs was employed and optimization was carried out to attain maximum EE% and ZP and minimum PS yielding an overall desirability of 0.851. Results indicated that increasing stearic acid enhanced EE%, Span 80 increase PS, and Tween …

Assessment Of Stroke Priority Status On Door-To-Reversal Time And Outcomes In Anticoagulant Associated Intracranial Hemorrhage, Kayla Mitzel, Jonathan Kline, Thomas J. Wolfel, Erika Dittmar, Nina Cruz, Felipe De Los Rios La Rosa, Heidi Clarke

Nursing & Health Sciences Research Journal

Background: The emergent reversal of anticoagulation in the setting of intracranial hemorrhage (ICH) is critical, and it is essential that comprehensive stroke centers adhere to the American Heart Association (AHA) metrics for door-to-reversal within the designated 90 minutes. The objective of this review is to evaluate individuals classified as stroke alert priority 1 and non-stroke alert and compare AHA metrics for door-to-reversal times and clinical outcomes when diagnosed with ICH.

Methods: Single-center observational, retrospective review that compared stroke alert priority 1 individuals to non-stroke alert individuals who were diagnosed with an ICH and taking an anticoagulant prior to admission. The …

Advancing Herbal Medicine: The Role Of Nanosomal Technology In Treating Skin Diseases, Pedro Anugerah Aswan, Baitha Palanggatan Maggadani, Wilzar Fachri, Raditya Iswandana

Pharmaceutical Sciences and Research

Herbal medicine has become popular worldwide, especially in developing countries, with around 80% of the population opting for herbal treatments. The perceived benefits of natural remedies, such as affordability and fewer side effects, drive this trend. Herbal therapies effectively manage skin diseases, infections, and common ailments. However, the absorption of bioactive compounds in herbal extracts is often limited. Recent developments in nano-based herbal delivery systems, like nanosomal, show promise in enhancing the efficacy of herbal remedies for topical applications, providing improved solubility, stability, and skin penetration. This review describes various nanosomal studies developed and successfully used to enhance the topical …

Exploring The Vitronectin Binding Affinity And Cell Viability Effect Of Small Molecule Metabolites From Medicinal Plants For Neuroblastoma, Stephenie C. A Alaribe, Sofia Granados-Aparici, Akolade R. Oladipupo, Isaac Vieco-Marti, Blessing E. Titilayo, Gordon Allen, Rosa Noguera

Pharmaceutical Sciences and Research

High-risk neuroblastoma (HR-NB) is an aggressive form of childhood cancer with a five-year survival rate of less than 50%, underscoring the need for more efficacious and less toxic treatments. The glycoprotein vitronectin (VN) has been linked to poor prognosis in patients with HR-NB, thus inhibitors of VN function represent a promising avenue for molecular mechanotherapy. This study investigated the binding affinity between the somatomedin B (SMB) domain of VN and natural compounds from the medicinal plant, Olax subscorpioidea, targeting the plasminogen activator inhibitor-1 (PAI-1). The therapeutic potential of α-amyrin (AMY), lupeol (LUP), and olax chalcone A (olax CHA) was tested …

Formulation And In Vitro Evaluation Of Kaffir Lime Fruit Peel Extract-Containing Gel For Sunscreen, Antioxidant, And Moisturizing Activity, Farida Lanawati Darsono, Lisa Soegianto

Pharmaceutical Sciences and Research

Kaffir lime peel waste (Citrus hystrix) has antioxidant effects that have the potential to protect the skin from exposure to UV-A and UV-B rays, as well as moisturize the skin. This study aims to determine the effect of increasing the concentration of condensed extract of kaffir lime fruit peel on its effectiveness as an antioxidant, sunscreen activity, and moisturizer. The condensed extract was obtained by maceration using 96% ethanol. In this study, we tested hydrophilic gels consisting of 4 extract concentrations in their formula: F1 (7.5%), F2 (10%), F3 (15%), and F4 (20%). The research phase begins with …

Additive Effects Of N-Acetylcysteine And [R4W4] Combination Treatment On Mycobacterium Avium, Kayvan Sasaninia, Iffat Hasnin Era, Nezam Newman, Jesse Melendez, Wajiha Akif, Eashan Sharma, Omid Nikjeh, Ira Glassman, Cristián Jiménez, Navya Sharma, Ama Xu, Maria Lambros, Miou Zhou, Rakesh Tiwari, Vishwanath Venketaraman

Pharmacy Faculty Articles and Research

Mycobacterium avium is an opportunistic pathogen and a leading contributor to nontuberculous mycobacterial infections in immunocompromised individuals. However, treatment duration, antibiotic toxicity, and resistance present challenges in the management of mycobacterium infections, prompting the need for novel treatment. N-acetylcysteine (NAC) has demonstrated potent antimycobacterial activity, while antimicrobial peptides such as the cyclic [R₄W₄] have shown additive effects when combined with first-line antibiotics. This study aimed to investigate the mechanism and efficacy of NAC and [R₄W₄] combination therapy against M. avium. A membrane depolarization assay was used to evaluate the effects of …

Dual Membrane Receptor Degradation Via Folate Receptor Targeting Chimera, Zhen Wang, Zhixin Li, Jenny Högström, Hiroyuki Inuzuka, Rui Jing, Peiqiang Yan, Tao Hou, Yihang Qi, Daoyuan Huang, Jingchao Wang, Ting Wu, Xiaoying Shi, Bolin Liu, Taru Muranen, Dingpeng Zhang, Wenyi Wei

School of Medicine Faculty Publications

Cancer drug resistance poses a significant challenge in oncology, often driven by intricate cross-talk among membrane-bound receptors that compromise mono-targeted therapies. We develop a dual membrane receptor degradation strategy leveraging Folate Receptor α (FRα) to address this issue. Folate Receptor α Targeting Chimeras-dual (FolTAC-dual) are engineered degraders designed to selectively and simultaneously degrade distinct receptor pairs: (1) EGFR/HER2 and (2) PD-L1/VISTA. Through modular optimization of modality configurations and geometries, we identify the “string” format as the most effective construct. Mechanistic studies demonstrate an ~85% increase in EGFR-binding affinity compared to the conventional knob-into-hole design, likely contributing to the improved efficiency …

Predictive Gene Expression Signatures For Alzheimer's Disease Using Post-Mortem Brain Tissue, Ashley Duche, Oliver Tan, Andrius Baskys, Rachita K. Sumbria, Moom R. Roosan

Pharmacy Faculty Articles and Research

Background: Alzheimer’s Disease (AD) is a progressive neurodegenerative disorder characterized by amyloid-beta (Aβ) plaques and tau protein aggregates in the brain. These pathological features manifest in specific regions, but mechanisms rendering some areas more susceptible to early AD-related changes remain poorly understood. To address this, we developed predictive gene expression signatures to explore molecular mechanisms underlying regional vulnerability to AD pathology.

Methods: Post-mortem brain tissues from participants of the Religious Orders Study and Memory and Aging Project (ROSMAP), Mayo Clinic, and Mount Sinai Brain Bank (MSBB) were used to derive gene expression signatures from six brain regions affected at varying …

Editorial: Molecular Mechanisms Of Ion Channel Activation And Modulation, Meng Cui, Miao Zhang

Pharmacy Faculty Articles and Research

"Ion channels are integral membrane proteins that regulate the passage of ions across cell membranes, thereby shaping processes as diverse as neuronal signaling, muscle contraction, and hormone secretion. Channel activation is typically initiated by a stimulus such as voltage, ligand binding, or mechanical stress that induces conformational changes and opens the channel pore. Beyond activation, channels are subject to fine-tuned modulation by a wide range of endogenous and exogenous agents, from lipids and neurotransmitters to pharmacological drugs. Modulators can stabilize the open, closed, or inactivated states, shift ligand affinities, or alter gating kinetics. Dissecting the structural and dynamic basis of …

Smart Dressings Accelerating Wound Healing With Tranexamic Acid-Infused Aligned Electrospun Nanofibers: In Vitro And In Vivo Assessments, Samar A. Salim, Abdullah Elbadry, Eman Gomaa, Mennatullah Faisal, Elbadawy A. Kamoun

Nanotechnology Research Centre

The development of advanced wound dressings capable of accelerating healing and achieving effective hemostasis remains a critical challenge in managing traumatic and surgical wounds. This study reports the fabrication and comprehensive evaluation of a novel multilayered, sandwich-structured nanofiber scaffold composed of Tranexamic acid (TXA), chitosan (CS), polyvinyl alcohol (PVA), L-arginine, and polylactic acid (PLA) for biodegradable wound dressing applications. Using sequential electrospinning, a four-layered scaffold was developed as a smart wound dressing, comprising an immediate-release TXA-CS-PVA layer for rapid clotting, a hydrophobic PLA barrier layer for protection, a sustained-release L-arginine-PVA layer to promote tissue regeneration, and a final PLA protective …

Peptide-Based Inorganic Nanoparticles As Efficient Intracellular Delivery Systems, Amir Nasrolahi Shirazi, Rajesh Vadlapatla, Ajoy Koomer, Anthony Nguyen, Vian Khoury, Keykavous Parang

Pharmacy Faculty Articles and Research

Background/Objectives: Peptide-based inorganic nanoparticles (PINPs) have emerged as promising candidates for intracellular delivery due to their unique structural and functional attributes. These hybrid nanostructures combine the high surface area and tunable optical/magnetic properties of metal cores (e.g., Au, Ag, Fe3O4) with the biocompatibility, targeting specificity, and responsive behavior of peptides. In particular, peptides with amphipathic or cell-penetrating features could facilitate efficient transport of molecular cargos across cellular membranes while enabling stimulus-responsive drug release in target tissues. Methods: We review key synthesis methods (especially green, peptide-mediated one-pot approaches), functionalization strategies (e.g., thiol-gold bonds, click chemistries), and characterization techniques (TEM, …

The 9th Annual Lafora Science Symposium: A Rare Epilepsy Community Makes Progress Towards Clinical Readiness, Meredith I. Williams, Katherine J. Donahue, Pascual Sanz, Souad Messahel, Jose M. Serratosa, Jordi Duran, Roberto Michelucci, Lorenzo Muccioli, Antonio Delgado-Escueta, Viet-Hong Nguyen, Berge A. Minassian, Matthew S. Gentry

Pharmacy Faculty Articles and Research

Lafora disease (LD) is a fatal childhood progressive myoclonus epilepsy and glycogen storage disease that is caused by recessive mutations in either EPM2A or EPM2B. The hallmarks of LD are cytoplasmic, aberrant glycogen-like aggregates, called Lafora bodies (LBs), that drive disease progression. The 9th Annual Lafora Science Symposium was held in San Diego, California and brought together over 70 researchers, clinicians, academic trainees, and friends and family members of patients with LD and 80 attendees joined virtually. This symposium focused primarily on international collaborations for therapeutic development and biomarker identification and strategies for preparing the Lafora community for upcoming …

Cbl Regulation Of C-Met Signaling In Corneal Epithelial Cells., Kate Elise Tarvestad Laise

Electronic Theses and Dissertations

The cornea is the most anterior portion of the eye and permits light passage through to retina, allowing formation of a clear image as long as it remains healthy. If the cornea sustains damage, it creates and entrance for foreign body invasion, infection, and ultimately blindness in the immunocompromised eye. Healing the corneal tissue is critical for vision restoration and pain alleviation, as it is the most densely innervated tissue in the body. Growth factors and their cognate receptors are currently under investigation as tools to restore proper corneal physiology. We hypothesize that manipulating the hepatocyte growth factor (HGF) /c-Met …

Lipid Nanoparticle-Mediated Drug Delivery To Cns Targets, Purva Khare

Electronic Theses and Dissertations

Lipid nanoparticles (LNPs) have revolutionized drug delivery, particularly in the delivery of gene silencing siRNA to the liver (Onpattro) and COVID-19 mRNA vaccines (Pfizer-BioNTech, Moderna). It is no exaggeration to state that the LNP delivery technology has protected billions of vaccinated people against a severe COVID-19 infection and subsequent mortality. Despite extensive research on LNPs for hepatic and muscle delivery, their potential for brain drug delivery remains underexplored. Many neurological disorders lack effective treatments, making LNP-based approaches promising for crossing or targeting drug delivery to the blood-brain barrier (BBB). Brain endothelial cells (BECs), a key component of the BBB, play …

In Vitro Α-Glucosidase Enzyme Inhibition Activity Test Of Water Extract From Sintok (Cinnamomum Sintoc Blume) Bark, Astrella Amanda Putri Saksono, Inana Ratu Soripada Simanjuntak, Mariana Wahjudi, Marisca Evalina Gondokesumo

Pharmaceutical Sciences and Research

Diabetes mellitus is a condition characterized by elevated blood glucose levels beyond the normal limits. One therapeutic approach for managing diabetes mellitus involves inhibiting the α-glucosidase enzyme, which plays a role in glucose absorption in the body. However, the use of oral antidiabetic drugs from the α-glucosidase inhibitor class often causes gastrointestinal side effects. Therefore, exploring natural materials as alternative treatments is a promising option. In Indonesia, one plant with potential as an alternative treatment is sintok (Cinnamomum sintoc Blume), a member of the Cinnamomum genus, which is widely utilized in traditional medicine for chronic diseases such as …

Potential Of Legume Seeds From The Leguminosae Family As Material Source Of Food And Medicine : A Literature Review, Ni Made Ayu Gangga Dewi, Nina Dewi Oktaviyanti, Aurapa Sakulpanich, Kartini Kartini

Pharmaceutical Sciences and Research

Leguminosae, also known as Fabaceae, is the third largest plant family after Orchidaceae and Asteraceae. This review aimed to explore the potential of several legume species indigenous to Indonesia, from the Leguminosae family, as sources of food and medicine. The data used for the analysis were collected from various online databases such as PubMed, ScienceDirect, and Google Scholar. The results showed that there were 13 species of Leguminosae family plants found easily in Indonesia including Cajanus cajan, Canavalia ensiformis, Mucuna pruriens, Arachis hypogaea, Vigna subterranea, Glycine max, Phaseolus vulgaris, Phaseolus lunatus, Vigna radiata, Vigna unguiculata subsp. unguiculata, Vigna angularis, Vigna …

Optimization Of Formula, Stability Testing, And Antioxidant Activity Of Clay Masks As Skin Moisturizers, Naniek Widyaningrum, Agung Dwi Anggoro Bhakti, Alghafiqy Harya Evan Maulana, Amalia Safitri, Adinda Fajrah Ramadhani, Anisa Febriani, Anggit Naufal Hanafi, Thendi Abdul Arief

Pharmaceutical Sciences and Research

Clay masks are cosmetic formulations designed to adhere closely to the skin, effectively lifting contaminants, cleansing the face, and absorbing impurities. We made a clay mask containing active ingredients such as niacinamide, alpha arbutin, ceramide, and hyaluronic acid. A careful selection of ingredients is essential for ensuring safety and mitigating potential dermatological issues. This study aimed to evaluate the physical characteristics, stability, primary irritation potential, and moisturizing efficacy of this clay mask formulation. Kaolin and bentonite are the primary base materials. The research included formulation optimization and physical stability testing using a cycling test, where each cycle was conducted over …